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

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

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514233500 Bicyclo ring system having the additional hetero ring as one of the cyclos 1098
514233200 Ring nitrogen shared by two of the cyclos 249
Entries
DocumentTitleDate
20130045974NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS - Compounds of the formula Ia*****02-21-2013
20090203684Tyrosine kinase inhibitors - The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives of formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.08-13-2009
20100048553Spirocyclic Cyclohexane Compounds - Spirocyclic cyclohexane compounds corresponding to formula I02-25-2010
20100160309INHIBITORS OF JANUS KINASES AND/OR 3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASE-1 - The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.06-24-2010
20090029983NOVEL HETEROCYCLIC COMPOUNDS HAVING ANTI-HBV ACTIVITY - This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases.01-29-2009
20100087429SPIRO-TRICYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I04-08-2010
20130085140INDENOISOQUINOLINONE DERIVATIVES, MANUFACTURING METHOD AND MEDICAL USE THEREOF - Indenoisoquinolinone derivatives (I), the manufacturing method and the medical use thereof, which belong to pharmaceutical chemistry and organic chemistry field, are disclosed. These compounds can be used for treating several medical symptoms related to postmenopausal syndrome, uterine fibers deterioration and aortic smooth muscle cells proliferation, especially ER-(+) depend breast cancer. Meanwhile, these compounds can also be used for treating glioma and lung cancer, and have inhibiting effect on tumor metastasis effect on tumor metastasis.04-04-2013
20100113440PYRIMIDINE SUBSTITUTED MACROCYCLIC HCV INHIBITORS - Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.05-06-2010
20100113439Antifungal agents - Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.05-06-2010
20130029980FLAVIN DERIVATIVES - The present invention relates novel flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives.01-31-2013
20090186888NOVEL FUSED PYRROLOCARBAZOLES - The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.07-23-2009
20090156593Spirocyclic Azaindole Derivatives - The invention relates to substituted azaindole derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted azaindole derivatives for producing medicaments.06-18-2009
20090124611Pyrazolopyridine-1,4-Diamines and Analogs Thereof - Pyrazolopyridine-1,4-diamines and analogs thereof, e.g., pyrazolo[3,4-c]pyridine-1,4-diamines, pyrazolo[3,4-c]quinoline-1,4-diamines, 6,7,8,9-tetrahydro pyrazolo[3,4-c]quinoline-1,4-diamines, and pyrazolo[3,4-c]naphthyridine-1,4-di-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.05-14-2009
20100130487SPIRO-OXINDOLE COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds of formula (I):05-27-2010
20100029634Chemokine Receptor Modulators - The invention provides compounds of Formula (I)02-04-2010
20090306071Inhibitors of Janus Kinases - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.12-10-2009
20090118271Preventive or Therapeutic Agents for Pancreatic Cancer, Ovarian Cancer, or Liver Cancer Comprising a Novel Water-Soluble Prodrug - Preventive or therapeutic agents for pancreatic cancer, ovarian cancer, or liver cancer of the present invention comprise a water-soluble prodrug represented by formula 1 described below, or a pharmaceutically acceptable salt, or a hydrate or solvate of the prodrug or pharmaceutically acceptable salt,05-07-2009
20090105241THIO-SUBSTITUTED TRICYCLIC AND BICYCLIC AROMATIC METHANESULFINYL DERIVATIVES - The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A):04-23-2009
20090093474THIAZOLYL-DIHYDRO-INDAZOLE - The present invention relates to new thiazolyl-dihydro-indazoles of general formula (I)04-09-2009
20090093473Spiro-benzimidazoles as inhibitors of gastric acid secretion - The invention provides compounds of the formula (I)04-09-2009
20130059843Thiazolyl- and Oxazolyl-Isoquinolinones and Methods for Using Them - The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.03-07-2013
20090029982PROTEIN KINASE INHIBITORS - Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the structure (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Z, L2 and w are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.01-29-2009
20090012077Novel Compound - 827 - The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.01-08-2009
