Entries |
Document | Title | Date |
20080214536 | Amido-Substituted 6-Phenylphenanthridines - Compounds of a certain formula (I) | 09-04-2008 |
20080214537 | BRIDGED PHENANTHRIDINES - Bridged phenanthridine compounds having the structure of formula I or of formula II are provided: | 09-04-2008 |
20080214538 | Pyridoindolone 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 |
20080234259 | Novel 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 |
20080255110 | IMIDAZOQUINOLINE DERIVATIVES AS ADENOSINE A3 RECEPTOR LIGANDS - This invention is directed to a compound of formula (I), | 10-16-2008 |
20080261968 | Heterobicyclic 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 |
20080261969 | 1,4-Dihydropyridine-Fused Heterocycles, Process for Preparing the Same, Use and Compositions Containing Them - This invention relates to compounds of formula (I) | 10-23-2008 |
20080269209 | Pyrazoloisoquinoline 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 |
20080287432 | Compounds 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 |
20080287433 | DERIVATIVES OF ARTEMISININ, AND THEIR USES IN THE TREATMENT OF MALARIA - A new artemisinin derivatives, of following general formula (I): | 11-20-2008 |
20080293712 | Benzo[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 |
20080312224 | Oxaphenanthrene Derivatives - The invention relates to compounds of the formula (I), in which R | 12-18-2008 |
20080318942 | Fredericamycin 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 |
20080318943 | Compounds and Uses Thereof - 848 - This invention relates to novel compounds having the structural formula I below: | 12-25-2008 |
20090012076 | Tyrosine 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 |
20090012077 | Novel 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 |
20090023720 | 2-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 |
20090023721 | Novel 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-HT | 01-22-2009 |
20090023722 | AMIDE 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 |
20090029982 | PROTEIN 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 |
20090029983 | NOVEL 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 |
20090029985 | PYRIDAZINE 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 |
20090036441 | Indole 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 |
20090042876 | Pyrroloquinoline Derivatives And Their Use As Protein Kinases Inhibitors - The present invention relates to inhibitors of protein kinases of formula I: | 02-12-2009 |
20090054429 | ARYLINDENOPYRIDINES AND ARYLINDENOPYRIMIDINES AND RELATED THERAPEUTIC AND PROPHYLACTIC METHODS - This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula: | 02-26-2009 |
20090062272 | IMIDAZOQUINOLINYL 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 |
20090069314 | Hydroxyalkyl 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 |
20090075995 | MODULATORS 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 |
20090075996 | HETEROTETRACYCLIC 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 |
20090075997 | DEUTERIUM-ENRICHED SATAVAPTAN - The present application describes deuterium-enriched satavaptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090075998 | 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors - The invention encompasses novel compounds of Formula I | 03-19-2009 |
20090093473 | Spiro-benzimidazoles as inhibitors of gastric acid secretion - The invention provides compounds of the formula (I) | 04-09-2009 |
20090093474 | THIAZOLYL-DIHYDRO-INDAZOLE - The present invention relates to new thiazolyl-dihydro-indazoles of general formula (I) | 04-09-2009 |
20090099165 | Protein 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 |
20090105241 | THIO-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 |
20090111804 | ARYLINDENOPYRIMIDINES 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 |
20090118271 | Preventive 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 |
20090124611 | Pyrazolopyridine-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 |
20090131423 | Tyrosine 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 |
20090131424 | THIAZOLYL-DIHYDRO-CHINAZOLINE - Disclosed are compounds of general formula (I), | 05-21-2009 |
20090143375 | Tricyclic Lactam Derivatives, Their Manufacture and Use as Pharmaceutical Agents - Objects of the present invention are the compounds of formula I | 06-04-2009 |
20090156592 | Fungicidal 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 |
20090156593 | Spirocyclic 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 |
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 |
20090186886 | Tricyclic 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 I | 07-23-2009 |
