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Plural ring nitrogens in the bicyclo ring system

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514228800 - Hetero ring is six-membered and includes at least nitrogen and oxygen as ring hetero atoms (e.g., monocyclic 1,2- and 1,3-oxazines, etc.)

514231200 - Morpholines (i.e., fully hydrogenated 1,4- oxazines)

514231500 - Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding

514232800 - Polycyclo ring system having the additional hetero ring as one of the cyclos

514233500 - Bicyclo ring system having the additional hetero ring as one of the cyclos

514233800 - Plural ring hetero atoms in the bicyclo ring system

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514234800 Quinoxalines (including hydrogenated) 24
Entries
DocumentTitleDate
20110183973Novel Compounds - The invention is directed to certain novel compounds directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.07-28-2011
20110201608SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES - The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof,08-18-2011
20130029985Novel Compounds - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):01-31-2013
20100160314Small Molecule Inhibitors of Toll-Like Receptor 9 - Small molecule compounds and compositions containing said compounds useful for inhibiting signaling by certain Toll-like receptors (TLRs), particularly TLR9, are provided. The compounds and compositions can be used to inhibit immune responses, including unwanted immune responses in particular. Compounds, compositions, and methods are provided to treat a variety of conditions involving unwanted immune responses, including for example autoimmune disease, inflammation, transplant rejection, and sepsis.06-24-2010
20090192155Identification of Compounds Suitable for Treating Ad - The invention provides a method of screening for compounds which inhibit the hyperphosphorylation of tau, and hence are suitable for treating AD and related conditions.07-30-2009
20110195964NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.08-11-2011
20100075960BENZIMIDAZOLE THIOPHENE COMPOUNDS - The present invention provides bezimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.03-25-2010
20120245175MK2 INHIBITORS - The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.09-27-2012
20120245173INHIBITION OF ACTIVATED CDC42-ASSOCIATED KINASE 1 - Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided.09-27-2012
20120245172HETEROCYCLIC AMINE DERIVATIVES - The present invention relates to compounds of formula I09-27-2012
20090005378PYRROLO-PYRIDINE KINASE MODULATORS - The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity.01-01-2009
20130035337FUSED BICYCLIC HETEROARYL DERIVATIVE - The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ.02-07-2013
200900622785- OR 6-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION - The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula03-05-2009
201001056795-PYRIDINONE SUBSTITUTED INDAZOLES - Various 5-substituted 1-substituted indazoles are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.04-29-2010
20100105678NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.04-29-2010
20090042880NOVEL 4-BENZIMIDAZOL-2-YLPYRIDAZIN-3-ONE DERIVATIVES - Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R02-12-2009
20090124615Benzimidazole Thiophene Compounds - The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.05-14-2009
20100130493COMBINATION OF VEGF RECEPTOR TYROSINE KINASE INHIBITORS FOR TREATMENT OF CANCER - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of ZD6474 in combination with ZD1839; to a pharmaceutical composition comprising ZD6474 and ZD1839; to a combination product comprising ZD6474 and ZD1839 for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and ZD1839; to the use of ZD6474 and ZD1839 in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.05-27-2010
20130090337CRYSTAL OF AMIDE COMPOUND - Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43±0.2, 7.62±0.2 and 4.32±0.2 angstroms.04-11-2013
201002737936-ARYL/HETEROALKYLOXY BENZOTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES, METHOD FOR PREPARING SAME, APPLICATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS c-MET INHIBITORS - The disclosure relates to compounds of formula (I):10-28-2010
20130072483SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I03-21-2013
20130072484TYROSINE KINASE INHIBITORS AS ANTI-KINETOPLASTID AND ANTI-APICOMPLEXAN AGENTS - The present invention provides methods of killing, inhibiting the growth, and/or inhibiting the reproduction of kinetoplastid or apicomplexan protozoan with tyrosine kinase inhibitors.03-21-2013
20130059850AZA-INDOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH - The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.03-07-2013
20080280899Inhibitors of Akt Activity - The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.11-13-2008
20090298824Organic compounds - Compounds of formula I12-03-2009
20090270390PYRIMIDINE DERIVATIVES - The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R10-29-2009
20120225870METHODS FOR TREATING CANCER RESISTANT TO ERBB THERAPEUTICS - Provided herein are methods for treating cancer that is resistant to treatment with an anti-ErbB therapeutic agent and which is associated with an activating MET gene mutation or a MET gene amplification. The methods involve administering to a subject a combination of an anti-ErbB therapeutic and an anti-MET therapeutic. Also provided are methods for reducing ErbB mediated signaling or PI3 kinase mediated signaling in a cancer cell.09-06-2012
20130065896FUSED IMIDAZOLE DERIVATIVE - Provided is a novel compound which shows an antagonistic effect against T-type calcium channels, and is useful as a pharmaceutical product.03-14-2013
20090023725Fused Heteroaryl Derivatives for Use as P38 Kinase Inhibitors - Compounds of formula (I):01-22-2009
20090018130Derivatives of 5-Aryl-1H-Pyrrolo [2, 3B] Pyridine-3-Carboxamide or 5-Aryl-1H-Pyrrolo [2, 3B] Pyridine-3-Carboxylic Acid - The present invention relates to new compounds of formula I as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.01-15-2009
200902036905-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,08-13-2009
200900120843-CINNOLINECARBOXAMIDE DERIVATIVES AND THEIR USE FOR TREATING CANCER - The invention relates to chemical compounds of formula (I):01-08-2009
20090012083N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - Disclosed are N-aroyl cyclic amine derivatives having the formula:01-08-2009
20090012082Mediators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.01-08-2009
20080312229Organic Compounds - There are provided according to the invention compounds of formula (I)12-18-2008
20120238571INDAZOLE DERIVATIVES AS PI 3-KINASE - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):09-20-2012
20120238570INHIBITORS OF THE HEDGEHOG PATHWAY - The present invention is directed to a compound of Formula I09-20-2012
20120238569THIAZOLE AND THIOPHENE COMPOUNDS - Provided herein are compounds of the formula (I):09-20-2012
20130165440JAK1 Inhibitors - JAK1 inhibitors of structural formula (I), wherein Ar06-27-2013
20080293715Therapeutic Pyrazolo[3,4-b]Pyridines and Indazoles - The present invention provides for compounds of Formula I:11-27-2008
