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Plural ring nitrogens in the additional hetero ring (e.g., imidazole, pyrazine, etc.)

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

514235500 - Ring nitrogen in the additional hetero ring

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514236200 Three or more ring hetero atoms in the additional hetero ring 141
514236500 The ring nitrogens are bonded directly to each other (e.g., pyridazine, etc.) 122
Entries
DocumentTitleDate
20100099676SULFONYLUREA DERIVATIVE CAPABLE OF SELECTIVELY INHIBITING MMP-13 - A compound represented by the general formula (I):04-22-2010
20130029987SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Diaminopyrimidine Compounds having the following structures:01-31-2013
20120172360NOVEL 1H-PYRIMIDIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS INHIBITORS OF AKT (PKB) PHOSPHORYLATION - The invention relates to the novel products of formula (I):07-05-2012
201000225385-FLUORO PYRIMIDINE DERIVATIVES - This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.01-28-2010
20090082352NOVEL PYRIMIDINE COMPOUND HAVING DIBENZYLAMINE STRUCTURE AND MEDICAMENT COMPRISING THE SAME - A compound represented by the following general formula (I), wherein R03-26-2009
20090325957MORPHOLINO PYRIMIDINE DERIVATIVES USEFUL IN THE TREATMENT OF PROLIFERATIVE DISORDERS - A compound of formula (I)12-31-2009
20100160322APOPTOSIS-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.06-24-2010
20100160321IMIDAZOLINONE AND HYDANTOINE DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of Formula (I) wherein R06-24-2010
20090192160COMPOUNDS - The invention relates to compounds of formula (I)07-30-2009
20110195966COMBINATION OF A PHOSPHATIDYLINOSITOL-3-KINASE (PI3K) INHIBITOR AND A MTOR INHIBITOR - The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound of formula (I) and (b) a mTOR inhibitor for the treatment of a target of rapamycin (mTOR) kinase dependent disease, especially a cancer disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.08-11-2011
20100075968Imidazolidine Carboxamide Derivatives as P2X7 Modulators - The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof:03-25-2010
20100075966Substituted Dihydroimidazoles and their Use in the Treatment of Tumors - The invention relates to dihydroimidazoles of formula rac-(I),03-25-2010
20100075965PI3 KINASE INHIBITORS AND METHODS OF THEIR USE - Phosphatidylinositol (PI) 3 kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, phospholipid kinases, G-protein coupled receptors, and phosphatases.03-25-2010
20100075967PYRIMIDINE DERIVATIVES FOR TREATMENT OF HYPERPROLIFERATIVE DISORDERS - Pyrimidine derivatives of formula (I)03-25-2010
201000565255- AND 6- SUBSTITUTED BENZIMIDAZOLE THIOPHENE COMPOUNDS - The present invention provides 5- and 6-substituted benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.03-04-2010
20130040949TYPE II RAF KINASE INHIBITORS - The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.02-14-2013
20080261978Chemokine receptor modulators - The invention provides compounds of Formula (I)10-23-2008
20100113445Chemical Compounds - The present invention relates to dianilinopyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dianilinopyrimidine derivatives are useful in the treatment of diseases associated with inappropriate Wee1 kinase activity.05-06-2010
20100113444PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.05-06-2010
20100041654Pyrimidine Derivatives And Their Use As CB2 Modulators - This relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.02-18-2010
20090156601PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF CANCER - The invention provides compounds which are pyrimidines of formula (I): wherein —XR06-18-2009
20100105683COMPOUNDS USEFUL FOR INHIBITING CHK1 - Aryl- and heteroaryl-substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.04-29-2010
20100105682CYCLOPROPYL-PIPERAZINE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a piperazine ring and a cyclopropyl ring are disclosed of the general formula (I) where X04-29-2010
20100016318ANTHRANILAMIDE INHIBITORS OF AURORA KINASE - The present invention relates to a compound represented by the following formula:01-21-2010
200902988304-Aryl-2-Amino-Pyrimidnes or 4-Aryl-2-Aminoalkyl-Pyrimidines as Jak-2 Modulators and Methods of Use - This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R12-03-2009
20090281099SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE AS A MEDICINE - The present invention concerns substituted pyrazinone derivatives according to the general Formula (I)11-12-2009
20130090338NEW CCR2 RECEPTOR ANTAGONISTS, METHOD FOR PRODUCING THE SAME, AND USE THEREOF AS MEDICAMENTS - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.04-11-2013
20110009408METHODS FOR IDENTIFIYING INHIBITORS AGAINST VIRUSES THAT USE A CLASS I FUSION PROTEIN - The invention concerns the generation of a three dimensional model of the six helix bundle (6HB) complexed with an inhibitor and the use of that model to identify, screen and/or develop inhibitors against viruses that use a class I fusion protein. Such inhibitors of viruses that use a class I fusion protein may be effective for treating, for example, respiratory infections by Respiratory Syncytial Virus (RSV).01-13-2011
20090306076Morpholine Carboxamide Prokineticin Receptor Antagonists - The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which prokineticin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which prokineticin receptors are involved.12-10-2009
20130072488ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANTS - Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.03-21-2013
20090093480INSECTICIDAL PYRIMIDINYL ARYL HYRDRAZONES - Pyrimidinyl aryl hydrazones are effective at controlling insects.04-09-2009
20130072487PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I)03-21-2013
20130072486PYRIMIDINE CYCLOHEXYL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.03-21-2013
20130065900PHARMACEUTICAL COMPOUNDS - The invention provides a compound of the formula (1):03-14-2013