20090186887 | NOVEL PYRIMIDOTHIENOINDAZOLES - The invention relates to novel pyrimidothienoindazoles of formula (I) | 07-23-2009 |
20090186888 | NOVEL 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 |
20090203684 | Tyrosine 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 |
20090209530 | INHIBITORS 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 |
20090215766 | TETRACYCLIC 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 |
20090221569 | USE 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 |
20090239859 | 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 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 |
20090247514 | Spirolactam aryl cgrp receptor antagonists - Compounds of formula I: | 10-01-2009 |
20090253695 | Hydroxyalkyl 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 |
20090258871 | Aza-Substituted Spiro Derivatives - A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: | 10-15-2009 |
20090275576 | 3-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 |
20090298821 | HYDROXY 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 |
20090306071 | Inhibitors 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 |
20090312317 | COUMARIN COMPOUNDS AND THEIR USE FOR TREATING CANCER - Coumarin compounds of formula (I): | 12-17-2009 |
20090318435 | PYRAZOLOPYRIDINES 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 |
20090325951 | THIENYL-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 |
20100004234 | SPECIFIC 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 |
20100016299 | Substituted 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 |
20100029634 | Chemokine Receptor Modulators - The invention provides compounds of Formula (I) | 02-04-2010 |
20100029635 | 6,7,8,9-SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO[3,2-B]INDOL-2-ONES USEFUL AS ANTI-INFECTIVE PHARMACEUTICAL AGENTS - This invention concerns the compounds | 02-04-2010 |
20100048551 | Tricyclic 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 |
20100048552 | COMPOUNDS 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 |
20100048553 | Spirocyclic Cyclohexane Compounds - Spirocyclic cyclohexane compounds corresponding to formula I | 02-25-2010 |
20100048554 | Spirocyclic Cyclohexane Compounds - Spirocyclic cyclohexane compounds corresponding to formula I | 02-25-2010 |
20100056510 | Macrocyclic 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 |
20100087429 | SPIRO-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 I | 04-08-2010 |
20100113439 | Antifungal 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 |
20100113440 | PYRIMIDINE 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 |
20100120760 | BENZOFURAN-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 |
20100125072 | SPIRO-OXINDOLE COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds of formula (I): | 05-20-2010 |
20100130487 | SPIRO-OXINDOLE COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds of formula (I): | 05-27-2010 |
20100137299 | SPIRO-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 |
20100160309 | INHIBITORS 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 |
20100168096 | ACYLGUANIDINE DERIVATIVE OR SALT THEREOF - [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT | 07-01-2010 |
20100173905 | HEPTACYCLIC 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 |
20100179140 | INDENOISOQUINOLINONE 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 |
20100184758 | BETA 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 |
20100190786 | INDOLIN-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 |
20100210639 | 9H-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 |
20100216785 | PHARMACEUTICAL COMPOSITIONS - Microemulsions of pharmaceutical compositions comprising, the following components (% by weight), the sum of the components being 100%:
| 08-26-2010 |
20100222338 | 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 I | 09-02-2010 |
20100227859 | TRICYCLIC 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 |
20100273791 | TRICYCLIC PYRAZOLE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS - The present invention relates to novel compounds of general formula (I), | 10-28-2010 |
20100280026 | COMPOSITIONS 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 |
20100311739 | Naphthalene 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 |
20100331324 | FUSED 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 |
20100331325 | NOVEL 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-HT | 12-30-2010 |
20110003805 | CONCOMITANT 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 |
20110034455 | INHIBITORS 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 |
20110053928 | PYRIMIDOTHIENOINDAZOLES - 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 |