20090012076Tyrosine kinase inhibitors - The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.01-08-2009
20120238563NOVEL UNSATURATED TETRACYCLIC TETRAHYDROFURAN DERIVATIVES - This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT09-20-2012
20080293712Benzo[C][2,7]Naphtyridine Derivatives, Methods of Making Thereof and Methods of Use Thereof - The present invention relates to Benzo[c][2,7]naphthyridine Derivatives, compositions comprising an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for modulating PDK-1 activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c][2,7]naphthyridine Derivative.11-27-2008
20120101092SMALL MOLECULE INHIBITORS OF MDM2 AND THE USES THEREOF - The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).04-26-2012
20090099165Protein Kinase Inhibitors - Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure:04-16-2009
20110281862ALFA-CARBOLINE INHIBITORS OF NPM-ALK, RET, AND BCR-ABL - The present invention relates to compounds of formula (I)11-17-2011
20110144099ARYLOXY AND ARYLALKYLENEOXY SUBSTITUTED IMIDAZOQUINOLINES - Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.06-16-2011
20100280026COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.11-04-2010
20110136802SHIP1 MODULATORS AND METHODS RELATED THERETO - Compounds of structure (I):06-09-2011
20110136800ARYL-AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE - The present invention relates to compounds defined by formula I06-09-2011
20110172226NOVEL HYDRAZIDE CONTAINING TAXANE CONJUGATES - The present invention relates to compounds of formula I or salts thereof, wherein, R07-14-2011
20100056510Macrocyclic Compound - The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof:03-04-2010
20090075995MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF - Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including inflammatory and immune diseases, having the structure of formula (I):03-19-2009
20100120760BENZOFURAN-CARBOXAMIDE DERIVATIVES AS ANTIVIRAL AGENTS - A compound of the formula (I): as defined herein, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing a compound of the formula (I) for use in inhibiting hepatitis C virus polymerase and/or of treating or preventing an illness due to hepatitis C virus,05-13-2010
20110112086PYRIDINONE ANALOGS - The present invention provides pyridinone analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing pyridinone analogs, and methods of using the same.05-12-2011
20100137299SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.06-03-2010
20110294799Organic Compounds - The invention relates to compound of the formula I12-01-2011
20090170843(Poly) aminoacetamide derivatives of epipodophyllotoxin their process of preparation and their applications in therapeutics as anticancer agents - The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.07-02-2009
20100048552COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHBITORS - 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, Bcr-Abl(T315I), ALK, BLK, BMX, BRK, C-kit, c-RAF, CSK, c-SRC, EGFR, Fes, FGFR3, Flt3, Fms, Fyn, IGF-1R, IR, JAK(2), JAK(3), KDR, Lck, NLK, p70S6K, PDGFRα, Ros, SAPK2α, SGK, SIK, Syk, Tie2 and TrkB kinases.02-25-2010
20120065199SUBSTITUTED QUINOLINES FOR USE AS VEGF INHIBITORS - A compound of formula (I)03-15-2012
20120035170NOVEL UNSATURATED TETRACYCLIC TETRAHYDROFURAN DERIVATIVES - This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT02-09-2012
20110172224NOVEL HETEROCYCLES - The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.07-14-2011
20100125072SPIRO-OXINDOLE COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds of formula (I):05-20-2010
20090042876Pyrroloquinoline Derivatives And Their Use As Protein Kinases Inhibitors - The present invention relates to inhibitors of protein kinases of formula I:02-12-2009
20110172225ANTIFUNGAL AGENTS - Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.07-14-2011
20090298821HYDROXY AND ALKOXY SUBSTITUTED IH-IMIDAZONAPHTHYRIDINES AND METHODS - 1H-Imidazo[4,5-c]naphthyridin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.12-03-2009
20110269753HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS - Compounds of the formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, N-oxides, metabolites and prodrugs thereof. These compounds are phosphodiesterase type 4 (PDE4) inhibitors. They are useful in the treatment of a variety of allergic or inflammatory diseases including asthma, COPD, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, psoriasis, rheumatoid arthritis, ulcerative colitis, Crohn's disease, uveitis, NASH and lupus.11-03-2011