20130065898USE OF DIHYDROIMIDAZOLONES FOR THE TREATMENT OF DOGS - The present invention relates to the use of substituted dihydroimidazolones, particularly [1-(4-Chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazol-2-one] (AWD 131-138) or a physiologically acceptable salt thereof for the treatment of epilepsy in dogs.03-14-2013
20130065899HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.03-14-2013
20090233929Imidazole Derivatives for the Treatment of Anxiety and Related Diseases - This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith.09-17-2009
20090233928IMIDAZOLO-5-YL-2-ANILO-PYRIMIDINES AS AGENTS FOR THE INHIBITION OF CELL PROLIFERATION - Compounds of the formula (I):09-17-2009
20080293718Novel 2-Amino-Imidazole-4-One Compounds and Their Use in the Manufacture of a Medicament to Be Used in the Treatment of Cognitive Impairment, Alzheimer's Disease, Neurodegeneration and Dementia - This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.11-27-2008
20090215778Alpha-substituted Arylmethyl Piperazine Pyrazolo [1,5-alpha]Pyrimidine Amide Derivatives - Derivatives of pyrazolopyrimidine compounds represented by Formula I are disclosed:08-27-2009
20100087436METHOD OF PREVENTING OR TREATING ORGAN, HEMATOPOIETIC STEM CELL OR BONE MARROW TRANSPLANT REJECTION - Methods of preventing or treating organ, hematopoietic stem cell or bone marrow transplant rejection are disclosed.04-08-2010
20120238575ANTIPROLIFERATIVE PYRIMIDYL, FUSED PYRIMIDYL AND PYRIMIDYL HYDRAZONES - The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.09-20-2012
20090062282Substituted Amino-Pyrimidones and Uses Thereof - This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia, Ib), and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.03-05-2009
20090105252Pyrimidine Derivatives and Their Use in Therapy as well as the Use of Pyrimidine Derivatives in the Manufacture of a Medicament for Prevention and/or Treatment of Alzheimer's Disease - Compounds of formula I04-23-2009
20110281872COMPOSITIONS AND METHODS FOR THE PREVENTION AND TREATMENT OF CANCER - The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.11-17-2011
20110281873Pyrimidine Compounds and Methods of Making and Using Same - Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.11-17-2011
20080269217Melanocortin-4 receptor binding compounds and methods of use thereof - Provided are MC4-R binding compounds of the formula XVII:10-30-2008
20100216792Pesticidal 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 field of veterinary medicine. The compounds are represented by formula (I):08-26-2010
20080214544Substituted heterocycles and methods of use - Selected compounds are effective for prophylaxis and treatment of diseases, such as c-met mediated diseases and/or HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.09-04-2008
20100234377PIPERAZINE COMPOUNDS FOR THE INHIBITION OF HAEMATOPOIETIC PROSTAGLANDIN D SYNTHASE - The present invention relates to compounds of general formula (I):09-16-2010
20110294810SUBSTITUTED (PYRIDYL)-AZINYLAMINE DERIVATIVES AS PLANT PROTECTION AGENTS - The present invention relates (pyridyl)-azinylamino derivatives of formula (I) wherein Q12-01-2011
20090298831PHENYL PIPERAZINE COMPOUNDS, PHARMACEUTICAL COMPOSITION INCLUDING THE SAME AND USE THEREOF - The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal.12-03-2009
20090029992SUBSTITUTED PYRAZOLE COMPOUNDS - Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.01-29-2009
20120190681PICOLINAMIDE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,07-26-2012
20100022539Isoxazole Compounds as Histamine H3 modulators - Certain isoxazole compounds are histamine H01-28-2010
20090036448PYRIMIDINE DERIVATIVES AND METHODS OF TREATMENT RELATED TO THE USE THEREOF - The present invention encompasses novel substituted pyrimidine compounds of Formula (I):02-05-2009
20090105251Renin inhibitors - Compounds, pharmaceutical compositions, kits and methods are provided for use with renin that comprise a compound selected from the group consisting of:04-23-2009
20090099183PYRIMIDINES AND USES THEREOF - The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor-cells.04-16-2009
20100125075Antibacterial Agents - Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(═O) or the formula: —C(═O)NH(OH); R05-20-2010
20130217687ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.08-22-2013
20100120769CYCLOHEXYL PIPERAZINYL METHANONE DERIVATIVES - The present invention relates to compounds of formula I05-13-2010
20110092506TRISUBSTITUTED AMINE COMPOUND - The present invention relates to a compound of the general formula (1):04-21-2011
20100249133APOPTOSIS PROMOTERS - Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.09-30-2010
20100249130BIARYL COMPOSITIONS AND METHODS FOR MODULATING A KINASE CASCADE - The invention relates to compounds of formula IB and methods for modulating one or more components of a kinase cascade using these compounds.09-30-2010
20080306066NON-IMIDAZOLE HETEROCYCLIC COMPOUNDS - Certain non-imidazole heterocyclic compounds are histamine H12-11-2008
20090170851Chroman Compounds - Compounds according to Formula (I):07-02-2009
20090275582Bi-Aryl Meta-Pyrimidine Inhibitors of Kinases - The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases.11-05-2009
20090281101THERAPEUTIC SUBSTITUTED HYDANTOINS, AND RELATED COMPOUNDS - Compounds comprising a structure11-12-2009
20090281100Benzimidazole quinolinones and uses thereof - Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.11-12-2009
20090286790ORGANIC COMPOUNDS - The present invention provides a compound of formula (I):11-19-2009
20090286789Bi-Aryl Meta-Pyrimidine Inhibitors of Kinases - The invention provides methods of treating a disease selected from systemic sclerosis, rheumatoid arthritis, mastocytosis, and chronic eosinophilic leukemia comprising administering biaryl meta-pyrimidine compounds having the general structure (A) to a subject in need thereof. The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the JAK kinase family, and various other specific receptor and non-receptor kinases.11-19-2009