20110065698 | NOVEL 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 |
20110105492 | ARYL 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 |
20110105493 | HETEROCYCLYL 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 |
20110105494 | HETEROARYL 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 |
20110112086 | PYRIDINONE 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 |
20110112087 | Thia-triaza-cyclopentazulenes - The present invention encompasses compounds of general formula (1) | 05-12-2011 |
20110112088 | PYRAZOLES FOR THE TREATMENT OF OBESITY AND OTHER CNS DISORDERS - This invention relates to compounds of the formula: | 05-12-2011 |
20110124639 | 3 BETA-HYDROXYSTEROID DEHYDROGENASE INHIBITORS - The present invention relates to methods of treating a patient infected by | 05-26-2011 |
20110136800 | ARYL-AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE - The present invention relates to compounds defined by formula I | 06-09-2011 |
20110136801 | Novel Compounds - The present invention provides compounds of formula (I): | 06-09-2011 |
20110136802 | SHIP1 MODULATORS AND METHODS RELATED THERETO - Compounds of structure (I): | 06-09-2011 |
20110144099 | ARYLOXY 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 |
20110160201 | COMPOUND 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 |
20110160202 | PYRAZINE 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 |
20110172224 | NOVEL 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 |
20110172225 | ANTIFUNGAL 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 |
20110172226 | NOVEL HYDRAZIDE CONTAINING TAXANE CONJUGATES - The present invention relates to compounds of formula I or salts thereof, wherein, R | 07-14-2011 |
20110190288 | DIHYDROPYRIDOPHTHALAZINONE 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 |
20110207727 | Thio-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 |
20110237581 | DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) and Formula (II): | 09-29-2011 |
20110269753 | HETEROCYCLIC 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 |
20110281862 | ALFA-CARBOLINE INHIBITORS OF NPM-ALK, RET, AND BCR-ABL - The present invention relates to compounds of formula (I) | 11-17-2011 |
20110294799 | Organic Compounds - The invention relates to compound of the formula I | 12-01-2011 |
20110312956 | ARYLINDENOPYRIMIDINES WITH REDUCED hERG CHANNEL BINDING - This invention provides novel arylindenopyrimidines of the Formula (I), | 12-22-2011 |
20120022060 | Tricyclic 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 |
20120022061 | BENZO [C] PHENANTHRIDINES AS ANTIMICROBIAL AGENTS - The present invention provides compounds of formula I: formula (I) wherein X | 01-26-2012 |
20120035170 | NOVEL UNSATURATED TETRACYCLIC TETRAHYDROFURAN DERIVATIVES - This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT | 02-09-2012 |
20120040978 | Heterocyclic 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 |
20120065199 | SUBSTITUTED QUINOLINES FOR USE AS VEGF INHIBITORS - A compound of formula (I) | 03-15-2012 |
20120071472 | RIMINOPHENAZINES 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 |
20120071473 | TRICYCLIC COMPOUND DERIVATIVES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY DISORDERS AND IMMUNOMODULATORY DISORDERS - Provided are compounds of the formula (I): | 03-22-2012 |
20120101091 | VIRAL POLYMERASE INHIBITORS - The present application provides compounds of formula I wherein X, Y, R | 04-26-2012 |
20120101092 | SMALL 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 |
20120108583 | Tricyclic 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 |
20120108584 | 2H OR 3H-BENZO[E]INDAZOL-1-YL CARBAMATE DERIVATIVES, THE PREPARATION AND THERAPEUTIC USE THEREOF - Compounds corresponding to the formula (I) | 05-03-2012 |
20120115862 | DIBENZOCYCLOHEPTATONE DERIVATIVES AND PHARMACEUTICAL AGENTS CONTAINING SAID COMPOUNDS - The present invention relates to compounds of the formula I | 05-10-2012 |
20120129849 | DEUTERATED 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 |
20120190678 | SUBSTITUTED 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 |
20120196854 | PHARMACEUTICAL 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 |
20120208809 | 9H-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 |
20120232074 | Imidazo [4, 5-C] Quinoline Derivatives As Bromodomain Inhibitors - Novel compounds of formula (I) | 09-13-2012 |
20120238563 | NOVEL UNSATURATED TETRACYCLIC TETRAHYDROFURAN DERIVATIVES - This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT | 09-20-2012 |
20120295903 | FLAVIN 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 |
20120302562 | 4H-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 |
20120302563 | SUBSTITUTED 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 |