20080287432Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds of formula I, 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 AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.11-20-2008
20090318435PYRAZOLOPYRIDINES AND ANALOGS THEREOF - Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, and 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.12-24-2009
20090312317COUMARIN COMPOUNDS AND THEIR USE FOR TREATING CANCER - Coumarin compounds of formula (I):12-17-2009
20080312224Oxaphenanthrene Derivatives - The invention relates to compounds of the formula (I), in which R12-18-2008
20100173905HEPTACYCLIC COMPOUNDS AND THE PHARMACEUTICAL USES THEREOF FOR PREVENTING AND TREATING DIABETES AND METABOLIC SYNDROME - The invention discloses a new use of a class of heptacyclic compounds in the preparation of formulations for the prevention and treatment of diabetes and metabolic syndromes; the present invention also discloses a new class of heptacyclic compounds; the present invention also discloses a process for preparing the heptacyclic compounds and a composition containing the same. The heptacyclic compounds of the present invention can be used to effectively preventing or treating diseases such as diabetes and metabolic syndromes.07-08-2010
20120295903FLAVIN DERIVATIVES - The present invention relates novel flavin derivatives and other flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives. The invention also provides method of making novel flavin derivatives.11-22-2012
20120196854PHARMACEUTICAL COMPOSITION COMPRISING AROMATIC HETEROCYCLIC COMPOUND - A pharmaceutical composition comprising as an active ingredient, an aromatic heterocyclic compound represented by the formula (I):08-02-2012
20090029985PYRIDAZINE COMPOUNDS AND METHODS - The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.01-29-2009
20090029984SYNERGISTIC COMBINATION FOR THE TREATMENT OF PAIN (CANNABINOID RECEPTOR AGONIST AND OPIOID RECEPTOR AGONIST) - The invention relates to a pharmaceutical dosage form comprising an analgesic combination for simultaneous or sequential use which comprises a peripherally restricted cannabinoid CB1 receptor agonist having a brain C01-29-2009
20110207727Thio-subsituted Anthra [1, 2-d] imidazole- 6, 11-dione Dervatives, Preparation Method and application thereof - A series of novel thio-substituted anthra[1,2-d]imidazole-6,11-dione dervatives, and the preparation method and application of said derivatives, said application having a pharmaceutical composition containing said derivatives with therapeutically effective amount for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.08-25-2011
20090069314Hydroxyalkyl Substituted Imidazoquinoline Compounds and Methods - Certain imidazoquinolines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, and an aryl or heteroaryl substituent at the 7-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-α biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.03-12-2009
20090186887NOVEL PYRIMIDOTHIENOINDAZOLES - The invention relates to novel pyrimidothienoindazoles of formula (I)07-23-2009
20090054429ARYLINDENOPYRIDINES AND ARYLINDENOPYRIMIDINES AND RELATED THERAPEUTIC AND PROPHYLACTIC METHODS - This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula:02-26-2009
20090036441Indole Derivatives With Antitumor Activity - 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.02-05-2009
20080318942Fredericamycin Derivatives - The invention relates to new fredericamycin derivatives, to pharmaceutical drugs containing them or their salts, and to the use of the fredericamycin derivatives for the treatment of diseases, especially tumor diseases.12-25-2008
20090325951THIENYL-AND FURANYL-ISOQUINOLINONES AND METHODS FOR USING THEM - The present invention relates to substituted thienyl- and furanyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders.12-31-2009
20090023722AMIDE SUBSTITUTED IMIDAZOQUINOLINES - Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain amide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.01-22-2009
20090023721Novel Substituted Tetracyclic Tetrahydrofuran, Pyrrolidine and Tetrahydrothiophene Derivatives and Their Use as a Medicament - This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT01-22-2009
200900237202-Amino 1H-Imidazo Ring Systems and Methods - 1H-Imidazo ring systems (e.g., imidazopyridines, imidazoquinolines, imidazonaphthyridines, 6,7,8,9-tetrahydro imidazoquinolines and imidazonaphthyridines) with an amino substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.01-22-2009
