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Additional hetero ring which is not part of 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

514359000 - Five-membered hetero ring containing at least one nitrogen ring atom (e.g., 1,2,3-triazoles, etc.)

514408000 - The five-membered hetero ring consists of one nitrogen and four carbons

514410000 - Polycyclo ring system having the five-membered hetero ring as one of the cyclos

514412000 - Bicyclo ring system having the five-membered hetero ring as one of the cyclos

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Entries
DocumentTitleDate
20100076049NOVEL OXINDOLE DERIVATIVE - A compound or a pharmaceutically acceptable salt thereof of the present invention is represented by the following general formula (I):03-25-2010
20130041008COMPOUNDS FOR ENZYME INHIBITION - One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.02-14-2013
20130210885CRYSTALLINE FORMS OF L-MALIC ACID SALT OF SUNITINIB - The present invention relates to crystalline forms of L-malic acid salt of sunitinib and its preparation. The crystalline forms of the present invention are designated as Form V and Form VI of L-malic acid salt of sunitinib. Formula (I).08-15-2013
20100144823NOVEL INDOLE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.06-10-2010
20100144822Use of Inhibitors of the Degradation of P27, in Particular Argyrin and Derivatives Thereof, for the Treatment of Proliferative Diseases - The present invention relates to the use of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular Argyrin and derivatives thereof, preferably Argyrin A, for the treatment of proliferative diseases, such as cancer, as well as the derivatization of said macrocycles.06-10-2010
20130059899METHODS OF IDENTIFYING MODULATORS OF GPR17 - The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.03-07-2013
20130065933PHARMACEUTICAL COMPOSITION FOR PERORAL ADMINISTRATION OF DIINDOLYLMETHANE - The invention relates to pharmacy. It comprises block copolymer pharmaceutical compositions containing 3,3′-diindolylmethane (DIM). The pharmaceutical composition for peroral administration comprises 3,3′-diindolylmethane as an active component and a target additive, the target additive being a block copolymer of oxyethylene and oxypropylene, in which the content of the hydrophobic block is less than 50 mass % and the molecular mass of the hydrophilic block is equal to 2,250 Da or more, at a ratio of the active component to the selected block copolymer varying between 10:1 and 2:1.03-14-2013
20120115922SMAC MIMETEC - A SMAC mimetic and pharmaceutical compositions thereof and methods of use.05-10-2012
20090012145THERAPEUTIC ESTERS - A compound comprising01-08-2009
20110257238Heteroaryl Dihydroindolones as Kinase Inhibitors - The present invention provides a compound represented by the formula:10-20-2011
20090176856MUSCARINIC RECEPTOR ANTAGONISTS - This present invention generally relates to muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.07-09-2009
20110003877SMAC Mimetic - A SMAC mimetic and pharmaceutical compositions thereof and methods of use.01-06-2011
20100120885Novel Derivatives of Psammaplin A, A Method For Their Synthesis And Their Uses For The Prevention Or Treatment Of Cancer - Derivatives of psammaplin A responding to formula (I), a method for their synthesis and their use for the preparation of a medicament for preventing and for treating a tumor or a cancer. Formula (I).05-13-2010
20090258920INJECTABLE FORMULATION OF ANTIBIOTIC AND SOLUTION FOR INTRAVENOUS ADMINISTRATION THEREOF - A pharmaceutical composition for injection comprising a depsipeptide antibiotic, WAP-8294A10-15-2009
20110301216ANTICANCER AND ANTIMICROBIAL COMPOUNDS FROM ANTARCTIC EXTREMOPHILIC MICROORGANSIMS - The present disclosure describes the isolation of extremophilic microorganisms from the Lakes of Schirmacher Oasis located in the East Antarctic Dronning Maud Land. The isolated organisms were characterized and certain pigments produced by these microorganisms were isolated. The present disclosure teaches that the isolated pigments exhibit anticancer and antimicrobial properties and can be used as new therapies for the treatment and prevention of cancer and microbially-mediated diseases.12-08-2011