20120322797 | SELECTIVE 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 |
20130012505 | BENZONAPHTHYRIDINAMINES 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 |
20130029980 | FLAVIN DERIVATIVES - The present invention relates novel flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives. | 01-31-2013 |
20130045974 | NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS - Compounds of the formula Ia***** | 02-21-2013 |
20130059843 | Thiazolyl- 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 |
20130085140 | INDENOISOQUINOLINONE 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 |
20130096112 | FURO[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 |
20130102597 | COMPOUNDS 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 |
20130102598 | INDENOQUINOLONE 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 |
20130102599 | PYRAZOLO [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 |
20130109686 | ISOINDOLONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS | 05-02-2013 |
20130116248 | SUBSTITUTED IMIDAZOQUINOLINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to substituted imidazo[4,5-c]quinoline derivatives, the compounds of formula (I), wherein R | 05-09-2013 |
20130143877 | COMPOSITION COMPRISING TETRACYCLIC COMPOUND - A composition which comprises substance represented by Formula (I), | 06-06-2013 |
20130143878 | SUBSTITUTED 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 |
20130150359 | PYRAZOLOQUINOLINES - 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 salts | 06-13-2013 |
20130158024 | TRICYCLIC 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 |
20130172336 | 4-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 |
20130172337 | Imidazo[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 |
20130178470 | HETEROCYCLIC 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 |
20130184271 | Methods 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 |
20130184272 | DIABETES 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 |
20130190305 | NEW 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 |
20130190306 | DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) and Formula (II): | 07-25-2013 |
20130190307 | FUSED HETEROARYLS AND THEIR USES - Provided are certain fused heteroaryls, compositions thereof and methods of use therefor. | 07-25-2013 |
20130274255 | HETEROCYCLIC PYRAZOLE COMPOUNDS, METHOD FOR PREPARING THE SAME AND USE THEREOF - The present invention relates to a compound of formula (I): | 10-17-2013 |
20130274256 | NOVEL INHIBITORS OF BACTERIAL BIOFILMS AND RELATED METHODS - Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms. | 10-17-2013 |
20130274257 | SUBSTITUTED HETEROCYCLES AS JANUS KINASE INHIBITORS - The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 10-17-2013 |
20130274258 | CARBAZOLE AND CARBOLINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC APPLICATIONS THEREOF - Compounds of general formula (I), wherein A, Y, R | 10-17-2013 |
20130289030 | NOVEL PHENAZINE DERIVATIVES AND THEIR USES - The present invention is directed to novel compounds of formula I | 10-31-2013 |
20130310374 | Substituted Imidazoquinoline Derivatives - The present invention relates to substituted imidazo[4,5-c]quinoline derivatives of formula (I), wherein R | 11-21-2013 |
20130317018 | Methods and Compositions for Unsilencing Imprinted Genes - The present invention provides methods and compositions for inducing expression of Ube3a in a cell by contacting the cell with a topoisomerase inhibitor. Particular embodiments include a method of treating a genomic imprinting disorder, such as Angelman syndrome, in a subject by administering to the subject an effective amount of a topoisomerase inhibitor. | 11-28-2013 |
20130345214 | Lipoxygenase Inhibitors - The disclosure provides bisindole suitable for inhibiting lipoxygenases or Aβ-formation, and treating associated diseases, such as Alzheimer's disease. The bisindoles are indolo[2,3-b]carbazole derivatives, and may be administered to a patient as part of a pharmaceutical formulation. | 12-26-2013 |
20140018360 | AZAINDENOISOQUINOLINE TOPOISOMERASE I INHIBITORS - The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer. | 01-16-2014 |
20140045833 | Protein Kinase Inhibitors - The present invention relates to a novel family of inhibitors of protein kinases of Formula (1) wherein X is selected from CH2, O, S(0)n, or NR6; and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src, Btk and Lck protein kinase families. | 02-13-2014 |
20140045834 | 7-(3,5-Dimethyl-4-Isoxazolyl)-8-(Methyloxy)-1H-Imidazo[4,5-C]Quinoline Derivatives - Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy. | 02-13-2014 |
20140051695 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof | 02-20-2014 |