20100004239Pyrrolo [3,2-C] Pyridine-4-One 2-Indolinone Protein Kinase Inhibitors - The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R01-07-2010
20120208812DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLES AS OREXIN RECEPTOR MODULATORS - Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.08-16-2012
20110281867COMPOSITIONS AND METHODS OF USE FOR TYROSINE KINASE INHIBITORS TO TREAT PATHOGENIC INFECTION - Compositions and methods are provided for using tyrosine kinase inhibitors to treat pathogenic infection. In particular, methods for using Abl-family tyrosine kinase inhibitors to treat pathogenic infection are provided. Infections to be treated according to the present invention include, particularly, those caused by microbial pathogens such as bacteria and viruses.11-17-2011
20090149459P38 INHIBITORS AND METHODS OF USE THEREOF - This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.06-11-2009
20100267718Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them - The present invention relates to bicyclic heterocycles of general formula10-21-2010
20090312322Use of Oxindole Derivatives in the Treatment of Dementia Related Diseases, Alzheimer's Disease and Conditions Associated with Glycogen Synthase Kinase-3 - The present invention relates to a new use of oxindole derivatives of formula I, as a free base or a pharmaceutically acceptable salt thereof, [Chemical formula should be inserted here. Please see paper copy.] wherein R12-17-2009
20110136806Bicyclic heterocycles, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof - The invention relates to bicyclic heterocycles of general formula (I), in which R06-09-2011
20090192156PHTHALAZINONE DERIVATIVES - A compound of the formula (I):07-30-2009
20110281868INDAZOLE INHIBITORS OF KINASE - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,11-17-2011
20110082143Bicyclic Heteroaryl Compounds - Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds.04-07-2011
20110301162AURORA KINASE MODULATORS AND METHODS OF USE - The present invention relates to chemical compounds having a general formula I12-08-2011
20110301161BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I):12-08-2011
20110294806AZAINDOLE DERIVATIVES AS KINASE INHIBITORS - This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.12-01-2011
20110294808Indazole Compounds As CCR1 Receptor Antagonists - Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.12-01-2011
20090099175Phosphodiesterase 10 inhibitors - The present invention if directed to certain cinnoline compounds that are PDE10 inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.04-16-2009
20090099178INDAZOLE COMPOUNDS AND METHODS OF USE THEREOF - This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseases or disorders associated with protein kinase signal transduction.04-16-2009
20090099177PYRIDYL COMPOUNDS - Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein R04-16-2009
20090099176PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDES - Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.04-16-2009
20090318444TETRAHYDRO- AND DIHYDROQUINAZOLINONES - The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula I as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones.12-24-2009
20120190680Heteroaryl Amide Analogues - Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib:07-26-2012
200900544322-(2-Hydroxybiphenyl-3-yl)-1H-Benzoimidazole-5-Carboxamidine Derivatives as Factor VIIA Inhibitors - The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.02-26-2009
20100280029NOVEL COMPOUNDS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):11-04-2010
20100267717Novel Heterocyclic NF-kB Inhibitors - The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof,10-21-2010
20100081656COMPOSITIONS AND METHODS FOR MODULATING C-KIT AND PDGFR RECEPTORS - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.04-01-2010
20090209537AURORA INHIBITORS - The present invention provides an Aurora inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (I) (wherein R08-20-2009
20090088428CYCLOHEXYLIMIDIAZOLE LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula I: (I) having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.04-02-2009
20080207614QUINAZOLINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF DIABETES AND OBESITY - The present invention relates to novel quinazoline derivatives effective in lowering blood glucose level and body weight, and a medicine for treatment and/or prevention of diabetes and/or obesity, which comprises the compound as an active ingredient.08-28-2008
20090281098BENZOIMIDAZOLE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHETASE - The present invention provides a benzimidazole compound represented by Formula (I)11-12-2009
20120289504Benzoimidazole Compounds and Uses Thereof - This invention generally relates to substituted benzoimidazole compounds, particularly methyl 2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-5-methyl-1H-benzo[d]imidazol-1-yl)methyl)morpholine-4-carboxylate and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.11-15-2012
20110207732AZAINDOLE DERIVATIVES - Compounds of the formula (I), in which X08-25-2011
20110207731SUBSTITUTED 4-(INDAZOLYL)-1,4-DIHYDROPYRIDINES AND METHODS OF USE THEREOF - This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine og the following formula (I) derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.08-25-2011
20090170846INHIBITORS OF THE HIV INTEGRASE ENZYME - The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus “HIV” integrase enzyme. Formula (I).07-02-2009
20080280900BICYCLIC PYRIMIDINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).11-13-2008
20120142686VIRAL POLYMERASE INHIBITORS - The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:06-07-2012
20080269211Indazole Derivatives - This invention relates to compounds of the formula (I):10-30-2008
20120295904HEMATOPOIETIC GROWTH FACTOR MIMETIC SMALL MOLECULE COMPOUNDS AND THEIR USES - The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders.11-22-2012
20100137306HETEROCYCLIC TRPV1 RECEPTOR LIGANDS - The invention relates to compounds of formulae I(a)-I(d):06-03-2010
20100137305AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.06-03-2010
20100137304NOVEL CRYSTALLINE FORMS OF THE ANTI-CANCER COMPOUND ZD1839 - The invention concerns certain crystalline solvates and hydrates of the compound of the Formula I06-03-2010
20090062277PHOSPHODIESTERASE 10 INHIBITORS - The present invention is directed to certain compounds useful as phosphodiesterase 10 (PDE10) inhibitors that have the formula03-05-2009
20100144730PYRIDINONYL PDK1 INHIBITORS - The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.06-10-2010
20090181964Propane-1,3-Dione Derivative or Salt Thereof - It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO07-16-2009
200901433802H- OR 3H-BENZO[E]INDAZOL-1-YL CARBAMATE DERIVATIVES, THE PREPARATION AND THERAPEUTIC USE THEREOF - Compounds corresponding to the formula (I)06-04-2009
20090186890Pharmaceutical Formulation of Iressa Comprising a Water-Soluble Cellulose Derivative - A pharmaceutical composition comprising 4-(3′-chloro-4′-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline or a pharmaceutically acceptable salt thereof (the Agent) and a water-soluble cellulose ether or an ester of a water-soluble cellulose ether. The water-soluble cellulose ether or ester of a water-soluble cellulose ether present in the composition inhibits the rate of precipitation of the Agent from solution.07-23-2009