20100292290NOVEL PROCESS TO PREPARE ALMOTRIPTAN - The present invention relates to a novel process for the preparation of almotriptan and pharmaceutically acceptable salts thereof, which affords product conveniently and efficiently with commercially acceptable yields and purity. The present invention also relates to a novel synthetic intermediate used in the process.11-18-2010
20110288143BLADDER CANCER TREATMENT AND METHODS - Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, the compositions comprise an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.11-24-2011
20090291998EPONEMYCIN AND EPOXOMICIN ANALOGS AND USES THEREOF - The present invention provides compounds having formula (1): wherein R11-26-2009
20100113555Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.05-06-2010
20100099731Use of Endothelial Interrupters in the Treatment of Neurodegenerative Diseases - In various embodiments, the present invention relates generally to methods of treating at least one neurodegenerative disease by administering a medicament comprising an endothelial interrupter.04-22-2010
20090286846Therapeutic use of N-(1H-Indolyl)-1H-indole-2-carboxamide derivatives - The invention relates to therapeutic use of compounds of general formula (I):11-19-2009
20080275101Solid Salt Forms Of A Pyrrole Substituted 2-Indolinone - The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.11-06-2008
20080287519Amorphous eletriptan hydrobromide and process for preparing it and other forms of eletriptan hydrobromide - The invention encompasses amorphous eletriptan hydrobromide, processes for preparing it and pharmaceutical compositions of it. The invention also relates to processes for preparing other forms of eletriptan hydrobromide such as Form α and Form β.11-20-2008
20090298904NOVEL PEPTIDES FROM ACTINOMADURA NAMIBIENSIS - The disclosure relates to a compound of the formula (I)12-03-2009
20120295948INDIRUBIN-3'-OXIME DERIVATIVES AS POTENT CYCLIN DEPENDENT KINASE INHIBITORS - The present invention relates to an indirubin-3′-oxime derivative as potent cyclin dependent kinase inhibitor with anti-cancer activity. More particularly, this invention relates to an indirubin-3′-oxime derivative as potent cyclin dependent kinase inhibitor having excellent anti-cancer activity against human lung cancer cell, human fibro sarcoma cell, human colon cancer cell, human leukemia cell, human stomach cancer cell, human nasopharyngeal cancer cell and/or human breast cancer cell.11-22-2012
20090264494USE OF NEUROPROTECTIVE 3-SUBSTITUTED INDOLONE COMPOSITIONS - The present invention include providing a therapeutically effective amount of a 3-substituted indolin-2-one compositions to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke10-22-2009
20120142749SOLID SALT FORMS OF A PYRROLE SUBSTITUTED 2-INDOLINONE - The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1, 2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.06-07-2012
20090163570BLADDER CANCER TREATMENT AND METHODS - Disclosed herein are various bladder cancer treatments and methods. The present disclosure can take advantage of propylene glycol concentrations and/or NAD(P)H:quinone oxidoreductase-1 (NQO1), Cytochrome P450 Oxidoreductase (P450R) and Glucose transporter 1 (Glut-1) protein expression in human transitional cell carcinoma of the bladder to offer individually targeted bladder cancer treatments.06-25-2009
20090186933INDOLE, AZAINDOLE AND RELATED HETEROCYCLIC PYRROLIDINE DERIVATIVES - This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.07-23-2009
20080234355DNA METHYL TRANSFERASE INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to inhibitors of DNMT containing zinc moiety derivatives that have enhanced or unique properties as inhibitors of DNA methyl transferases (DNMT) and their use in the treatment of DNMT related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.09-25-2008
20110230538PHARMACEUTICAL FOR USE IN THE TREATMENT OF URETEROLITHIASIS - The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di (lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R09-22-2011