20090291951Novel Cyclic Compound Having Pyrimidinylalkylthio Group - The present invention has its object to study synthesis of novel cyclic compounds having a pyrimidinylalkylthio group and to find pharmacological actions of the compounds. According to the present invention, a compound represented by the formula (1) or a salt thereof is provided.11-26-2009
201101722312,4- DIAMINOPYRIMIDINE DERIVATIVES - There are provided compounds of formula I07-14-2011
20110269759PYRIMIDINE COMPOUNDS AS DELTA OPIOID RECEPTOR MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:11-03-2011
20080242667Pyrimidinyl-Pyrazole Inhibitors of Aurora Kinases - The present invention provides a compound represented by Formula (I):10-02-2008
20080275045Potassium Channel Modulating Agents and Their Medical Use - This invention relates to novel potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions.11-06-2008
20100130496PYRIMIDINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3-KINASE - The invention provides a pyrimidine compound of formula (I):05-27-2010
20080280906Imidazolyl-Pyrimidine Compounds for Use in the Treatment of Proliferative Disorders - Compounds of formula (I):11-13-2008
20080287438Agent for preventing or treating neuropathy - The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula: wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is —O—, —S—, —NR11-20-2008
20080287437Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors - This invention relates to novel compounds having the formula (I):11-20-2008
20080287439Pyrimidine compounds - The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders.11-20-2008
20110207734Azine Derivatives and Methods of Use Thereof - The present invention relates to Azine Derivatives, pharmaceutical compositions comprising the Azine Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.08-25-2011
20080269216Imidazole Variants as Modulators of Gaba Receptor For the Treatment of Gi Disorders - The present invention relates to novel compounds having a positive allosteric GÀBAB receptor (GDR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). A compound of the general formula I10-30-2008
20090264429Aryl - Hydroxyethylamino - Pyrimidines and Triazines as Modulators of Fatty Acid amide Hydrolase - Certain aryl-hydroxyethylamino-pyrimidine and triazine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.10-22-2009
20100137310RENIN INHIBITORS - The invention provides compounds, pharmaceutical compositions, kits, method of preparing, and method of using the compounds which exhibit renin and other S9 proteases activities and consist of the formula:—wherein the variables are as defined herein.06-03-2010
20100137311SUBSTITUTED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine derivatives of the general formula I or salts thereof06-03-2010
20110269760TUBULIN INHIBITORS - Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).11-03-2011
20090163501Aurora kinase modulators and method of use - The present invention relates to chemical compounds having a general formula I06-25-2009
20120196859HETEROCYCLIC ANALOGS OF PROPARGYL-LINKED INHIBITORS OF DIHYDROFOLATE REDUCTASE - The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as 08-02-2012
20110207733PYRIMIDINE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE - The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.08-25-2011
20090137589Stereoisomerically Enriched 3-Aminocarbonyl Bicycloheptene Pyrimidinediamine Compounds And Their Uses - The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.05-28-2009
20090163500COMPOSITIONS AND METHODS FOR TREATING LYSOSOMAL DISORDERS - The present invention provides compositions and methods for treating lysosomal disorders using a class of substituted imidazole derivatives or compounds.06-25-2009
200901433842,4,6-Trisubstituted Pyrimidines as Phosphotidylinositol (Pi) 3-Kinase Inhibitors and Their Use in the Treatment of Cancer - The invention concerns pyrimidine derivatives of Formula (I) wherein each of Q06-04-2009
20090163499Imidazole-substituted arylamides as P2X3 and P2X2/3 antagonists - Compounds of the formula I:06-25-2009
20090137588HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.05-28-2009
20080318954Compounds - The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts thereof, wherein: Z12-25-2008
20090118285USE OF KCNQ-OPENERS FOR TREATING OR REDUCING THE SYMPTOMS OF SCHIZOPHRENIA - The invention relates to a novel method for treating or reducing the symptoms of schizophrenia, said method comprising administering to a host in need thereof an effective amount of a compound able to selectively increase the ion flow through KCNQ potassium channels. Furthermore the invention relates to the use of selective KCNQ potassium channel openers for the preparation of a pharmaceutical composition for treating or reducing the symptoms of schizophrenia and related symptoms, disorders and diseases. Furthermore the invention relates to a method of screening for a compound, which is a selective KCNQ potassium channel opener and which is capable of having an anti-psychotic potential.05-07-2009
20090005382METHODS OF USING AND COMPOSITIONS COMPRISING TRYPTOPHAN HYDROXYLASE INHIBITORS - Methods and compositions comprising tryptophan hydroxylase inhibitors are disclosed. Particular methods are directed at reducing or avoiding serotonin-mediated adverse effects associated with some drugs.01-01-2009
20110230484PYRAZOLYL-PYRIMIDINE DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel pyrazolyl-pyrimidine derivatives and their use as potassium channel modulating agents. In another aspect the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.09-22-2011
20090082351PESTICIDE PYRIMIDINYLOXY SUBSTITUTED PHENYLAMIDINE DERIVATIVES - The present invention relates to 2,5-disubstituted-4-pyrimidinyl-substituted-phenyl-amidine derivatives of formula (I) in which the substituents are as in the description, notably to 2,5-dialkyl-4-pyrimidinyl-substituted-phenyl-amidine derivatives, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.03-26-2009
20110230483Pyridine and Pyrazine derivative for the Treatment of CF - The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.09-22-2011
20090209540Novel Biaryl Benzolmidazole 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.08-20-2009