20100152183BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.06-17-2010
20090186891ORGANIC COMPOUNDS - The present invention provides compounds of the following structure;07-23-2009
200901375832-AMINOQUINAZOLINE DERIVATIVES - The present invention provides 2-aminoquinazoline derivatives represented by formula (I):05-28-2009
20090005379Azaindole-2-Carboxamide Derivatives - The present invention relates to compounds of formula (I) wherein R01-01-2009
20090137585N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS - N-Benzoyl arylsulfonamides having the formula05-28-2009
20090186892METHODS FOR TREATING LUNG CANCERS - The present invention provided methods for treating lung cancers using therapeutic agents for lung cancers comprising erbB receptor inhibitors as active ingredients. Methods for examining the responsiveness of lung cancer patients to erbB receptor inhibitors by using blood amphiregulin (AREG) as an indicator were provided. Furthermore, methods for treating lung cancers in which responsiveness to an erbB receptor inhibitor is determined based on blood AREG concentration, and in which therapeutic agents are selectively administered to patients expected to be responsive, were also provided. Advanced therapeutic effects can be expected by administering an erbB receptor inhibitor to patients predicted to be responsive. The present invention contributes to the improvement of therapeutic effects of gefitinib (Product name: Iressa®) and such on lung cancers.07-23-2009
20080318951Dual-acting benzoimidazole antihypertensive agents - The invention is directed to compounds having the formula:12-25-2008
20080318950Quinazoline Derivatives as a Multiplex Inhibitor and Method For the Preparation Thereof - The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof as a multiplex inhibitor, a method for the preparation thereof, and a pharmaceutical composition and a therapeutic composition comprising same as an active ingredient. The inventive quinazoline derivative as a multiplex inhibitor can selectively and effectively inhibit diseases caused by the overactivity of a tyrosine kinase.12-25-2008
20090325955GYRASE INHIBITORS AND USES THEREOF - The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.12-31-2009
20110144105AZAINDOLE GLUCOKINASE ACTIVATORS - Provided herein are compounds of the formula (I):06-16-2011
20090054431NOVEL HETEROCYCLE COMPOUNDS - The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.02-26-2009
20090082348INDAZOLE DERIVATIVES - The present invention provides a compound represented by Formula (I):03-26-2009
20090082349THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.03-26-2009
20090023726Heterocyclylalkyl Derivatives as Novel Inhibitors of Histone Deacetylase - This invention comprises the novel compounds of formula (I)01-22-2009
20090105247QUINAZOLINE AND QUINOLINE DERIVATIVES AS IRREVERSIBLE PROTEIN TYROSINE KINASE INHIBITORS - A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).04-23-2009
20110230482COMPOUNDS MODULATING C-FMS AND/OR C-KIT ACTIVITY - Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.09-22-2011
20080261975Tec Kinase Inhibitors - Disclosed are compounds of formula (I):10-23-2008
20090203691Novel 1H-indazole compounds - The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.08-13-2009
20120077811PRODRUG FORMS OF KINASE INHIBITORS AND THEIR USE IN THERAPY - The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I:03-29-2012
20090197881Azaindole Derivative Having PGD2 Receptor Antagonistic Activity - The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases.08-06-2009
20090197882INDAZOLE DERIVATIVES FOR THE TREATMENT OF HSP90-INDUCED DISEASES - Novel indazole derivatives of the formula (I), in which R08-06-2009
20090209536AMINOQUINAZOLINE CANNABINOID RECEPTOR MODULATORS FOR TREATMENT OF DISEASE - The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.08-20-2009
20090253697Novel Indole Derivatives, Preparation Thereof as Medicinal Products and Pharmaceutical Compositions, and Especially as KDR Inhibitors - The disclosure relates to compounds of formula (I):10-08-2009
20090247520INHIBITORS OF ANTIGEN RECEPTOR-INDUCED NF-kappa B ACTIVATION - A method to identify selective inhibitors of antigen receptor-mediated NF-κB activation is provided, as well as compositions having one or more of those inhibitors and methods of using those inhibitors.10-01-2009
20090247519AMINO-ETHYL-AMINO-ARYL (AEAA) COMPOUNDS AND THEIR USE - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain amino-ethyl-amino-aryl (AEAA) compounds which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.10-01-2009
20090239861QUINAZOLINE DERIVATIVES AS ANTICANCER AGENTS - A quinazoline derivative of the Formula I:09-24-2009
20100160315NOVEL 2, 3-DIAMINO-QUINAZOLINONE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the 2,3-diamino-quinazolinone derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2,3-diamino-quinazolinone derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of K06-24-2010
20090018132Substituted Heterocyclic Ethers and Their Use in CNS Disorders - The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.01-15-2009
20090018131QUINAZOLINE DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives.01-15-2009
200900482514-(1H-INDAZOL-5-YL-AMINO)-QUINAZOLINE COMPOUNDS AS ERBB RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER - A quinazoline derivative of the Formula I:02-19-2009
20090048250INDAZOLINONE COMPOSITIONS USEFUL AS KINASE INHIBITORS - The present invention provides compounds of formula I:02-19-2009
20110059963COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.03-10-2011
20100160316QUINAZOLINES USEFUL AS MODULATORS OF ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.06-24-2010
20110130400TRPV4 ANTAGONISTS - The present invention relates to diazabicyclo[2.2.1]hept-2-yl analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.06-02-2011
20100216791PYRIDINYLQUINAZOLINAMINE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS - The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.08-26-2010
20100240649QUINAZOLINE AND QUINOLINE DERIVATIVES AS IRREVERSIBLE PROTEIN TYROSINE KINASE INHIBITORS - A compound of formula (I),09-23-2010
20090042879PHTHALAZINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME - The present invention provides a novel compound having an excellent PDE4 inhibitory activity and TNF-α production-suppressing activity, and also provides a preventive and therapeutic agent for atopic dermatitis or the like. The present invention includes a novel phthalazinone derivative of the following general structural formula [1] or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising it as an active ingredient.02-12-2009
20130217684NOVEL BIARYL BENZOIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.08-22-2013