20090062368DEUTERIUM-ENRICHED SUNITINIB - The present application describes deuterium-enriched sunitinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-05-2009
20110144179Substituted Heterocyclic Mercaptosulfonamide Metalloprotease Inhibitors - The present invention generally relates to substituted heterocyclic mercaptosulfonamide compounds, precursors, and derivatives as well as methods for the preparation of and pharmaceutical compositions comprising these compounds. These compounds are designed to be potent selective inhibitors of matrix metalloproteinases (MMPs), including, for example, gelatinases, collagenases, matrilysins, metalloelastase, stromelysin, and membrane-type 1 matrix metalloproteinase. These inhibitors may be used for the control of physiological and pathological processes and disease conditions in which MMPs are believed to play significant functions.06-16-2011
20110112164NOVEL POLYMORPHS AND PROCESSES FOR THEIR PREPARATION - The present invention relates to novel polymorph forms III and IV of sunitinib malate, pharmaceutical compositions comprising the novel polymorphs and the use of the pharmaceutical compositions. The present invention further relates to processes for the preparation of polymorph form I, III and IV of sunitinib malate.05-12-2011
20090258921INDOLE DERIVATIVES - Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof:10-15-2009
20080207728BICYCLIC ACYLTRYPTOPHANOLS - The present invention relates to acyltryptophanols of the general formula I,08-28-2008
20100179207COMPOUNDS - The present invention pertains generally to certain compounds of the deoxyactagardine A and B type. Such compounds are suitable for use in the treatment of microbial infections, for example 07-15-2010
20100144821COMPOUNDS AND METHODS FOR TREATING PROTEIN FOLDING DISORDERS - The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, Aβ protein or α-synuclein protein aggregation.06-10-2010
20090318525Process For Preparing A 3-Pyrrole Substituted 2-Indolinone Malate Salt - The invention relates to the malic acid salt of N-[2-(diethylamino)ethyl]-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide, to the use thereof as an intermediate for preparing the malic acid salt of sunitinib, and to pharmaceutical compositions comprising said malic acid salt of sunitinib.12-24-2009
20090111867INDOLE ACETIC ACIDS EXHIBITING CRTH2 RECEPTOR ANTAGONISM AND USES THEREOF - The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D04-30-2009
20100305182COMPOUNDS AND METHODS FOR MODULATING COMMUNICATION AND VIRULENCE IN QUORUM SENSING BACTERIA - The present invention provides compositions and methods for modulating the communication and virulence of quorum sensing bacteria. In various exemplary embodiments, the invention provides a combinatorial library of quorum sensing compounds including synthetic analogs of naturally occurring and non-naturally occurring acyl-homoserine lactone (AHL) analogs, and methods of synthesizing and using these compounds.12-02-2010
20090062367DEUTERIUM-ENRICHED ELETRIPTAN - The present application describes deuterium-enriched eletriptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-05-2009
20110086900COMPOSITIONS FOR PREVENTION/PROPHYLACTIC TREATMENT OF POISON IVY DERMATITIS - The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) Tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a composition containing at least one water soluble urushiol ester compound.04-14-2011
20110124700SYSTEMS AND METHODS OF CANCER STAGING AND TREATMENT - Methods of assessing the sensitivity of a cancer cell to a tyrosine kinase inhibitor are disclosed. Such methods include assessing the expression of miR-497 and correlating reduced expression with sensitivity to the tyrosine kinase inhibitor. Also disclosed are methods of assessing the sensitivity of a cell to a tyrosine kinase inhibitor that includes assessing the expression of FGF1, HOXC10, and/or LHFP. Additionally disclosed are methods of treating patients with tyrosine kinase inhibitors such as sunitinib based on results obtained from the disclosed methods and kits that facilitate the methods.05-26-2011
20110071206Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.03-24-2011
20100004308Benzofuran-3-yl(indol-3-yl) Maleimides as Potent GSK3 Inhibitors - Compounds of formula:01-07-2010