20090105250COMPOUNDS AND COMPOSITIONS 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 the Abl, Bcr-Abl, FGFR3, PDGFRβ and b-Raf kinases.04-23-2009
20090005380CYCLOHEXYL DERIVATIVES - The present invention relates to compounds of formula I01-01-2009
20090018134Compounds - 945 - A compound of formula (I)01-15-2009
20080261977Pyrimidine Derivatives as Cannabinoid Receptor Modulators - The present invention relates to novel pyrimidine derivatives such as compounds of the formula (I) and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.10-23-2008
20090203695Compounds IV - The present application relates to new compounds of formula (I),08-13-2009
201102304856-PHENYL-PYRIMIDIN-4-YL-(PHENYLAMINE OR PHENOXY) DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel 6-phenyl-phymidin-4-yl-(phenylannine or phenoxy) derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.09-22-2011
20120077813Imidazole Substituted Pyrimidines Useful in the Treatment of Glycogen Synthase Kinase-3 Related Disorders such as Alzheimer's Disease - The present invention relates to a new compound of formula (I) wherein R03-29-2012
20090209539Pyrimidine derivatives as alk-5 Inhibitors - Compounds of formula (I) in free or salt or solvate form, where T08-20-2009
20090221583NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE - The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.09-03-2009
20090221582Piperazine Derivatives And Their Use In Therapy - Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB09-03-2009
20090221579Substituted Amino-Compounds and Uses Thereof - This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.09-03-2009
20090221581Methods of treating pain - The invention relates to methods of treating any type of pain comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases.09-03-2009
20090247523CARBOXAMIDE 4-[(4-PYRIDYL)AMINO]PYRIMIDINES USEFUL AS HCV INHIBITORS - The present invention relates to the use of carboxamide 4-[(4-pyridyl)amino]-pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections.10-01-2009
200902398646- (PYRIDINYL) -4-PYRIMIDONE DERIVATES AS TAU PROTEIN KINASE 1 INHIBITORS - A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof:09-24-2009
20100273795ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.10-28-2010
20100184766APOPTOSIS-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.07-22-2010
20120094999EGFR INHIBITORS AND METHODS OF TREATING DISORDERS - The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.04-19-2012
20100261722HIV INHIBITING 5, 6-SUBSTITUTED PYRIMIDINES - HIV replication inhibitors of formula10-14-2010
20100184765Protein 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, CSK, C-Src, EphB1, EphB2, EphB4, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, SAPK2α, Src, SIK, Syk, Tie2 and TrkB kinases.07-22-2010
20110059969PIPERAZINES AS ANTI-OBESITY AGENTS - The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.03-10-2011
20080207619Diaminopyrimidines as P2X3 and P2X2/3 modulators - Compounds and methods for treating diseases mediated by a P2X08-28-2008
20100280031LIPID FORMULATION OF APOPTOSIS PROMOTER - An orally deliverable pharmaceutical composition comprises a drug-carrier system having a Bcl-2 family protein inhibitory compound, e.g., ABT-263, in solution in a substantially non-aqueous carrier that comprises at least one phospholipid and a pharmaceutically acceptable solubilizing agent. The composition 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.11-04-2010
20100240656COMPOUNDS AS HSP90 INHIBITORS - The invention provides novel compounds of formula (I) wherein: one of the a, b, c or d members is a nitrogen atom and the remaining members are carbon atoms; and R09-23-2010
20130217688HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.08-22-2013
20110130401NEW CHEMICAL COMPOUNDS - Compounds of general formula (1)06-02-2011
20100137309FUNGICIDES PHENYL-PYRIMIDNYL-AMINO DERIVATIVES - The present invention relates to phenyl-pyrimidinyl-amino derivatives of formula (I) wherein Q06-03-2010
20100197689NOVEL PROCESSES FOR THE PREPARATION OF PIPERAZINYL AND DIAZAPANYL BENZAMIDE DERIVATIVES - The present invention is directed to novel processes for the preparation of substituted piperazinyl and diazepanyl benzamides, useful for the treatment of disorders and conditions mediated by the histamine receptor.08-05-2010
20090181967New compounds I - The present application relates to new compounds of formula (I),07-16-2009
20090111810SUBSTITUTED PYRIMIDINE-5-CARBOXAMIDE AND 5-CARBOXYLIC ESTER KINASE INHIBITORS - The present invention is directed to substituted pyrimidine-5-carboxamide and 5-carboxylic ester compounds of Formula (I):04-30-2009
20090118284Novel compounds that are ERK inhibitors - Disclosed are the ERK inhibitors of formula 1.0:05-07-2009
20100305128Pyrimidinyl-Thiophene Kinase Modulators - The present invention provides novel pyrimidinyl-thiophene kinase modulators and methods of using the novel pyrimidinyl-thiophene kinase modulators to treat diseases mediated by kinase activity.12-02-2010
20130137689NOVEL ACYLPIPERAZINONES AND THEIR USE AS PHARMACEUTICALS - The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.05-30-2013
20090069327COMPOUNDS AND COMPOSITIONS 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 the Abl, Bcr-Abl, Bmx, b-RAF, c-RAF, c-SRC, KDR, CSK, FGFR3, JAK2, Lck, Met, PKCα, SAPK2α, Tie2, TrkB and P70S6K kinases.03-12-2009
20100311751SOLID DISPERSIONS CONTAINING AN APOPTOSIS-PROMOTING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound, e.g., ABT-263, 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 dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent 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.12-09-2010
20110112093PYRIMIDINYL-PIPERAZINES USEFUL AS D3/D2 RECEPTOR LIGANDS - The present invention relates to new dopamine D05-12-2011
20110172230UREA COMPOUND OR SALT THEREOF - [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder.07-14-2011
20110021525P70S6 Kinase Modulators and Method of Use - The invention provides compounds and methods for inhibition of kinases, more specifically p70S6 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.01-27-2011