20090076003Phthalazine Derivatives with Angiogenesis Inhibiting Activity - The invention relates to new phthalazine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment of a disease, especially of a disease that responds to the inhibition of tyrosine kinases, more especially the inhibition of the vascular endothelial growth factor (VEGF) receptor kinase, preferably the treatment of a proliferative disease, such as a tumour disease.03-19-2009
20120196856ARYL AMINOPYRIDINE PDE10 INHIBITORS - The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.08-02-2012
201002223444-ANILINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS - A quinazoline derivative of the Formula (I):09-02-2010
20100222345NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS FOR OPIOID RECEPTORS - This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.09-02-2010
20120142685ORGANIC COMPOUNDS - The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.06-07-2012
20090181965MODULATORS FOR AMYLOID BETA - The invention relates to compounds of formula07-16-2009
20090318445PDF INHIBITORS - The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed.12-24-2009
20080306064Benzimidazole Derivatives - Benzimidazole derivatives, methods of preparing the same and their pharmaceutical uses for the treatment of inflammatory diseases including COPD.12-11-2008
20110130399Phthalazine Derivatives with Angiogenesis Inhibiting Activity - The invention relates to new phthalazine derivatives of formula I,06-02-2011
20130131059METHOD FOR TREATING OPHTHALMIC DISEASES USING KINASE INHIBITOR COMPOUNDS IN PRODRUG FORMS - This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula I to the eyes of the patient in need of.05-23-2013
20100305121NOVEL ANTAGONISTS OF THE HUMAN FATTY ACID SYNTHASE THIOESTERASE - The present invention provides for compounds of formula (I)-(XIII), as well as pharmaceutically acceptable salts thereof, metabolites thereof, pro-drugs thereof, and pharmaceutical kits that include such compounds. The present invention also provides for the compounds of formula (I)-(XIII) for use in medical therapy or diagnosis. The present invention also provides for the use of the compounds of formula (I)-(XIII) in treating cancer in mammals (e.g., humans), as well inhibiting tumor cell growth in such mammals. The present invention also provides for methods of inhibiting FAS. The methods include contacting FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of inhibiting the TE domain of the FAS. The methods include contacting the thioesterase TE domain of the FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of treating cancer in mammals, as well as methods of inhibiting tumor cell growth in such mammals. The methods include administering a compound of formula (I)-(XIII) to a mammal in need of such treatment.12-02-2010
20090069320Substituted 4-Amino-Quinazoline Compounds with Metabotropic Glutamate Receptor Regulating Activity and Uses Thereof - Substituted 4-amino-quinazoline compounds corresponding to formula I03-12-2009
20100324041PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. Formula, (I).12-23-2010
20100227862DIAZA-SPIRO [4.5] DECANES USEFUL AS PESTICIDES - A method of combating and controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I) wherein Y is a single bond, C═O, C═S or S(O)09-09-2010
201100344596,7-DIALKOXY QUINAZOLINE DERIVATIVES AND METHODS OF TREATING DRUG RESISTANT AND OTHER TUMORS - Compounds of formula (I)02-10-2011
20110118258QUINAZOLIN-OXIME DERIVATIVES AS HSP90 INHIBITORS - Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.05-19-2011
201100398452-AMINOQUINAZOLINE DERIVATIVE - A 2-aminoquinazoline derivative represented by formula (I) {wherein R02-17-2011
20110118259BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX - This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith.05-19-2011
201100398446-7,DIALKOXY QUINAZOLINE DERIVATIVES USEFUL FOR TREATMENT OF CANCER RELATED DISORDERS - In view of the great potential the quinazoline class of compounds offer, we started the synthesis and screening of a large number of new chemical entities with novel structural features. It has been surprisingly and unexpectedly found that quinazolines having 3-Ethynyl anilino group at the 4th position and specifically substituted alkoxy groups in the 6 and 7 positions, impart much enhanced and special anti-proliferative properties when compared to other prominent members of the quinazoline class of drugs. Also, surprisingly the compounds of this invention are much less toxic and the safety profile is exceedingly beneficial for therapeutic applications. The novel chemical entities described in this invention are designated by the general structure (I) and have not been synthesized earlier nor investigated for their therapeutic benefits and safety profile. Compound (I) is NRC-2694, when structure (A).02-17-2011
20110130398SPIROINDOLINONE PYRROLIDINES - There are provided compounds of the formula06-02-2011
20100144731Novel Biccyclic Compounds As GATA Modulators - Novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided.06-10-2010
20110086853Therapeutic Compounds - Compounds of formula I or pharmaceutically acceptable salts thereof:04-14-2011
201001603172-(2-OXOINDOLINE-3-YLIDENE)METHYL-5-(2-HYDROXY-3-MORPHOLIN-4-YL-PROPYL)-6,- 7-DIHYDRO-1H-PYRROL[3,2-C]PYRIDINE-4(5H)-ONE COMPOUNDS AND USE AS PROTEIN KINASE INHIBITORS - Pyrrolo[3,2-c]pyridine-4-one-2-indolinone compounds, especially 2-(2-oxoindoline-3-ylidene)methyl-5-(2-hydroxy-3-morpholin-4-yl-propyl)-6,7-dihydro-1H-pyrrol[3,2-c]pyridine-4(5H)-one compounds. Their preparation and pharmaceutical composition, and pharmaceutical use as protein kinase inhibitors.06-24-2010
20120245174COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.09-27-2012
20110245246Quinazoline Derivatives Useful as Anti-Tumor Medicament - he present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti-tumor medicament.10-06-2011
20090048252THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.02-19-2009
20110178083PDE-10 INHIBITORS - Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.07-21-2011
20100069382Agent for prophylaxis or treatment of alcohol dependence or drug dependence - The present invention provides an agent for the prophylaxis or treatment of substance abuse and dependence, which contains a compound of the formula (I) represented by (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, or a pharmaceutically acceptable salt thereof as an active ingredient.03-18-2010
20100056517ARYLSULFONAMIDE COMPOUNDS - The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins:03-04-2010
20100056515BENZIMIDAZOLE COMPOUNDS - There is provided a compound of the formula (I):03-04-2010
201000565161-HYDROXY NAPHTHYRIDINE COMPOUNDS AS ANTI-HIV AGENTS - 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.03-04-2010
20090215771JNK INHIBITORS - The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.08-27-2009
20090215770Substituted Quinazoline Derivatives as Inhibitors of Aurora Kinases - The invention provides quinazoline derivatives of formula (I):08-27-2009
20110251194ANTINEOPLASTIC DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure concerns heterobicyclic compounds of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as enantiomers, diastereoisomers and mixtures thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.10-13-2011
20110082142SELECTIVE KINASE INHIBITORS - A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C04-07-2011