20090209530INHIBITORS OF CYCLIN-DEPENDENT KINASES, COMPOSITIONS AND USES RELATED THERETO - The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.08-20-2009
20080261968Heterobicyclic metalloprotease inhibitors - The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.10-23-2008
200802619691,4-Dihydropyridine-Fused Heterocycles, Process for Preparing the Same, Use and Compositions Containing Them - This invention relates to compounds of formula (I)10-23-2008
20090221569USE OF LHRH ANTAGONISTS FOR INTERMITTENT TREATMENTS - The invention relates to methods of treatment or prophylaxis of physiological and/or pathological conditions with at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonistsuch that the at least one LHRH antagonist is administered in a dose, which does not cause chemical (hormonal) castration.09-03-2009
20090247514Spirolactam aryl cgrp receptor antagonists - Compounds of formula I:10-01-2009
20090253695Hydroxyalkyl Substituted Imidazonaphthyridines - Certain imidazonaphthyridines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-α biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.10-08-2009
20090156592Fungicidal Azocyclic Amides - Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof,06-18-2009
20080318943Compounds and Uses Thereof - 848 - This invention relates to novel compounds having the structural formula I below:12-25-2008
20100273791TRICYCLIC PYRAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS - The present invention relates to novel compounds of general formula (I),10-28-2010
20100184758BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS - Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.07-22-2010
20110112087Thia-triaza-cyclopentazulenes - The present invention encompasses compounds of general formula (1)05-12-2011
20100227859TRICYCLIC COMPOUNDS AS MATRIX METALLOPROTEINASE INHIBITORS - The present teachings relate to compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, R4, X, and Y are as defined herein. The present teachings also provide methods of making the compounds of formula I and methods of inhibiting matrix metalloproteinases, in particular, MMP-12, that may be involved in pathological disorders found in mammals, including a human.09-09-2010
201002106399H-PYRIMIDO[4,5-B]INDOLES, 9H-PYRIDO[4',3':4,5]PYRROLO[2,3-D]PYRIDINES, AND 9H 1,3,6,9 TETRAAZA-FLUORENES AS CHK1 KINASE FUNCTION INHIBITORS - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4′,3′:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.08-19-2010
200900759982-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors - The invention encompasses novel compounds of Formula I03-19-2009
20090075997DEUTERIUM-ENRICHED SATAVAPTAN - The present application describes deuterium-enriched satavaptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20110112088PYRAZOLES FOR THE TREATMENT OF OBESITY AND OTHER CNS DISORDERS - This invention relates to compounds of the formula:05-12-2011
20100222338BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I09-02-2010
20090258871Aza-Substituted Spiro Derivatives - A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided:10-15-2009
20090143375Tricyclic Lactam Derivatives, Their Manufacture and Use as Pharmaceutical Agents - Objects of the present invention are the compounds of formula I06-04-2009
20080269209Pyrazoloisoquinoline Derivatives - New compounds of formula I, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors. (I)10-30-2008
20090062272IMIDAZOQUINOLINYL SULFONAMIDES - Imidazoquinolinyl, imidazopyridinyl, and imidazonaphthyridinyl sulfonamide compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.03-05-2009
20110034455INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 - This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.02-10-2011
20100331325NOVEL SUBSTITUTED TETRACYCLIC TETRAHYDROFURAN, PYRROLIDINE AND TETRAHYDROTHIOPHENE DERIVATIVES - This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT12-30-2010
20100216785PHARMACEUTICAL COMPOSITIONS - Microemulsions of pharmaceutical compositions comprising, the following components (% by weight), the sum of the components being 100%: 08-26-2010
20090215766TETRACYCLIC INHIBITORS OF JANUS KINASES - The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.08-27-2009
20120302563SUBSTITUTED NORINDENOISOQUINOLINES, SYNTHESES THEREOF, AND METHODS OF USE - Described herein are substituted norindenoisoquinoline compounds, and pharmaceutical compositions and formulations comprising the norindenoisoquinoline compounds. Also described herein are methods for using the compounds for the treatment and/or prevention of topoisomerase mediated diseases, such as cancer.11-29-2012