20110263670NOVEL POLYMORPHS OF SUNITINIB AND PROCESSES FOR THEIR PREPARATION - The present invention relates to novel polymorphs of sunitinib free base designated form II and form III and to processes for their preparation. The invention also relates to their use as APIs and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising said novel polymorphs and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.10-27-2011
20120302620NOVEL PYRONE-INDOLE DERIVATIVES AND PROCESS FOR THEIR PREPARATION - The present invention relates to a method for treating a variety of maladies and conditions; which comprises administering a formulation comprising an effective amount of a pyrone-indole derivative of formula (I):11-29-2012
20110257237PROCESS FOR THE PREPARATION OF CRYSTALLINE FORMS OF SUNITINIB MALATE - The present invention, relates to novel processes for the preparation of sunitinib malate formula (I), pharmaceutical compositions comprising said polymorph and the use of the said pharmaceutical compositions in the treatment of various forms of cancer.10-20-2011
20110190366SUBSTITUTED 2-INDOLINONE AS PTK INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.08-04-2011
20100152270PESTICIDE COMPOSITION COMPRISING A STRIGOLACTONE DERIVATIVE AND A FUNGICIDE COMPOUND - A composition comprising at least a strigolactone derivative (a) of general formula:06-17-2010
20090048327Polymorphs of Pyrrole Substituted 2-Indolinone Protein Kinase Inhibitors - The present invention relates to polymorphs of the 3-pyrrole substituted 2-indolinone compound 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide.02-19-2009
20110306647NOVEL POLYMORPHS OF SUNITINIB MALATE - The present invention provides a novel crystalline form of sunitinib malate, process for its preparation and to pharmaceutical composition containing it. The present invention also provides a process for preparation of sunitinib malate crystal form I. Thus, for example, sunitinib malate was added to water, the mixture was heated to 80 deg C. to obtain a clear solution and stirred for 30 minutes at 80 deg C., slowly cooled to room temperature and the solution was subjected to freeze drying at about −90 deg C. for 8 hours to give sunitinib malate crystalline form III.12-15-2011
200901315033,5 - SUBSTITUTED INDOLE COMPOUNDS HAVING NOS AND NOREPINEPHRINE REUPTAKE INHIBITORY ACTIVITY - The present invention relates to novel 3,5-substituted indole compounds of Formula (I) having nitric oxide synthase (NOS) inhibitory activity together with inhibitory activity at the norepinephrine transporter (NET), to pharmaceutical and diagnostic compositions containing them, and to their medical use.05-21-2009
20090076120Crystal of Aminopyrrolidine Derivative and Production Method Thereof - Two crystal forms of (R)-3-[2-(2-amino-5-trifluoromethoxybenzamido)acetamido]-1-(6-methylindol-3-ylmethyl)pyrrolidine which exhibit specific X-ray powder diffraction patterns or infrared absorption spectra, amorphous form thereof, a pharmaceutical composition containing the crystal or amorphous form as an active ingredient, as well as methods for preparing them are provided.03-19-2009
20120046330PHARMACEUTICAL COMPOSITIONS OF (R)-1-(2,2-DIFLUOROBENZO[D] [1,3]DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METH- YLPROPAN-2-YL)-1H-INDOL-5-YL) CYCLOPROPANECARBOXAMIDE AND ADMINISTRATION THEREOF - A pharmaceutical composition comprising Compound 1, (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.02-23-2012
20100273852PHARMACEUTICAL COMPOSITION - There is provided a pharmaceutical composition comprising (1) (R)-5,6-dimethoxy-2-[2,2,4,6,7-pentamethyl-3-(4-methylphenyl)-2,3-dihydro-1-benzofuran-5-yl]isoindoline, (2) a lipophilic component, and (3) a surfactant, which can stably and sufficiently provide improvement in the absorbability of the drug without being affected by the amount and quality of a meal.10-28-2010
20120252861Medical Compositions for Intravesical Treatment of Bladder Cancer - Anti-cancer coating compositions comprising 3-hydroxymethyl-5-aziridinyl-1-1-methyl-2-[1H-indole-4,7-dione]propenol (E09) are disclosed. More specifically, the coating compositions comprise EO9 and a formulation vehicle. The formulation vehicle improves the solubility and stability of EO9. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.10-04-2012