20110021524COMPOSITIONS AND METHODS FOR TREATING CANCERS - This invention provides a combination of ATP-competitive BCR-ABL inhibitor and a non-ATP competitive BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with BCR-ABL.01-27-2011
20110245249Heterocyclically Substituted Anilinopyrimidines - Heterocyclically substituted anilinopyrimidines of the formula (I)10-06-2011
20110118263BENZOTHIOPHENE ALKANOL PIPERAZINE DERIVATIVES AND THEIR USE AS ANTIDEPRESSANT - The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar05-19-2011
2010002964811-Beta HSD1 Inhibitors - This invention relates to inhibiting 11βHSD1.02-04-2010
201000630492-CARBOCYCLOAMINO-4-IMIDAZOLYLPYRIMIDINES AS AGENTS FOR THE INHBITION OF CELL PROLIFERATION - Compounds of formula (I):03-11-2010
20100056524Compound - A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof,03-04-2010
20100056523INHIBITORS OF AKT ACTIVITY - Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.03-04-2010
20090215777Pyrimidine Derivatives As HSP90 Inhibitors - The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates or N-oxides thereof; wherein: A is N or a group CR08-27-2009
20100069388N-HYDROXYACRYLAMIDE COMPOUNDS - A compound having the following formula (I): wherein —R03-18-2010
20100069387IKK Inhibitors for the Treatment of Endometriosis - This invention relates to a method of treating and/or preventing endometriosis comprising administering an IKK inhibitor. The IKK inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis-related infertility.03-18-2010
20110098301Pyrimidine Derivatives for Treatment of Hyperproliferative Disorders - Pyrimidine derivatives of formula04-28-2011
20110082146COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.04-07-2011
20110152262NOVEL COMPOUNDS - Compounds of formula (I)06-23-2011
20110077248IMIDAZOPYRIDINE 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.03-31-2011
20110071151ABT-263 CRYSTALLINE FORMS - ABT-263 free base and crystalline forms thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.03-24-2011
20090076006HSP90 INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to HSP90 inhibitors containing a zinc binding moiety and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.03-19-2009
20100261723TRISUBSTITUTED PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES - A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.10-14-2010
20100016316ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I) or (II):01-21-2010
20100113446HYDANTOIN COMPOUNDS - The invention relates to the use of hydantoin compounds useful for treating or preventing autoimmune disorders. The present invention also provides compositions and uses thereof.05-06-2010
20130165443BIPHENYL AND PHENYL-PYRIDINE AMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I:06-27-2013
20120202811NOVEL COMPOUNDS - Compounds of formula (I)08-09-2012
20090029994Trisubstituted amine compound - The present invention relates to a compound of the general formula (1):01-29-2009
20090029993METHODS OF AFFECTING GASTROINTESTINAL TRANSIT AND GASTRIC EMPTYING, AND COMPOUNDS USEFUL THEREIN - Methods and compounds are disclosed for affecting gastrointestinal motility and gastric emptying, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.01-29-2009
20090203696Aryl- and Heteroaryl-Ethyl-Acylguanidine Derivatives, Their Preparation and Their Application in Therapeutics - Disclosed are compounds according to formula (I):08-13-2009
20120122867NOVEL PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND FURTHER DISEASES - The invention concerns compounds of Formula (I): wherein L05-17-2012
20080255118Cyanopyrimidinones - The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.10-16-2008
20080255120SUBSTITUTED 2,5-HETEROCYCLIC DERIVATIVES - The present invention relates to new substituted five-membered compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:10-16-2008
20080255119DIPHENYL-DIHYDRO-IMIDAZOPYRIDINONES10-16-2008
20090005381METHODS OF TREATING SEROTONIN-MEDIATED DISEASES AND DISORDERS - Methods are disclosed for treating serotonin-mediated diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.01-01-2009
20100298326Carboxamide compounds and their use as calpain inhibitors - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.11-25-2010
20100305126Pyrimidine Inhibitors of Kinase Activity - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof,12-02-2010
20100305125SALT OF ABT-263 AND SOLID-STATE FORMS THEREOF - ABT-263 bis-HCl and crystalline polymorphs thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.12-02-2010
20100305127NOVEL COMPOUNDS - Compounds of formula (I)12-02-2010
20100324045CYCLIC UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih)1 (Ij), (Ik), (Il12-23-2010
20110124646Novel cyclic compound having pyrimidinylalkylthio group - A method of treating a disease associated with angiogenesis by administering a therapeutically effective amount of a compound represented by the formula (1) or a salt thereof05-26-2011
20120309760PIPERAZINE COMPOUND HAVING A PGDS INHIBITORY EFFECT - The present invention provides a piperazine compound represented by Formula (I) or a salt thereof,12-06-2012
20090176784ANTI-INFECTIVE AGENTS AND USES THEREOF - This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.07-09-2009
20090176785METHOD OF TREATING ARTHRITIS - Methods of preventing or treating arthritis is disclosed.07-09-2009
201101902984-PHENOXYMETHYLPIPERIDINES AS MODULATORS OF GPR119 ACTIVITY - The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.08-04-2011
20100029649PHENYL-SUBSTITUTED PYRIMIDINE COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the formula (I),02-04-2010
20100022537I-PHENY 1-3,4-DIHYDROPYRIMIDIN-2(1H)-ONE DERIVATIVES AND THEIR USE - This invention relates to novel heterocyclic derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.01-28-2010
20110218200METHODS OF TREATING AMYLOID DISEASE USING ANALOGS OF 1-(4-NITROPHENYL) PIPERAZINE - The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.09-08-2011
20100016317HIV INHIBITING 6-SUBSTITUTED PYRIMIDINES - HIV replication inhibitors of formula01-21-2010