20140073637 | AMINO-SUBSTITUTED-ALKYLOXY-BENZO[E]PYRIDO[4,3-B]INDOLE DERIVATIVES AS NEW POTENT KINASE INHIBITORS - The present invention relates to a new class of benzo[e]pyrido-indole, the amino-substituted-alkyloxy-benzo[e]pyrido[4,3-b]indole derivatives, having a particular kinase inhibition profile and useful as a therapeutic agent, in particular an anti-tumoral agent. | 03-13-2014 |
20140080824 | STRUCTURE-GUIDED IDENTIFICATION OF BINDING INTERACTIONS OF HUMAN LAMININ RECEPTOR PRECURSOR WITH LAMININ AND IDENTIFICATION OF COMPOUNDS THAT AFFECT BINDING - The present invention pertains to compounds which interfere with the binding of laminin to the laminin receptor (LamR). Such compounds are useful for treating diseases such as cancer, Alzheimer's Disease, and certain viral and bacterial infections. | 03-20-2014 |
20140148451 | Autophagy Inhibitors - The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors. | 05-29-2014 |
20140187547 | AZAINDENOISOQUINOLINE TOPOISOMERASE I INHIBITORS - The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer. | 07-03-2014 |
20140194417 | IRAK INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 07-10-2014 |
20140243327 | RIMINOPHENAZINES 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 | 08-28-2014 |
20140275064 | DYRK1 INHIBITORS AND USES THEREOF - The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds. | 09-18-2014 |
20140288068 | ALKYL-AMINE HARMINE DERIVATIVES FOR PROMOTING BONE GROWTH - In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III. | 09-25-2014 |
20140336188 | N-SUBSTITUTED INDENOISOQUINOLINES AND SYNTHESES THEREOF - N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof. | 11-13-2014 |
20140343051 | METHODS TO MODULATE ACUTE MYELOID LEUKEMIA STEM/PROGENITOR CELL EXPANSION AND/OR DIFFERENTIATION - Novel methods for modulating acute myeloid leukemia stem/progenitor cell expansion and/or differentiation are disclosed. These methods are based on the use of aryl hydrocarbon receptor (AhR) modulators and/or compounds of formula I or II | 11-20-2014 |
20140343052 | Phenylxanthene Derivatives - The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. | 11-20-2014 |
20140350007 | CRYSTALLINE FORMS OF TRICYCLIC COMPOUND ACID SALT OR HYDRATE THEREOF, AND METHOD FOR MAKING THEREOF - The present invention relates to a novel crystalline acid salt of a tricyclic derivative or a hydrate thereof and a production method thereof. The crystalline acid salt or the hydrate thereof according to the present invention is stable with respect to humidity and stable with respect to hygroscopicity, and the quality control during manufacturing drugs is favorable. In addition, the crystalline acid salt or the hydrate thereof may be used in a pharmaceutical composition for preventing or treating neuropathic pain, epilepsy, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), Huntington's disease, schizophrenia, chronic and acute pain, ischemic brain injury, neuronal loss after hypoxia, trauma and nerve damage, which are medical conditions induced by PARP overactivity. | 11-27-2014 |
20150011542 | Methods of Treating Adverse Intestinal Effects of Non-Steroidal Anti-Inflammatory Drugs - Methods of treating adverse intestinal effects of a non-steroidal anti-inflammatory drugs (NSAID) in a subject by administering to the subject a therapeutically effective amount of a selective bacterial beta-glucuronidase inhibitor. The adverse intestinal effects to be treated include the formation or growth of an intestinal ulcer, increased intestinal permeability, the loss of intestinal villi, bleeding of the intestinal mucosa, and an increased intestinal inflammatory response. The methods are useful for treating the adverse effects of any NSAID such as propionic acid derivatives, carboxylic acid derivatives, enolic acid derivatives, fenamic acid derivatives, sulphonanilidies, and selective COX-2 inhibitors. The bacterial beta-glucuronidase inhibitors are selective for the inhibition of bacterial beta-glucuronidase enzymes and do not inhibit mammalian beta-glucuronidase. | 01-08-2015 |
20150011543 | PYRIMIDO[4,5-B]INDOLE DERIVATIVES AND USE THEREOF IN THE EXPANSION OF HEMATOPOIETIC STEM CELLS - Pyrimido[4,5-b]indole derivatives are provided. These compounds are useful to expand hematopoietic stem cell populations, particularly, human hematopoietic stem cell populations. The compounds are also useful in the medical treatment of diseases that involve hematopoietic stem cells. | 01-08-2015 |
20150031692 | SUBSTITUTED PYRANO AND FURANOQUINOLINES, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments. | 01-29-2015 |
20150045356 | PIPERAZINE-SUBSTITUTED BENZOTHIOPHENE DERIVATIVES AS ANTIPSYCHOTIC AGENTS - Provided is a superior, novel heterocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes less side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof. | 02-12-2015 |