20120015999FORMULATIONS OF (R)-1-(2,2-DIFLUOROBENZO[D] [1,3] DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METHYLPRO- PAN-2-YL)-1H-INDOL-5-YL)CYCLOPROPANECARBOXAMIDE - The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith.01-19-2012
20120309808COMPOSITIONS AND METHODS FOR EPIGENETIC MODIFICATION OF NUCLEIC ACID SEQUENCES - Provided herein are pharmaceutical compositions and methods for treating disorders characterized by reduced expression of anti-oxidative stress enzymes in a subject. In one aspect, the present invention provides a method for inducing expression of anti-oxidative stress enzymes in a subject in need thereof. The method includes administering to the subject a therapeutically effective amount of a demethylating agent. The demethylating agent includes a phytochemical that induces expression of Nrf2 and Nrf2-mediated genes expressing anti-oxidative stress. Such phytochemicals include indoles, such as 3,3′-diindolylmethane (DIM) and indole-3-carbinol (I3C), and isothiocyanates, such as phenethyl isothiocyanate (PEITC) and sulforaphane (SFN).12-06-2012
20120309807METHODS AND COMPOSITIONS RELATED TO REGULATION OF CYTOKINE PRODUCTION BY GLYCOGEN SYNTHASE KINASE 3 (GSK-3) - This invention relates generally to a method of treating inflammation and associated diseases and disorders by administering an agent that inhibits glycogen synthase kinase 3 activity.12-06-2012
20110105580NOVEL POLYMORPHIC FORMS OF SUNITINIB BASE - The present invention relates to novel polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-2,4-dimethyl-1H-pyrrole-3-carboxamide-Sunitinib base (I). The present invention also relates to methods of preparing such polymorphic crystals.05-05-2011
201201229483-ALKYL-5-FLUOROINDOLE DERIVATIVES AS MYELOPEROXIDASE INHIBITORS - The invention relates to a compound of formula (Ia)05-17-2012
20090131502Biologically active compounds - The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease and diseases involving matrix or cartilate degradation.05-21-2009
20120232123LIQUID PHARMACEUTICAL COMPOSITIONS - Aqueous liquid pharmaceutical composition comprising a) almotriptan and b) at least one compound selected from i) 1′-methyl-5-((pyrrolidin-1-ylsulfonyl)methyl)spiro[indoline-3,3′-pyrrolidin]-2-ol, and ii) 3-(2-(dimethylamino)ethyl)-5-((pyrrolidin-1-ylsulfonyl)methyl)-1H-indol-2-ol.09-13-2012
20120252860Novel N, N'-Hydrazino-bis-isatin Derivatives with Selective Activity Against Multidrug-Resistant Cancer Cells - The invention is directed to a compound of Formula (I),10-04-2012
20100048662Novel Pyrone-Indole Derivatives and Process for Their Preparation - The present invention relates to novel pyrone-indole derivatives, pharmaceutical formulations containing them, and use of the compounds in the manufacture of Medicaments for treating or preventing various diseases.02-25-2010
20120258995New Indolinone Protein Kinase Inhibitors - The present invention relates to new indolinone compounds and their pharmaceutically acceptable salts and prodrugs for treating and preventing VEGFR related cellular disorders such as cancer.10-11-2012
20120264803METHOD FOR PREDICTING THERAPEUTIC EFFECTS OF CHEMOTHERAPY ON HEPATOCELLULAR CARCINOMA PATIENTS - The present invention provides a method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients who have been treated with transarterial embolization and an antitumor agent for treating cancer patients who have been predicted to have a high probability of obtaining sufficient therapeutic effects from such chemotherapy. The present invention also provides a method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients who have been treated with transarterial embolization using the expression level of PDGF-BB or IL-8 as an indicator and an antitumor agent for treating cancer patients who have been predicted to have a high probability of obtaining therapeutic effects by such prediction method.10-18-2012
20120322844SUBSTITUTED 2-INDOLINONE AS PTK INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.12-20-2012