20100331329BENZAMIDE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS - The invention concerns a compound of the formula (I)12-30-2010
20110118264PHENYL PIPERAZINE COMPOUNDS, PHARMACEUTICAL COMPOSITION INCLUDING THE SAME AND USE THEREOF - The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal05-19-2011
20090221584Bisaryl-sulfonamides - Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPARγ or PPARδ. In particular, the compounds of the invention modulate the function of PPARγ or PPARδ. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.09-03-2009
20100210648PYRAZOLYLAMINOPYRIMIDINE DERIVATIVES USEFUL AS TYROSINE KINASE INHIBITORS - This invention relates to novel compounds having the formula (I):08-19-2010
20120149703AZA-SUBSTITUTED SPIRO DERIVATIVES - A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided:06-14-2012
20100048567Inhibitors of syk and JAK protein kinases - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.02-25-2010
20110319413PIPERAZINE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHASE - This invention relates to a piperazine compound represented by Formula (I),12-29-2011
20120065204NOVEL N-HYDROXY-BENZAMIDS FOR THE TREATMENT OF CANCER - The present invention provides a compound of formula (I)03-15-2012
20120004230IMIDAZOLE DERIVATIVES - The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1.01-05-2012
20090221580Substituted aminopropenyl piperidine or morpholine derivatives as novel inhibitors of histone deacetylase - This invention comprises the novel compounds of formula (I) wherein R09-03-2009
20120010206IMIDAZOLOPYRIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel imidazolopyridine compounds are disclosed that have a formula represented by the following:01-12-2012
20110003812Human Adam-10 Inhibitors - Magnesium salts/complexes of compounds useful for inhibiting the ADAM-IO protein and methods of making and purifying them are provided. Further provided are compositions comprising magnesium salts/complexes of the compounds in combination with a pharmaceutically acceptable carrier. The compounds well as such compositions comprising them are useful for the treatment of cancer, arthritis, diseases related to angiogenesis, such as renal diseases, heart diseases, such as heart failure, atherosclerosis, and stroke, inflammation, ulcer, infertility, scleroderma, endometriosis, mesothelioma, and diabetes. In addition, methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role are provided.01-06-2011
20100204232XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZ0 [1,4] OXAZIN-3-ONE) -6-YL] -5-FLUORO-N2- [3-(METHYLAMINOCAR BONYLMETHYLENEOXY) PHENYL] 2,4-PYRIMIDINEDIAMINE - The present invention relates to the xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine. This compound is a suitable drug substance and is useful in the treatment of conditions including asthma.08-12-2010
20110166137Substituted Naphthalenyl-Pyrimidine Compounds - The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.07-07-2011
20110065706Therapeutic Agents 812 - A compound of formula I03-17-2011
20100240655BROMO-PHENYL SUBSTITUTED THIAZOLYL DIHYDROPYRIMIDINES - Bromo-phenyl substituted thiazolyl dihydropyrimidines and combinations thereof with other antiviral agents for combating HBV infections.09-23-2010
201002800302-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS - Compounds of the formula (I), in which R11-04-2010
20110039847AMIDE DERIVATIVES AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds represented by Structural Formula (I) 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.02-17-2011
20120059005COMBINATION OF (A) A PHOSPHOINOSITIDE 3-KINASE INHIBITOR AND (B) AN ANTIDIABETIC COMPOUND FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES - The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) an insulin sensitivity enhancer compound for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.03-08-2012
20090069328ALPHA-ALKYL SUBSTITUTED N-ACYLTRYPTOPHANOLS - The present invention relates to α-alkyl substituted N-acyltryptophanols of the formula I03-12-2009
20120065205PYRAZINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to pyrazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.03-15-2012
20120157456SUBSTITUTED AMINOPROPENYL PIPERIDINE OR MORPHOLINE DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)06-21-2012
20120122868APAF-1 INHIBITOR COMPOUNDS - Derivatives of 2,5-piperazinedione of formula (I) are apoptotic peptidase activating factor 1 (Apaf-1) inhibitors, therefore they are useful as active pharmaceutical ingredients for the prophylaxis and/or treatment of a pathological and/or physiological condition associated with an increase of apoptosis.05-17-2012
20120071479PYRAZINE DERIVATIVES AS ENAC BLOCKERS - Compounds of Formula I:03-22-2012
20120208817Novel Dihydropyrimidin-2(1H)-one Compounds as S-Nitrosoglutathione Reductase Inhibitors - The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.08-16-2012
20120208816ORGANIC COMPOUNDS - The present invention provides a compound of formula (I):08-16-2012
20100075964IMIDAZOLE BASED LXR MODULATORS - Compounds of the invention, such as compounds of Formulae IIa, IIb, IIc or IId, and pharmaceutically acceptable salts, isomers, and prodrugs thereof, are useful as modulators of the activity of liver X receptors, where R03-25-2010
201203161692-ARYL-PROPIONAMIDE DERIVATIVES USEFUL AS BRADYKININ RECEPTOR ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - (R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.12-13-2012
20120316170Imidazole Derivative - To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I):12-13-2012
20090131437DISUBSTITUTED UREAS AS KINASE INHIBITORS - The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.05-21-2009
20090131436Pyrimidine Derivatives - Novel pyrimidine derivatives of formula (I) to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.05-21-2009
20090312326SUBSTITUTED IMIDAZOLES - This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.12-17-2009
20120129856COMPOUNDS, COMPOSITIONS AND METHODS USEFUL FOR CHOLESTEROL MOBILISATION - The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.05-24-2012