20110152260Indazole derivatives as modulators of interleukin-1 receptor-associated kinase - The present invention relates to modulators of IRAK kinases of formula (I) and provides compositions comprising such modulators, as well as methods therewith for treating IRAK-mediated or IRAK-associated conditions or diseases.06-23-2011
20110077245SUBSTITUTED 2-ALKYL QUINAZOLINONE DERIVATIVES AS PARP INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I)03-31-2011
20110059962TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF - Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections, are also provided.03-10-2011
20100016307NOVEL COMPOUNDS - The present invention relates to compounds of formula (I):01-21-2010
20080249090Substituted pyridone compounds and methods of use - The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I10-09-2008
20130165441Novel Polymorphs and Salts - The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity.06-27-2013
20090118280Compounds Which Potentiate AMPA Receptor and Uses Thereof in Medicine - Compounds of formula (I) and salts are provided:05-07-2009
20090118279COMPOUND CONTAINING BASIC GROUP AND USE THEREOF - The present invention relates to a compound represented by formula (I):05-07-2009
20090111806Azaquinolone based compounds exhibiting prolyl hydroxylase Inhibitory activity, compositions, and uses thereof - are useful as inhibitors of HIF prolyl hydroxylases where the definitions of the variables are provided herein.04-30-2009
20080312230Organic Compounds - There are provided according to the invention compounds of formula (I),12-18-2008
20090170847Imidazopyridine Derivatives Inhibiting Protein Kinase Activity, Method for the Preparation Thereof and Pharmaceutical Composition Containing Same - The inventive imidazopyridine derivative can be used in a pharmaceutical composition for preventing or treating diseases such as diabetes, obesity, dementia, cancer, and inflammation, since it can efficiently inhibit the activities of several protein kinases including glycogen synthase kinase-3 (GSK-3), aurora kinase, extracellular signal-regulated kinase (ERK), protein kinase B (AKT), and the likes, to control signal transductions thereof.07-02-2009
20080255112Pyrimidine-Substituted Benzimidazole Derivatives as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Alk, Abl, BRK, Blk, BMX, CSK, c-Src, c-Raf, EGFR, Fes, FGFR3, Fms, Fyn, IGF-IR, IR, IKKα, IKKβ, JAK2, JAK3, KDR, Lck, Met, p70S6k, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SIK, Tie2, TrkB and/or WNK3 kinases.10-16-2008
20100075961MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF - Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is —N—, —NR03-25-2010
20110053932Protein Kinase Inhibitors and Methods for Using Thereof - The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, p38, Src, SIK, Syk, Tie2 and TrkB kinases.03-03-2011
20110053931QUINOLINE COMPOUNDS AND METHODS OF USE - Compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.03-03-2011
20100286142Compounds and Methods for Kinase Modulation, and Indications Therefor - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.11-11-2010
20110263598KINASE INHIBITORS AND METHOD OF TREATING CANCER - The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof:10-27-2011
20100298321BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.11-25-2010
20110136805BICYCLIC HETEROCYCLES, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF, AND METHOD FOR PRODUCTION OF SAME - The present invention relates to bicyclic heterocycles of general formula06-09-2011
20100305119Method for the treatment of anthrax infections - A method of treating an anthrax infection wherein a compound of formula I12-02-2010
20100305122APOPTOSIS INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.12-02-2010
20100305120COMPOUNDS FOR TREATING MUSCULAR DYSTROPHY - Compounds of formula (I): wherein X, L12-02-2010
20100179143NAPHTHYRIDINE, DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using naphthyridine derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of naphthyridine derivatives.07-15-2010
20100179142Cancer Combination Therapy Comprising AZD2171 and ZD1839 - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with ZD1839; to a pharmaceutical composition comprising AZD2171 and ZD1839; to a combination product comprising AZD2171 and ZD1839 for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and ZD1839; to the use of AZD2171 and ZD1839 in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.07-15-2010
201100821406-(PYRROLOPYRIDINYL) PYRIMIDIN-2-YLAMINE DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF CANCER AND AIDS. - Compounds of the formula (I), in which R04-07-2011
20120309756COMPOUNDS MODULATING C-FMS AND/OR C-KIT ACTIVITY AND USES THEREFOR - Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.12-06-2012
20090176780NITROGENOUS HETEROCYCLIC COMPOUNDS - The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.07-09-2009
20100048562ORGANIC COMPOUNDS - The present invention provides a compound of formula I:02-25-2010
20100029643HETEROCYCLYC SULFONAMIDES HAVING EDG-1 ANTAGONISTIC ACTIVITY - The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man.02-04-2010
201000225342-BENZIMIDAZOLYL-6-MORPHOLINO-4- (AZETIDINE, PYRROLIDINE, PIPERIDINE OR AZEPINE) PYRIMIDINE DERIVATIVES AS PI3K AND MTOR INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R01-28-2010
20110218198Pyrrolopyridinylpyrimidin-2-ylamine derivatives - Compounds of the formula I in which X, R09-08-2011
20100120768METHODS, KITS, AND COMPOSITIONS FOR GENERATING NEW HAIR FOLLICLES AND GROWING HAIR - The invention features methods, kits, and compositions for generating new hair follicles and growing hair on a subject.05-13-2010
20080207615Method to determine responsiveness of cancer to epidermal growth factor receptor targeting treatments - The present invention is directed to a method for determining the responsiveness of cancer to an epidermal growth factor receptor (EGFR) treatment. In a preferred embodiment, the presence of at least one variance in the kinase domain of the erbB1 gene confers sensitivity to the tyrosine kinase inhibitor gefitinib. Thus, a diagnostic assay for these mutations will allow for the administration of gefitinib, erlotinib and other tyrosine kinase inhibitors to those patients most likely to respond to the drug.08-28-2008
20110306613CHEMICAL COMPOUNDS - There is provided pyrimidinyl compounds of Formula (I),12-15-2011
20110306612QUINAZOLINONE, QUINOLONE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.12-15-2011
20110306611Transcription factor modulating compounds and methods of use thereof - Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.12-15-2011
20100179144QUINAZOLINE DERIVATIVES AS P13 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives.07-15-2010
20090286784INDAZOLE, BENZISOXAZOLE, AND BENZISOTHIAZOLE KINASE INHIBITORS - Compounds having the formula11-19-2009
20120040983Phthalazine Compounds as P38 Map Kinase Modulators and Methods of Use Thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A02-16-2012