201203025624H-THIENO[3,2-C]CHROMENE-BASED INHIBITORS OF NOTUM PECTINACETYLESTERASE AND METHODS OF THEIR USE - Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.11-29-2012
20090111804ARYLINDENOPYRIMIDINES AND THEIR USE AS ADENOSINE A2a - This invention relates to novel arylindenopyrimidines A, B, and C, and their therapeutic and prophylactic uses. Disorders treated and/or prevented using these compounds include Parkinson's Disease.04-30-2009
20090075996HETEROTETRACYCLIC COMPOUNDS AS TPO MIMETICS - 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 TPO activity, particularly diseases or disorders that involve thrombocytopenia.03-19-2009
20100311739Naphthalene Diimide Compounds - The invention relates to novel compounds which are naphthalene diimides of general formula (I). The compounds are used in therapy, particularly in cancer treatment.12-09-2010
20080214537BRIDGED PHENANTHRIDINES - Bridged phenanthridine compounds having the structure of formula I or of formula II are provided:09-04-2008
20080214536Amido-Substituted 6-Phenylphenanthridines - Compounds of a certain formula (I)09-04-2008
20080255110IMIDAZOQUINOLINE DERIVATIVES AS ADENOSINE A3 RECEPTOR LIGANDS - This invention is directed to a compound of formula (I),10-16-2008
20110053928PYRIMIDOTHIENOINDAZOLES - The invention relates to novel pyrimidothienoindazoles of formula (I), processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.03-03-2011
20100179140INDENOISOQUINOLINONE ANALOGS AND METHODS OF USE THEREOF - The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog.07-15-2010
20110190288DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) FOR USE IN TREATMENT OF DISEASES ASSOCIATED WITH A PTEN DEFICIENCY - A compound having the structure set forth in Formula (I) and Formula (II):08-04-2011
20110136801Novel Compounds - The present invention provides compounds of formula (I):06-09-2011
201000296356,7,8,9-SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO[3,2-B]INDOL-2-ONES USEFUL AS ANTI-INFECTIVE PHARMACEUTICAL AGENTS - This invention concerns the compounds02-04-2010
20100016299Substituted benzoxepino-isoxazoles and use thereof - The present application relates to novel substituted benzoxepinoisoxazole derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis, restenosis and ischemias.01-21-2010
20100004234SPECIFIC KINASE INHIBITORS - Resorcylic acid lactones having a C5-C6 cis double bond and a ketone at C7 and other compounds capable of Michael adduct formation are potent and stable inhibitors of a subset of protein kinases having a specific cysteine residue in the ATP binding site.01-07-2010
20100190786INDOLIN-2-ONES AND AZA-INDOLIN-2-ONES - The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to certain indolin-2-ones and aza-indolin-2-ones which possess anti-tumour activity and are accordingly useful in methods of treatment of the human or animal body, in particular such compounds are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.07-29-2010
20120040978Heterocyclic Fused Cinnoline M1 Receptor Positive Allosteric Modulators - The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.02-16-2012
201202088099H-PYRROLO[2,3-B: 5,4-C'] DIPYRIDINE AZACARBOLINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c′]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers and salts of said substances of formula (I) and to the therapeutic use thereof for treating cancer.08-16-2012
20090186886Tricyclic 1,2,4-Triazine Oxides and Compositions for Therapeutic Use in Cancer Treatments - The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I07-23-2009
20120101091VIRAL POLYMERASE INHIBITORS - The present application provides compounds of formula I wherein X, Y, R04-26-2012
20100331324FUSED HETEROCYCLIC COMPOUNDS USEFUL AS MODULATORS OF NUCLEAR HORMONE RECEPTOR FUNCTION - Disclosed are fused heterocyclic compounds of Formula (I) or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.12-30-2010
20120115862DIBENZOCYCLOHEPTATONE DERIVATIVES AND PHARMACEUTICAL AGENTS CONTAINING SAID COMPOUNDS - The present invention relates to compounds of the formula I05-10-2012
20120022061BENZO [C] PHENANTHRIDINES AS ANTIMICROBIAL AGENTS - The present invention provides compounds of formula I: formula (I) wherein X01-26-2012
20120022060Tricyclic Azaindoles - Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.01-26-2012