20150045357 | SMALL MOLECULE INHIBITORS OF MCL-1 AND USES THEREOF - This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a [(1-Piperazinyl)-4-pyridinylmethyl]-Naphtho[1,2-b]furan structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases. | 02-12-2015 |
20150051204 | COMPOUNDS FOR TREATMENT OF METABOLIC SYNDROME - Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders. | 02-19-2015 |
20150051205 | SELECTIVE 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-glucuronidase 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 antineoplasatic agents or glucuronidase-substrate agents or compounds. | 02-19-2015 |
20150065498 | N-LINKED LACTAM M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as 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. | 03-05-2015 |
20150065499 | 3-AMINOTHIENO[3,2-c]QUINOLINE DERIVATIVES, METHODS OF PREPARATION AND USES - The present invention relates to compounds according to Formula I: and salts thereof, wherein R | 03-05-2015 |
20150080390 | COMPOSITIONS USEFUL FOR TREATING HERPES SIMPLEX KERATITIS, AND METHODS USING SAME - The present invention relates generally to compositions and methods for treating diseases and disorders caused by herpes simplex virus type 1, including herpes simplex keratitis, in a subject. In certain embodiments, the compositions of the present invention comprise an ATM inhibitor and an anti-herpetic agent. In other embodiments, the compositions comprise a Chk2 inhibitor and an anti-herpetic agent. In yet other embodiments, the compositions comprise a Chk2 inhibitor and an ATM inhibitor, and optionally an anti-herpetic agent. | 03-19-2015 |
20150119388 | NOVEL PRO- AND CODRUG DERIVATIVES FOR NANOPARTICLE DELIVERY OF SELECT ANTICANCER AGENTS FORMED USING RAPIDLY CLEAVABLE PHENOLIC ESTER BRIDGES - An ester of ArOH according to the formula R—X—CO—OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O—CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R—X—CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R—X— is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety. A dispersion of nanoparticles in an aqueous medium includes nanoparticles including an ester of ArOH according to the formula R—X—CO—OAr wherein ArOH is a pharmaceutically active compound in which Ar is a substituted or unsubstituted aryl or heteroaryl radical, and wherein R is as defined above or R—X—CO-0 is as defined above. The ester or dispersion may be used to treat a diagnosed medical condition in a patient. | 04-30-2015 |
20150119389 | NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS - Compounds of the formula Ia***** | 04-30-2015 |
20150133442 | METHODS AND COMPOSITIONS FOR THE INHIBITION OF PIN1 - The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels. | 05-14-2015 |
20150133443 | Thiazolyl- 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. | 05-14-2015 |
20150133444 | MELAMPOMAGNOLIDE B DERIVATIVES - The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans. | 05-14-2015 |
20150133445 | SYNTHESIS AND USE OF DUAL TYROSYL-DNA PHOSPHODIESTERASE I (Tdp1) - TOPOISOMERASE I (Top1) INHIBITORS - The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds. | 05-14-2015 |
20150141418 | TETRAHYDROCARBAZOLES AS ACTIVE AGENTS FOR INHIBITING VEGF PRODUCTION BY TRANSLATIONAL CONTROL - The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production. | 05-21-2015 |
20150299166 | DEUTERATED ALK INHIBITORS - This invention relates to novel ALK inhibitors of Formula I: | 10-22-2015 |
20150307486 | ERGOLINE DERIVATIVES AS DOPAMINE RECEPTOR MODULATORS - The invention provides compounds of formula (I) wherein R | 10-29-2015 |
20150342932 | ANTI-VIRAL COMPOUNDS - Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway. | 12-03-2015 |
20150352098 | SUBSTITUTED PYRANO AND FURANOQUINOLINES, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments. | 12-10-2015 |
20160002256 | IRAK INHIBITORS AND USES THEREOF - The present invention provides thienopyridine compounds, compositions thereof, and methods of using the same. | 01-07-2016 |
20160002257 | IRAK INHIBITORS AND USES THEREOF - The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same. | 01-07-2016 |
20160009729 | NITROGEN-CONTAINING HETEROCYCLIC RING SUBSTITUTED DIHYDROARTEMISININ DERIVATIVES AND USE THEREOF | 01-14-2016 |
20160031883 | 2-SUBSTITUTED IMIDAZO[4,5-D]PHENANTHROLINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER - The present invention provides 2-substituted imidazo[4,5-d]phenanthroline compounds, which are capable of inhibiting proliferation of one or more renal cancer cells, pancreatic cancer cells, prostate cancer cells, colon cancer cells, leukemia cells, brain cancer/tumour cells or non-small cell lung cancer cells. | 02-04-2016 |