20120214811RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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.08-23-2012
20120165332SULFONAMIDES AND SULFAMIDES AS ZAP-70 INHIBITORS - The invention relates to compounds of formula (I)06-28-2012
20100081658HETEROCYCLIC ANTIVIRAL COMPOUNDS - Compounds having the formula I wherein R04-01-2010
20120252811COMBINATIONS OF THERAPEUTIC AGENTS FOR TREATING CANCER - The invention relates to a combination comprising a Bcr-Abl, c-Kit and PDGF-R tyrosine kinase inhibitor; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.10-04-2012
20110207735CYANOPYRIMIDINONES - The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.08-25-2011
20100048569DIAZOLE DERIVATIVES - The present invention relates to diazole derivatives of the general formula02-25-2010
20100048568PYRIMIDINE HYDRAZIDE COMPOUNDS AS PGDS INHIBITORS - This invention is directed to a compound of formula (I):02-25-2010
20120178756COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.07-12-2012
20100286147FUNGICIDAL AMIDES - Disclosed are compounds of Formulae 1 and 1A (including all geometric and stereoisomers), N-oxides, and salts thereof,11-11-2010
20100009987AMINOTHIAZOLE DERIVATIVES AS INHIBITORS OF MARK - Compounds of formula (I): inhibit microtubule affinity regulating kinase (MARK) and therefore find use in treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.01-14-2010
20100009988PIPERAZINYL-, PIPERIDINYL- AND MORPHOLINYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)01-14-2010
20100173909PIPERIDINE COMPOUNDS AND USES THEREOF - 596 - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.07-08-2010
20100267723Imidazole Substituted Pyrimidines - A compound of formula (I)10-21-2010
20120264752DUAL-ACTING ANTIHYPERTENSIVE AGENTS - The invention is directed to compounds having the formula:10-18-2012
20120232079NOVEL ACYLPIPERAZINONES AND THEIR USE AS PHARMACEUTICALS - The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.09-13-2012
20120232078Novel Medicaments - Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.09-13-2012
20110003814PYRIMIDINES USEFUL AS MODULATORS OF VOLTAGE-GATED ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated ion 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.01-06-2011
20110003813SUBSTITUTED BIARYL PIPERAZINYL-PYRIDINE ANALOGUES - Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula:01-06-2011
20100190789PIPERIDINE/PIPERAZINE DERIVATIVES - The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(═O)—; —O—C(═O)—; C(═O)—C(═O)—; —NR07-29-2010
20110046135NEW COMPOUNDS I - The present application relates to new compounds of formula (I),02-24-2011
20110046134NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE - The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.02-24-2011
20120322802NOVEL 2, 4-PYRIMIDINE DERIVATIVES AND USE THEREOF - The present invention relates to novel 2,4-pyrimidine derivatives and a use thereof, and more particularly, to pyrimidine derivatives which are effective for systemic lupus erythematosus, a composition for preventing and treating systemic lupus erythematosus comprising the same as an active ingredient and a method for screening the same. The present inventors found novel materials inhibiting surface translocation of gp96 by mimicking a function of AIMP1 which is a molecular anchor for an intracellular residence of gp96, and identified in vitro and in vivo activity of the materials for preventing and treating SLE by alleviating SLE plasma in autoimmune diseases. Therefore, the present invention provides a novel method for screening a therapeutic agent for SLE, and preventing or treating SLE using the mechanism.12-20-2012
20120270875PYRIMIDINE AMIDE COMPOUNDS - Provided herein are compounds of the formula (I):10-25-2012
20110237586BIARYL COMPOSITIONS AND METHODS FOR MODULATING A KINASE CASCADE - The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I:09-29-2011
20100249132IMIDAZOLE DERIVATIVES - Compounds of the formula (I), in which R09-30-2010
20100249131MORPHOLINO PYRIMIDINE DERIVATIVES USED IN DISEASES LINKED TO MTOR KINASE AND/OR PI3K - A compound of formula (I) or a pharamaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.09-30-2010
20100160323NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE - The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.06-24-2010
20100234375HIV INHIBITING 5-(HYDROXYMETHYLENE AND AMINOMETHYLENE) SUBSTITUTED PYRIMIDINES - This invention concerns 5-(hydroxymethylene and aminomethylene)pyrimidine derivatives having HIV (Human Immunodeficiency Virus) replication inhibiting properties, to the preparation thereof and to pharmaceutical compositions comprising these compounds.09-16-2010
20100234376[4,5']Bipyrimidinyl-6,4'-Diamine Deriviatives as Protein Kinase Inhibitors - The invention provides a novel class of compounds of the Formula I:09-16-2010
20100234374Heterocycle Substituted Ketone Derivatives as Histone Deacetylase (HDAC) Inhibitors - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.09-16-2010
20120277232Pyridine and Pyrazine Derivative for the Treatment of CF - The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.11-01-2012
20100204231AMINO-THIAZOLYL-PYRIMIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER - The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.08-12-2010
20100204233IMIDAZOLE DERIVATIVES - The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1.08-12-2010
20100204230PIPERAZINE DERIVATIVES FOR TREATMENT OF AD AND RELATED CONDITIONS - Compounds of formula (I) selectively inhibit production of Aβ(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(β) in the brain.08-12-2010
20100204229FUNGICIDE HETEROCYCLYL-PYRIMIDINYL-AMINO DERIVATIVES - The present invention relates to heterocyclyl-pyrimidinyl-amino derivatives of formula (I)08-12-2010
20110294811ABT-263 CRYSTALLINE FORMS - ABT-263 free base and crystalline forms thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.12-01-2011
20100168105Spirocyclopropyl Piperidine Derivatives - Disclosed herein is at least one piperidine derivative, at least one pharmaceutical composition comprising at least one piperidine derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith07-01-2010