20080287433 DERIVATIVES OF ARTEMISININ, AND THEIR USES IN THE TREATMENT OF MALARIA - A new artemisinin derivatives, of following general formula (I):11-20-2008
201201085842H OR 3H-BENZO[E]INDAZOL-1-YL CARBAMATE DERIVATIVES, THE PREPARATION AND THERAPEUTIC USE THEREOF - Compounds corresponding to the formula (I)05-03-2012
20120108583Tricyclic Compounds As mPGES-1 Inhibitors - The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.05-03-2012
20120071473TRICYCLIC COMPOUND DERIVATIVES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY DISORDERS AND IMMUNOMODULATORY DISORDERS - Provided are compounds of the formula (I):03-22-2012
20120071472RIMINOPHENAZINES WITH 2-(HETEROARYL)AMINO SUBSTITUENTS AND THEIR ANTI-MICROBIAL ACTIVITY - The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating 03-22-2012
20110065698NOVEL PROTEIN KINASE MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate protein kinase CK2 activity, Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.03-17-2011
20110105494HETEROARYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2A RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease.05-05-2011
20110105493HETEROCYCLYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease.05-05-2011
20110105492ARYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease05-05-2011
20090131424THIAZOLYL-DIHYDRO-CHINAZOLINE - Disclosed are compounds of general formula (I),05-21-2009
20090131423Tyrosine Kinase Inhibitors - The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.05-21-2009
20120129849DEUTERATED SERINE-THREONINE PROTEIN KINASE MODULATORS - The present invention provides deuterated compounds having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. The deuterated compounds of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such deuterated compounds as therapeutic agents.05-24-2012
20120232074Imidazo [4, 5-C] Quinoline Derivatives As Bromodomain Inhibitors - Novel compounds of formula (I)09-13-2012
20100048554Spirocyclic Cyclohexane Compounds - Spirocyclic cyclohexane compounds corresponding to formula I02-25-2010
20100048551Tricyclic Compounds Useful as Inhibitors of Kinases - The present invention provides inhibitors of kinases, specifically IκB kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-κB-mediated diseases.02-25-2010
20120190678SUBSTITUTED PYRAZOLO-QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to substituted pyrazolo[4,3-h]quinazoline compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular PIM kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.07-26-2012
201101246393 BETA-HYDROXYSTEROID DEHYDROGENASE INHIBITORS - The present invention relates to methods of treating a patient infected by 05-26-2011
20110003805CONCOMITANT DRUG - Provided is a combination drug. The present invention provides a pharmaceutical agent comprising (1) a HER2 inhibitor having a pyrrolopyrimidine skeleton or pyrazolopyrimidine skeleton, and (2) not less than one pharmaceutical agent selected from an mTOR inhibitor, a PI3 kinase inhibitor and a cMet inhibitor in combination.01-06-2011
20120322797SELECTIVE BETA-GLUCURONIDASE INHIBITORS AS A TREATMENT FOR SIDE EFFECTS OF CAMPTOTHECIN ANTINEOPLASTIC AGENTS - Compounds, compositions and methods are provided that comprise selective β-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial β-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial β-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.12-20-2012
20110237581DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) and Formula (II):09-29-2011
20100168096ACYLGUANIDINE DERIVATIVE OR SALT THEREOF - [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT07-01-2010
20130012505BENZONAPHTHYRIDINAMINES AS AUTOTAXIN INHIBITORS - The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.01-10-2013
20110160202PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS - Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.06-30-2011
20110160201COMPOUND WITH SEROTONINERGIC ACTIVITY, PROCESS FOR PREPARING IT AND PHARMACEUTICAL COMPOSITION COMPRISING IT - Compound of formula (I) in which R1, R2 and R3 are defined in the following description, and the pharmaceutically acceptable acid-addition or base-addition salts thereof. The invention also relates to a process and an intermediate for preparing it, and to a pharmaceutical composition comprising it. The invention also relates to the use of a novel 2H-pyrrolo[3,4-c]quinoline compound for preparing a pharmaceutical composition that is active in the treatment of disturbances of the serotoninergic system.06-30-2011