20110071148COMPOUNDS AS THE ESTROGEN RELATED RECEPTORS MODULATORS AND THE USES THEREOF - The compounds according to formula VIII, their pharmaceutically acceptable acid or base addition salts, and the uses thereof is disclosed. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for the preparing a medicament for modulating estrogen related receptor (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity, etc. The definition of the groups of the formula is defined as the description.03-24-2011
20080234265Histone Deacetylase Inhibitors Sensitize Cancer Cells to Epidermal Growth Factor Inhibitors - Disclosed is the use of a combination of histone deacetylase inhibitors and epidermal growth factor receptor (EGFR) inhibitors to treat cancer.09-25-2008
200903259542-BENZIMIDAZOLYL-6-MORPHOLINO-4-PHENYLPYRIMIDINE DERIVATIVES AS PI3K AND MTOR INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention concerns pyrimidine derivatives of Formula (I), wherein each of p, R12-31-2009
20100298322Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use - A compound of the formula (I) wherein X is CR11-25-2010
20120208811Aminopyrazole Derivative - A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C08-16-2012
20120046286Novel Compounds - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):02-23-2012
20120046285BRADYKININ RECEPTOR AGONISTS AND USES THEREOF TO TREAT OCULAR HYPERTENSION AND GLAUCOMA - The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.02-23-2012
20110028473METHODS OF TREATING DRUG RESISTANT AND OTHER TUMORS BY ADMINISTERING 6,7-DIALKOXY QUINAZOLINE DERIVATIVES - Methods employing and uses of a compound of formula (I) in inhibiting the growth of a tumor cell in a subject in need thereof. Methods employing and uses of a compound of formula (I) in treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods employing and uses of a compound of formula (I) in treating HER-2 positive breast cancer in a subject in need of treatment for HER-2 positive breast cancer. Methods employing and uses of a compound of formula (I) in treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.02-03-2011
20120010204Phthalazinone Derivatives - Compounds of the formula (I):01-12-2012
20120059003INHIBITORS OF INV(16) LEUKEMIA - This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment.03-08-2012
20100035878INHIBITORS OF C-JUN N-TERMINAL KINASES FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS RELATING TO APOPTOSIS AND/OR INFLAMMATION - The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.02-11-2010
20080275039Geldanamycin Derivatives and the Method for Biosynthesis Thereof - The present invention relates to geldanamycin derivatives, benzoquinone ansamycin biosynthesized by gene manipulation of 11-06-2008
20120059002NOVEL ANTI-INFLAMMATORY AGENTS - Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.03-08-2012
20120108590MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.05-03-2012
20110009406TETRAHYDRO-1H-PYRROLO FUSED PYRIDONES - The present invention relates to tetrahydro-1H-pyrrolo fused pyridone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.01-13-2011
20090023727PHTHALAZINONE DERIVATIVES - A compound of the formula (I):01-22-2009
20120122863Quinazolinedione Chymase Inhibitors - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving Chymase.05-17-2012
20120071477CDKI PATHWAY INHIBITORS AND USES THEREOF - The invention relates to the compounds and methods for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds and methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.03-22-2012
20110092502DIAMINOTHIAZOLES USEFUL AS AXL INHIBITORS - Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.04-21-2011
20110092501NOVEL INHIBITORS - The invention relates to novel pyrrolidine derivatives of formula (I):04-21-2011
20110077246BICYCLIC HETEROCYCLIC COMPOUNDS PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESS FOR PREPARING THE SAME - The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula03-31-2011
201100821411-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1, CX3CR1 AND P40 - The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.04-07-2011
20110065702INDAZOLYL, BENZIMIDAZOLYL, BENZOTRIAZOLYL SUBSTITUTED INDOLINONE DERIVATIVES AS KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER - The present invention is directed to a compound is represented by Structural Formula (A):or a pharmaceutically acceptable salt therof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.03-17-2011
20120316164METHOD FOR INHIBITING THE GROWTH OF CANCER STEM CELLS - The present invention provides a method for inhibiting the growth of cancer stem cells, particularly colorectal cancer stem cells, liver cancer stem cells, lung cancer stem cells or breast cancer stem cells, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of antimycin A or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.12-13-2012
20120316166HETARYLAMINONAPHTHYRIDINES - Novel hetarylaminonaphthyridine derivatives of formula (I)12-13-2012
20120316165SUBSTITUTED BENZAMIDE DERIVATIVES - The present invention relates to compounds of formula12-13-2012
20120122864INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.05-17-2012
20090131432XANTHINE DERIVATES, THEIR PREPARATION AND THEIR USE IN PHARMACEUTICAL COMPOSITIONS - Compounds of formula (I)05-21-2009
20110183975NOVEL 6-AZAINDOLE AMINOPYRIMIDINE DERIVATIVES HAVING NIK INHIBITORY ACTIVITY - The present invention relates to a compound of formula I: wherein: R07-28-2011
201101839741,2,4-OXADIAZOLE SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES AS SMO ANTAGONISTS - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smo antagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract.07-28-2011
20120220587PYRIDINYLIMIDAZOLONE DERIVATIVES FOR THE INHIBITION OF PI3 KINASES - Compounds of the formula (I), in which X08-30-2012
20120220588QUINAZOLINE COMPOUNDS - Disclosed are compounds having the formula: wherein R08-30-2012
20120129853METHODS OF TREATMENT USING SELECTIVE BCL-2 INHIBITORS - This invention pertains to methods of treating systemic lupus erythematosus, lupus nephritis or Sjogren's Syndrome with compounds that selectively inhibit the activity of Bcl-2 anti-apoptotic proteins. Specifically, the current invention is directed to treatment with compounds that selectively inhibit the activity of Bcl-2 proteins, with a lesser affinity for inhibiting the activity of other BCL-2 family proteins, including Bcl-x05-24-2012
20120129855PHTHALAZINONE DERIVATIVES - A compound of the formula (I):05-24-2012
20120129854Pesticidal Arylpyrrolidines - The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the yield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.05-24-2012
20120165330QUINAZOLINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.06-28-2012
20120135989AZAINDOLE DERIVATIVE - The present invention provides a (di)azaindole derivative represented by the formula (I). A compound of the present invention inhibits a Cdc7 protein kinase activity and suppresses cell proliferation.05-31-2012
20120252806INHIBITORS OF AKT ACTIVITY - The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.10-04-2012
20100048561QUINAZOLINES FOR PDK1 INHIBITION - The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.02-25-2010
20100048565BENZIMIDAZOLE DERIVATIVES - Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives.02-25-2010
20100048564FUSED BICYCLIC HETEROARYL DERIVATIVE - The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ.02-25-2010