20110319463PREVENTIVE OR THERAPEUTIC AGENTS FOR OPTIC NERVE DISORDERS COMPRISING 4,6-DICHLORO-1H-INDOLE-2-CARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF AS ACTIVE INGREDIENTS - A method for preventing or treating an optic nerve disorder, inhibiting retinal nerve cell death or recovering a neurofilament light chain expression level by administering to a patient a pharmacologically effective amount of at least one of the compound represented by the following formula (1):12-29-2011
20120101143Compounds Having Activity in Increasing Ion Transport by Mutant-CFTR and Uses Thereof - The invention provides compositions, pharmaceutical preparations and methods for increasing activity (e.g., ion transport) of the mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR), e.g., DF508 CFTR, G551D-CFTR, G1349D-CFTR, or D1152H-CFTR, that are useful for the treatment of cystic fibrosis (CF). The compositions and pharmaceutical preparations of the invention may comprise one or more phenylglycine-containing compounds or sulfonamide-containing compounds of the invention, or an analog or derivative thereof.04-26-2012
20120289572Nicotinic Acetylcholine Receptor Sub-Type Selective Amides of Diazabicycloalkanes - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).11-15-2012
20120289571POLYMERIC CONJUGATES OF AROMATIC AMINE CONTAINING COMPOUNDS INCLUDING RELEASABLE UREA LINKER - The present invention relates to releasable urea linker systems involving amine-containing chemical compounds and biologically active agents. In particular, the present invention relates to reversibly releasable linkers based on intramolecular cyclization-assisted releasable urea linkages to aromatic amine-containing compounds. The present invention also relates to polymeric conjugates of indolinone-based tyrosine kinase inhibitors.11-15-2012
20130012564SMAC Mimetic - A SMAC mimetic and pharmaceutical compositions thereof and methods of use.01-10-2013
20100130581COMPOUNDS AND METHODS FOR THE TREATMENT OF PAIN - This invention relates to derivatives of an endomorphin, or of an endomorphin analog, comprising at least one moiety selected from a lipid moiety, a cyclitol moiety and a saccharide moiety.05-27-2010
20110160272METHODS AND COMPOSITIONS FOR USE OF ANGIOGENESIS INHIBITORS IN THE PREVENTION AND/OR CONTROL OF EPILEPSY - In accordance with some preferred embodiments, without limitation, the invention comprises methods and compositions for the prophylactic and/or antiepileptic administration of angiogenesis inhibitors in conjunction with seizures or traumatic insults to the brain, which administration may limit the extent of trauma-associated angiogenesis and/or decrease the likelihood that angiogenesis will give rise to regional epileptogenecity by preventing/reducing the associated increases in blood-brain barrier permeability among new or existing blood vessels along with their epileptogenic effects.06-30-2011
20090312390INHIBITORS OF GLYCOGEN SYNTHASE KINASE-3 (GSK-3) FOR TREATING GLAUCOMA - The use of inhibitors of GSK-3 useful for treating glaucoma is disclosed.12-17-2009
20080227843THERAPEUTIC USE OF N-(1H-INDOLYL)-1H-INDOLE-2-CARBOXAMIDE DERIVATIVES - The invention relates to therapeutic use of compounds of general formula (I):09-18-2008
20080227842Non-fluorescent chlorophyll catabolites - The invention relates to a compound of formula (I), or a pharmacologically or cosmetically acceptable salt or derivative thereof, wherein R09-18-2008
20080227841INTRAVESICAL APAZIQUONE ADMINISTRATION FOLLOWING TRANSURETHRAL RESECTION - Bladder cancer treatments include the intravesical administration of apaziquone immediately (e.g. within about 6 hours) following transurethral resection.09-18-2008
200802211933-AMINO CHROMANE DERIVATIVES - The present invention relates to 3-amino chromane derivatives; to compositions containing such compounds; to methods of synthesizing such compounds; and to methods of using such compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety.09-11-2008
20080221192Compounds 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, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC kinases.09-11-2008