201301723364-ANILINOFURO[2,3-B]QUINOLINE DERIVATIVES, THEIR PREPARATION PROCESSES, AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME - Disclosed herein are novel 4-anilinofuro[2,3-b]quinoline derivatives of formula (I):07-04-2013
20080234259Novel Cannabinoid Receptor Ligands, Pharmaceutical Compositions Containing Them, and Process For Their Preparation - The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).09-25-2008
20130178470HETEROCYCLIC AMINOBERBAMINE DERIVATIVES, THE PREPARATION PROCESS AND USE THEREOF - The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.07-11-2013
20130143877COMPOSITION COMPRISING TETRACYCLIC COMPOUND - A composition which comprises substance represented by Formula (I),06-06-2013
20080214538Pyridoindolone Derivatives Substituted in the 3-Position by a Phenyl, Their Preparation and Their Application in Therapeutics - The present disclosure relates to pyridoindolone derivatives of general formula (I):09-04-2008
20130172337Imidazo[4,5-c]quinolines as DNA-PK inhibitors - The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).07-04-2013
20130096112FURO[3,2-G]CHROMENE COMPOUNDS AND USES THEREOF - Disclosed are furo[3,2-g]chromene derivatives represented by formula (I), stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as uses thereof as estrogen receptor modulators.04-18-2013
20130116248SUBSTITUTED IMIDAZOQUINOLINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to substituted imidazo[4,5-c]quinoline derivatives, the compounds of formula (I), wherein R05-09-2013
20130102598INDENOQUINOLONE COMPOUND, PREPARATION METHOD AND USE THEREOF - An indenoquinolone compounds of Formula (A) is disclosed, wherein the definition of each group is described in the description. These compounds may specifically inhibit topoisomerase I, and they have good activities against many kinds of human tumor cells, such as lung cancer, colon cancer, breast cancer, liver cancer and the like. They can be used in the manufacture of antitumor drugs. The method for preparing the compound of formula (A), and pharmaceutical compositions containing such compounds and the use in the manufacture of antitumor drugs are also disclosed.04-25-2013
20130102599PYRAZOLO [4,3-C] CINNOLIN-3-ONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one compounds of formula (I)04-25-2013
20130143878SUBSTITUTED DIBENZONAPHTHYRIDINES, PHARMACEUTICAL USES THEREOF AND PROCESSES THERFOR - The invention described herein pertains to substituted dibenzonaphthyridine compounds, pharmaceutical compositions, and formulations comprising the dibenzonaphthyridine compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.06-06-2013
20130150359PYRAZOLOQUINOLINES - The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formula (II) or (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of its salts06-13-2013
200902755763-HETEROARYL-3,5-DIHYDRO-4-OXO-4H-PYRIDAZINO[4,5-B]INDOLE-1-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE - A subject-matter of the invention is the compounds of general formula (I)11-05-2009
20130158024TRICYCLIC NECROSTATIN COMPOUNDS - The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described.06-20-2013
20130184272DIABETES THERAPEUTIC AGENT - The problem of the present invention is to provide a compound useful for the prophylaxis or treatment of diseases related to the control of the differentiation of muscle cell or adipocyte differentiation, such as diabetes, obesity, dyslipidemia, and having a superior efficacy.07-18-2013
20130184271Methods for Treating Parkinson's Disease Using Pro-Neurogenic Compounds - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.07-18-2013
20110312956ARYLINDENOPYRIMIDINES WITH REDUCED hERG CHANNEL BINDING - This invention provides novel arylindenopyrimidines of the Formula (I),12-22-2011
20130190307FUSED HETEROARYLS AND THEIR USES - Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.07-25-2013
20130190306DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) and Formula (II):07-25-2013
20130190305NEW 5,8-DIHYDRO-6H-PYRAZOLO[3,4-H]QUINAZOLINES AS IGF-1R/IR INHIBITORS - The present invention encompasses compounds of general formula (I)07-25-2013
20130102597COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS - Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.04-25-2013
20090239859PROTEIN KINASE MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.09-24-2009

Patent applications in class Polycyclo ring system having the additional hetero ring as one of the cyclos

Patent applications in all subclasses Polycyclo ring system having the additional hetero ring as one of the cyclos