20100048563SUBSTITUTED INDOLEPYRIDINIUM AS ANTI-INFECTIVE COMPOUNDS - The present invention concerns the compounds of formula (I)02-25-2010
20100273794Benzimidazolone Compounds Having 5-HT4 Receptor Agonistic Activity - This invention provides a compound of the formula (I):10-28-2010
20120083493SMALL-MOLECULE MODULATORS OF TRP-P8 ACTIVITY - Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.04-05-2012
20120225872METHODS OF PREPARING AND USING QUINAZOLINE AND QUINOLINE DERIVATIVES - A method of preparing a compound of formula (I),09-06-2012
20120225871SMALL-MOLECULE MODULATORS OF TRP-P8 ACTIVITY - Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.09-06-2012
201202589684-PHENYLAMINO-PYRIMIDINE DERIVATIVES HAVING PROTEIN KINASE INHIBITOR ACTIVITY - The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein 10-11-2012
20110112091DERIVATIVES OF TETRABROMOBENZIMIDAZOLE, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, A METHOF OF USING THE SAME, A METHOD FOR MODULATING OR REGULATING SERINE/THREONINE KINASES, AND SERINE/THREONINE KINASES MODULATING AGENT - A derivative of tetrabromobenzimidazole, a process for the preparation thereof, a pharmaceutical composition, a method for using the same, a method for modulating or regulating serine/threonine kinases, and a serine/threonine kinases modulating agent. The invention relates to novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, this invention relates to new derivatives of tetrabromobenzimidazole with Pim kinases inhibitory properties, which exhibits superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on Pim kinases, such as leukemias and prostate cancer.05-12-2011
20110124643PYRIDINOPYRIDINONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The present invention relates to pyridopyridone derivatives of formula (I):05-26-2011
20110124642POTASSIUM CHANNEL MODULATORS - Disclosed herein are KCNQ potassium channels modulators of formula (I)05-26-2011
20080300248Quinazoline Derivatives, Preparation Methods and Uses Thereof - The present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti-tumor medicament.12-04-2008
20080300247Benzimidazole Thiophene Compounds - The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.12-04-2008
20110003810HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS - The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.01-06-2011
20110046132BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS - The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.02-24-2011
20120270871PYRROLOPYRIDINYLPYRIMIDIN-2-YLAMINE DERIVATIVES - Pyrrolopyridinylpyrimidin-2-ylamine derivatives of the formula (I), in which R10-25-2012
20120277228Novel Azaheterocyclic Compounds - The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.11-01-2012
20120277229SUBSTITUTED 3-(1H-BENZO[D]IMIDAZOL-2-YL)-1H-INDAZOLE ANALOGS AS INHIBITORS OF THE PDK1 KINASE - In one aspect, the invention relates to substituted 3-(1H-benzo[d]imidazol-2-yl)-1H-indazole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the PDK1 kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the PDK1 kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.11-01-2012
20120277226BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (IA) and (IB):11-01-2012
20120277227BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (IA), (IB) and (IC):11-01-2012
20120329795QUINAZOLINE DERIVATIVES - The invention concerns quinazoline derivatives of Formula I:12-27-2012
20120329794Ab1 KINASE INHIBITORS - The present invention provides an Abelson kinase (Abl kinase) inhibitor which comprises, as an active ingredient, an indazole derivative represented by Formula (I) (wherein R12-27-2012
20100204226QUINAZOLINONES AS PROLYL HYDROXYLASE INHIBITORS - Quinazolinone compounds of formula (I) are described,08-12-2010
20100204225Organic compounds - There are provided according to the invention compounds of formula (I), in free or salt form, wherein R08-12-2010
20100204224AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC SODIUM CHANNELS - Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents; wherein (1) represents (A), (B) or (C); R08-12-2010
20120101096Compounds and Methods for Treating Mammalian Gastrointestinal Microbial Infections - Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.04-26-2012
20120135990IAP INHIBITORS - The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.05-31-2012
201300125101-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1 AND CX3CR1 - The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1.01-10-2013
20130012509NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I)01-10-2013
20130012508NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I)01-10-2013
20130012511SOLUBLE GUANYLATE CYCLASE ACTIVATORS - The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.01-10-2013
20110160205NOVEL 1-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1, CX3CR1 AND P40 - The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.06-30-2011
20110160204PYRIDOPYRAZINES AND DERIVATIVES THEREOF AS ALK AND c-MET INHIBITORS - The present invention provides a compound of Formula I06-30-2011
20080255111Tissue Factor Production Inhibitor - A medicament which has an activity of inhibiting production of tissue factor and comprises an LXR ligand as an active ingredient; and a medicament for treatment and/or prophylaxis of vascular restenosis following angioplasty, endarterectomy, percutaneous transluminal coronary angioplasty (PTCA) or stent implantation, or treatment and/or prophylaxis of blood coagulation diseases, diseases induced by platelet aggregation including stable or unstable angina pectoris, cardiovascular and cerebrovascular diseases including thromboembolism formation diseases accompanying diabetes, rethrombosis following thrombolysis, cerebral ischemic attack, infarction, stroke, ischemia-derived dementia, peripheral artery disease, thromboembolism formation diseases during use of an aorta-coronary artery bypass, glomerulosclerosis, renal embolism, tumor or cancer metastasis, which comprises an LXR ligand as an active ingredient.10-16-2008
20130172342BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT - The present invention is directed to methods of treating diseases or conditions mediated by elevated persistent sodium channel, such as ocular disorders, pain, multiple sclerosis, and seizure disorders utilizing a compound of Formula I07-04-2013
20080234266Squaric Acid Derivatives II - Compounds of the formula (I), in which R, X, X′ and R09-25-2008
20080234264Method to determine responsiveness of cancer to epidermal growth factor receptor targeting treatments - The present invention is directed to a method for determining the responsiveness of cancer to an epidermal growth factor receptor (EGFR) treatment. In a preferred embodiment, the presence of at least one variance in the kinase domain of the erbB1 gene confers sensitivity to the tyrosine kinase inhibitor gefitinib. Thus, a diagnostic assay for these mutations will allow for the administration of gefitinib, erlotinib and other tyrosine kinase inhibitors to those patients most likely to respond to the drug.09-25-2008
20080234263Quinazoline Derivatives - The invention concerns quinazoline derivatives of Formula (I) wherein each of R09-25-2008