20130131136NOVEL METHODS FOR PREDICTING THE RESPONSIVENESS OF A PATIENT AFFECTED WITH A TUMOR TO A TREATMENT WITH A TYROSINE KINASE INHIBITOR - The present invention relates to a method for predicting the responsiveness of a patient affected with a tumor to a treatment with a tyrosine kinase inhibitor such as sunitinib. More specifically, the method of the invention comprises a step of determining the expression level of one marker consisting of the FSHR in a biological sample obtained from said patient, and more specifically in the blood endothelial cells from the tumors.05-23-2013
20100280091TRI-SUBSTITUTED 2-BENZHYDRYL-5-BENZYLAMINO-TETRAHYDRO-PYRAN-4-OL AND 6-BENZHYDRYL-4-BENZYLAMINO-TETRAHYDRO-PYRAN-3-OL ANALOGUES, AND NOVEL 3,6-DISBUSTITUTED PYRAN DERIVATIVES - Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.11-04-2010
20110251253SOLID FORMS OF (R)-1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6- -FLUORO-2-(1-HYDROXY-2-METHYLPROPAN-2-YL)-1H-INDOL-5-YL) CYCLOPROPANECARBOXAMIDE - The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.10-13-2011
20110275690NEW CRYSTAL FORM OF SUNITINIB MALATE - A process for the preparation of a new crystal form of sunitinib malate, along with pharmaceuticals comprising the same are described.11-10-2011
20110275689Preparation of 3-Pyrrole Substituted 2-Indolinone Derivatives - The present invention relates to novel intermediates and further to the use of said intermediates in processes for the preparation of indolinone derivatives, in particular 3-pyrrole substituted 2-indolinones having amide moieties on the pyrrole ring. Such compounds are useful in die treatment of abnormal cell growth, such as cancer, in mammals.11-10-2011
20130150422COMPOSITIONS AND METHODS FOR TREATMENT OF CYSTIC FIBROSIS AND DISEASES ASSOCIATED WITH ABERRANT PROTEIN CELLULAR PROCESSING - The disclosure relates to resorcylic acid lactones and indolinone-containing compounds for use in treatment of diseases associated with aberrant protein processing, such as cystic fibrosis (CF; mucoviscidosis). The disclosure more generally relates to treatment of aberrant protein processing, such as errors in protein folding, trafficking or post-translational modification.06-13-2013
20100317709SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR COMPOUNDS - The invention relates to compounds, in particular 2-amino-3,4,5,-trisubstituted thiophenes, pharmaceutical compositions containing them and the uses of said compounds and compositions for diseases related to sphingosine-1-phosphate (S1P) receptors, predominantly S1P3 receptors. The diseases include cardiovascular diseases, atherosclerosis, cancer, pulmonary oedema, autoimmune disorders and Adult Respiratory Distress Syndrome.12-16-2010
20120029046CRYSTALLINE FORM OF SUNITINIB AND PROCESSES FOR ITS PREPARATION - The present invention relates to a novel crystalline form of sunitinib free base designated form I and to processes for its preparation. The invention also relates to its use as an API and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising the novel crystalline form and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.02-02-2012
20120077859C-substituted Diindolylmethane Compositions and Methods for the Treatment of Multiple Cancers - The present embodiment of the invention is generally directed to compositions comprising suspensions of poorly water soluble compounds recrystallized in nanoparticulate sizes ranging from 0.1 to 5 μm. In addition, the embodiment of the invention is directed to methods for preparation and administration of these compositions to a patient for prevention and treatment of disease states. In particular, the embodiment of the invention is directed to compositions comprising suspensions of poorly water-soluble compounds, such as antimitotics and antibiotics, in nanoparticulates and methods of prevention and treatment of chronic disease states, such as cancer, by intraperitoneal and intravenous administration of such compositions.03-29-2012
20130210886Novel Derivatives Useful as Antiviral Agents - The invention relates to compounds of formula (I) for use in the prevention and/or treatment of viral infections: Wherein X, Y, Z, T, R08-15-2013

Patent applications in class Additional hetero ring which is not part of the bicyclo ring system