20160039842 | OXAZOLO[5,4-C]QUINOLIN-2-ONE COMPOUNDS AS BROMODOMAIN INHIBITORS - The present invention relates to compounds useful as bromodomain inhibitors. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compounds and compositions in the treatment of various diseases and disorders. | 02-11-2016 |
20160068543 | IRAK INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 03-10-2016 |
20160081999 | SYNTHESIS AND USE OF DUAL TYROSYL-DNA PHOSPHODIESTERASE I (Tdp1) - TOPOISOMERASE I (Top1) INHIBITORS - The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds. | 03-24-2016 |
20160083397 | PARTHENOLIDE DERIVATIVES AND THEIR MODULATION OF PROCESSES CONTROLLED BY REGULATED TRANSLATION - The present invention provides parthenolide derivatives. In particular, the present invention provides parthenolide derivatives that modulate processes controlled by regulated mRNA translation and have anticancer activity. | 03-24-2016 |
20160089372 | Compositions Useful for Treating Herpes Simplex Labialis and/or Herpes Esophagitis, and Methods Using Same - The present invention relates generally to compositions and methods for treating diseases and disorders caused by herpes simplex virus type 1, including herpes simplex labialis or herpes esophagitis, in a subject. In certain embodiments, the compositions of the invention comprise an ATM inhibitor and an anti-herpetic agent. In other embodiments, the compositions comprise a Chk2 inhibitor and an anti-herpetic agent. In yet other embodiments, the compositions comprise a Chk2 inhibitor and an ATM inhibitor, and optionally an anti-herpetic agent. | 03-31-2016 |
20160108016 | Novel Cannabinergic Compounds and Uses Thereof - Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS. | 04-21-2016 |
20160115508 | PARTHENOLIDE DERIVATIVES, METHODS FOR THEIR PREPARATION AND THEIR USE AS ANTICANCER AGENTS - Methods are provided for the generation of parthenolide derivatives functionalized at carbon atoms C9 and C14. Natural cytochrome P450 enzymes, and engineered variants of these enzymes, are used to carry out the hydroxylation of these sites in parthenolide. These P450-catalyzed C—H hydroxylation reactions are coupled to chemical interconversion of the enzymatically introduced hydroxyl group to install a broad range of functionalities at these otherwise unreactive sites of the molecule. The methods can also be used to produce bifunctionalized parthenolide derivatives, which in addition to modifications at the level of carbon atom C9 or C14, are also functionalized at the level of carbon atom C13. | 04-28-2016 |
20160122360 | TETRAHYDRO-2H-PYRANO[3,2-C]ISOCHROMENE-6-ONES AND ANALOGS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - The present invention relates to 2,3,4,4a-tetrahydro-3,4,8,10-tetrahydroxy-2-(hydroxymethyl)-9-methoxypyrano[3,2-c]isochromen-6(10bH)-one analogs of the Formula I, wherein, R, R′ and R″ are as herein described. In addition, the invention relates to methods of using compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma and chronic obstructive pulmonary disorder. | 05-05-2016 |
20160168165 | MYC MODULATORS AND USES THEREOF | 06-16-2016 |
20160176839 | DEHYDROLEUCODINE DERIVATIVES AND USES THEREOF | 06-23-2016 |
20160185743 | 15-Oxospiramilactone Derivatives, Preparation Method and Uses Thereof - The invention relates to a derivative of 15-oxospiramilacton, particularly to a compound of Formula I or II, or an isomer, a solvate or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the compound as pharmaceutically active ingredient, a method for preparing the same, and use thereof in manufacture of an anti-tumor agent. The derivative of 15-oxospiramilactone of the invention have an activity against multiple tumor cell lines, and the anti-tumor activity is positively correlated to an activity inhibiting the Wnt signaling pathway. | 06-30-2016 |
20160376243 | 1,2-NAPHTHOQUINONE BASED DERIVATIVE AND METHOD OF PREPARING THE SAME - Disclosed are a compound represented by Formula (1), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, tautomer, enantiomer, or pharmaceutically acceptable diastereomer thereof, a method of preparing the same, and a pharmaceutical composition, which have effects for treatment or prevention of metabolic syndromes, comprising the same:
| 12-29-2016 |
20160376258 | 1,2-NAPHTHOQUINONE BASED DERIVATIVE AND METHOD OF PREPARING THE SAME - Disclosed are a compound represented by Formula (1), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, tautomer, enantiomer, or pharmaceutically acceptable diastereomer thereof, a method of preparing the same, and a pharmaceutical composition, which have effects for treatment or prevention of metabolic syndromes, comprising the same: | 12-29-2016 |