20130178472ARYLSULFONAMIDE PYRIDINE-PYRIDINONE DERIVATIVES, PREPARATION OF SAME, AND THERAPEUTIC USE THEREOF - The invention relates to pyridine-pyridinone derivatives general formula (I):07-11-2013
20130178473COMPOUNDS MODULATING C-FMS AND/OR C-KIT ACTIVITY AND USES THEREFOR - Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.07-11-2013
20110269758NAPHTHYRIDINONES AS PROTEIN KINASE INHIBITORS - Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.11-03-2011
20130172343Derivatives of 1H-isoindol-3-amine, 1H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as Beta-secretase Inhibitors - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I: (I). In another embodiment, the compounds have a general Formula II: (II). In another embodiment, the compounds have a general Formula III: (III). Variables A07-04-2013
20090137584SULFONYL BENZIMIDAZOLE DERIVATIVES - This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R05-28-2009
20130096117Novel Compounds - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):04-18-2013
20130096118CARBOLINE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.04-18-2013
201301026022-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions - Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof:04-25-2013
20130143880POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 - The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR06-06-2013
20100280028CXCR3 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula (I):11-04-2010
20080207613Selective Kinase Inhibitors - A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C08-28-2008
20080207612Benzimidazole Derivatives, Compositions Containing Them, Preparation Thereof and Uses Thereof - Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R08-28-2008
20080200458Methods and compositions for the treatment of body composition disorders - This invention relates to methods of treating, managing and preventing body composition disorders, and to compounds and pharmaceutical compositions useful in such methods.08-21-2008
20110212961Pyrazole Derivatives as Kinase Inhibitors - The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof:09-01-2011
20110224205USE OF CURCUMIN OR ITS ANALOGUES IN CANCER THERAPY UTILIZING EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE INHIBITOR - Provided is combined use of an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) and curcumin or its analogue in cancer therapy, which reduces side effects resulting from the EGFR-TKI and reduces doses of the EGFR-TKI needed for the therapy, particular in a patient resistant to the treatment with the EGFR-TKI alone.09-15-2011
20130150363Method of Treating Cancer Using a cMET and AXL Inhibitor and an ErbB Inhibitor - The present invention relates to a method of treating cancer in a patient comprising administering to the patient therapeutically effective amounts of: 06-13-2013
20130150364HETEROCYCLIC COMPOUND06-13-2013
20100286143Methods and materials for genetic analysis of tumors - This invention relates generally to methods and materials for rapid detection of mutations for tumor genotyping.11-11-2010
20080261974Novel Chemical Compounds - This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.10-23-2008
20100317660Mediators of hedgehog signaling pathways, compositions and uses related thereto - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.12-16-2010
20100317659JAK KINASE MODULATING COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.12-16-2010
20120283260BRADYKININ RECEPTOR AGONISTS AND USES THEREOF TO TREAT OCULAR HYPERTENSION AND GLAUCOMA - The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.11-08-2012
20120283259NOVEL INHIBITORS - Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.11-08-2012
20120283258MEDIATORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED HERETO - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.11-08-2012
20110294807COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASE - Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds. Formula (I)12-01-2011
20100069383COMPOUNDS AND THERAPEUTICAL USE THEREOF - Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.03-18-2010
20110312959Derivatives of Azaindoles as Inhibitors of Protein Kinases ABL and SRC - The present invention relates to compounds of general formula I and use thereof as inhibitors of protein kinases AbI and Src and the method of production thereof. The present invention also relates to pharmaceutical compositions and medici-nal products comprising these compounds.12-22-2011
20130190310MIG6 AND THERAPEUTIC EFFICACY - We identify markers capable of guiding the decision to incorporate epidermal growth factor receptor (EGFR) inhibitors, in particular EGFR tyrosine kinase inhibitors (TKIs), into chemotherapeutic regimens. Mitogen-inducible gene 6 (Mig6), a negative regulator of EGFR, is selectively upregulated during the development of resistance to the EGFR tyrosine kinase inhibitor (TKI) erlotinib, resulting in decreased EGFR phosphorylation. The ratio of Mig6/EGFR expression highly correlates with erlotinib sensitivity. A low Mig6/EGFR ratio correlates with a high response rate to gefitinib and a marked increase in progression-free survival for patients. The ratio of Mig6 to EGFR is a major predictor of biologic and clinical responses to EGFR inhibitors.07-25-2013
20130190309PHTHALAZINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.07-25-2013
20090312321COMPOSITIONS AND METHODS FOR FGF RECEPTOR KINASES INHIBITORS - Described are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent disease or disordered associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activity of kinases such as Abl, ALK, AMPK, Aurora, Axl, Bcr-Abl, BIK, Bmx, BRK, BTK, c-Kit, CSK, cSrc, CDK1, CHK2, CK1, CK2, CaMKII, CaMKIV, DYRK2, EGFR, EphB1, FES, FGFR1, FGFR2, FGFR3, Flt1, Flt3, FMS, Fyn, GSK3β, IGF-1R, IKKα, IKKβ, IR, IRAK4, ITK, JAK2, JAK3, JNK1α1, JNK2α, KDR, Lck, LYN, MAPK1, MAPKAP-K2, MEK1, MET, MKK4, MKK6, MST2, NEK2, NLK, p70S6K, PAK2, PDGFR, PDGFRα, PDK1, Pim-2, Plk3, PKA, PKBα, PKCα, PKCtheta, PKD2, c-Raf, RET, ROCK-I, ROCK-II, Ron, Ros, Rsk1, SAPK2a, SAPK2b, SAPK3, SAPK4, SGK, SIK, Syk, Tie2, TrkB, WNK3, and ZAP-70.12-17-2009
20130196990Benzimidazole Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.08-01-2013
20120046284Salts and hydrates of 4-[(3-chloro-4-fluoro-phenyl)amino]-6-(cis-4--cyclohexan-1-yloxy)-7-metho- xy-quinazoline, their use as a medicament and the preparation thereof - The present invention relates to a compound of formula (I),02-23-2012
201301026032,4-DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER - The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.04-25-2013
20120088767BENZIMIDAZOLE DERIVATIVES AS PI3 KINASE INHIBITORS - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kβ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.04-12-2012
20120094997SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I):04-19-2012
20130210821Methods for Treating Obesity - The disclosure provides for methods of treating obesity and related disorders. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.08-15-2013

Patent applications in class Plural ring nitrogens in the bicyclo ring system

Patent applications in all subclasses Plural ring nitrogens in the bicyclo ring system