20100168104HIV INHIBITING 5-AMIDO SUBSTITUTED PYRIMIDINES - This invention concerns pyrimidine derivatives of formula07-01-2010
20100168107IMIDAZOLE COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS - The present invention relates to compounds of the Formula I07-01-2010
20100168106Amino-5-(5-membered)heteroarylimidazolone Compounds And The Use Thereof For Beta-secretase Modulation - The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I07-01-2010
20100144732PYRIMIDINE KINASE INHIBITORS - The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein Q, X, Y, Z, R06-10-2010
20100173910TRIAMINOPYRIMIDINE CYCLOBUTENEDIONE DERIVATIVES USED AS PHOSPHATASE CDC25 INHIBITORS - The present invention relates to triaminopyrimidine derivatives of formula (I)07-08-2010
20130023533NEW 5-ALKYNYL-PYRIDINES - 5-alkynyl-pyridine of general formula (I)01-24-2013
20130172349INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE - Compounds of formula I07-04-2013
200802426661-6-Substituted (3R,6R)-3-(2,3-Dihydro-1H-Inden-2-Yl)-2,5-Piperazinedione Derivatives as Oxytocin Receptor Antagonists For the Treatment of Preterm Labour, Dysmenorrhea and Endometriosis - The present invention relates to Compound S of Formula (I).10-02-2008
20090253698Brain, Spinal and Nerve Injury Treatment - A treatment for brain, spinal and nerve injury comprising use of a substance P receptor antagonist optionally in combination with a magnesium compound. There is also provided a formulation for use in this treatment comprising a substance P receptor antagonist and a magnesium compound.10-08-2009
20080234272Novel Piperazines as Antimalarial Agents - The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, especially malaria.09-25-2008
20080227782PYRIMIDINE AMIDE COMPOUNDS AS PGDS INHIBITORS - This invention is directed to a compound of formula (I):09-18-2008
20080221103New heterocyclic compounds - Provided herein are heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, wherein R09-11-2008
20090124620PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITOR - The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof.05-14-2009
20130137688NOVEL COMPOUNDS - This invention relates to compounds of formula I05-30-2013
20130172350PYRIMIDINE COMPOUNDS AND THEIR USES - Pyrimidine compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof, are useful are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases and in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever.07-04-2013
20130172348NOVEL AND SELECTIVE CCR2 ANTAGONISTS - The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain.07-04-2013
20130096123RADIATION SENSITISER COMPOSITIONS - The invention provides an oral liquid composition of a hypoxic radiation sensitiser comprising the radiation sensitiser in a concentration of greater than 5 mg/ml, and a method of treating a subject with a hypoxic condition comprising administration to the subject of a combination of a composition of the invention and radiation.04-18-2013
20130102605INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted thiazoles 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.04-25-2013
20080200461MODULATORS OF ACETYL-COENZYME A CARBOXYLASE AND METHODS OF USE THEREOF - The present invention provides compounds of formula I:08-21-2008
20110224211Anti-Viral Compounds, Compositions, And Methods Of Use - Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.09-15-2011
201102756332,4-DIAMINOPYRIMIDINE DERIVATES AS PTK2- INHIBITORS FOR THE TREATMENT OF ABNORMAL CELL GROWTH - The present invention encompasses compounds of general formula (1) wherein R11-10-2011
20110237585SUBSTITUTED PROPENYL PIPERAZINE DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I)09-29-2011
20130158032AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I:06-20-2013
20120283261SUBSTITUTED N-PHENYLPYRIMIDIN-2-AMINE ANALOGS AS INHIBITORS OF THE AXL KINASE - In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl 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 Axl 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.11-08-2012
20130184280SUBSTITUTED THIAZOLES AS VEGFR2 KINASE INHIBITORS - Disclosed herein are substituted thiazoles and their salts that are VEGFR2 kinase inhibitors, useful in the treatment of cancer.07-18-2013
20130184278APOPTOSIS-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.07-18-2013
20130184279N-((3-BENZYL)-2,2-(BIS-PHENYL)-PROPAN-1-AMINE DERIVATIVES AS CETP INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND CARDIOVASCULAR DISEASES - Compounds of formula Ia and Ib07-18-2013
20110306615NOVEL IMIDAZOLIDINE DERIVATIVE AND USE THEREOF - According to the present invention, a compound represented by formula (I):12-15-2011
20120004229SUBSTITUTED DIKETOPIPERAZINES AND THEIR USE AS OXYTOCIN ANTAGONISTS - Compounds of formula (1)01-05-2012
201200289792-(PIPERIDIN-1-YL)-4-HETEROCYCLYL-THIAZOLE-5-CARBOXYLIC ACID DERIVATIVES AGAINST BACTERIAL INFECTIONS - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.02-02-2012
20120028978SUBSTITUTED BICYCLIC HCV INHIBITORS - Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.02-02-2012
20130196993N-HETEROARYL COMPOUNDS - This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.08-01-2013
20120295907INSECTICIDAL COMPOUNDS - The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.11-22-2012
20120088768PINANE-SUBSTITUTED PYRIMIDINEDIAMINE DERIVATIVES USEFUL AS AXL INHIBITORS - Pinane-substituted pyrimidinediamine derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with Axl catalytic activity are also disclosed.04-12-2012
20120095001SUBSTITUTED-1,3,8-TRIAZASPIRO[4.5]DECANE-2,4-DIONES - The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.04-19-2012
20120095000COMPOUNDS FOR ACTIVATING TGF-BETA SIGNALING - Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-β signaling are described.04-19-2012

Patent applications in class Plural ring nitrogens in the additional hetero ring (e.g., imidazole, pyrazine, etc.)

Patent applications in all subclasses Plural ring nitrogens in the additional hetero ring (e.g., imidazole, pyrazine, etc.)