Entries |
Document | Title | Date |
20080207606 | Novel heterocycles - Novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof are described. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell-damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever. More particularly these compounds are useful as PDE4 inhibitors, and useful for treating PDE4 mediated diseases. | 08-28-2008 |
20080221088 | 3,4-Substituted Thiazoles as Ampk Activators - The present application provides novel thiazole derivatives that are useful as activators of Adenosine 5′-Monophosphate-Activated Protein Kinase and pharmaceutical compositions containing such compounds. | 09-11-2008 |
20080221089 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful. | 09-11-2008 |
20080249084 | Triazole Compounds and Uses Related Thereto - The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound is useful as a therapeutic drug for the treatment of diabetes, obesity or metabolic syndrome. | 10-09-2008 |
20080255105 | Biphenyl Derivatives and Their Use in Treating Hepatitis C - A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R | 10-16-2008 |
20080261961 | KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof. | 10-23-2008 |
20080269207 | 3,4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASE AND GLYCOGEN SYNTHASE KINASE-3 MODULATORS - The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. | 10-30-2008 |
20080280889 | Inhibitors of Akt Activity - The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration (if the compounds of the invention. | 11-13-2008 |
20080280890 | HYDROXYLAMINE COMPOUNDS AND METHODS OF THEIR USE - The present disclosure provides compounds that include hydroxylamines of formula I or II, pharmaceutical compositions, and methods for their use. The methods utilize hydroxylamine compounds and/or their pharmaceutical compositions for the treatment of angiogenesis, hepatitis, complement-mediated pathologies, drusen-mediated pathologies, macular degeneration and certain other ophthalmic conditions, inflammation, arthritis, and related diseases and for the inhibition of complement activation. | 11-13-2008 |
20080287424 | AZOLYLACYLGUANIDINES AS beta-SECRETASE INHIBITORS - The present invention provides an azolylacylquanidine compound of formula I | 11-20-2008 |
20080293704 | FACTOR Xa INHIBITORS - The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 11-27-2008 |
20080293705 | A1 ADENOSINE RECEPTOR ANTAGONISTS - Compounds of the general formula (I) are described: | 11-27-2008 |
20080306055 | Heterocyclic Mchr1 Antagonists And Their Use In Therapy - Compounds of formula I depicted below, pharmaceutical compositions containing them, processes for preparing the compounds, and their use in the treatment of obesity, type II diabetes, metabolic syndrome, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy and related conditions, neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease, and pain related disorders. The compounds are melanin concentrating hormone receptor 1 (MCHr1) antagonists. | 12-11-2008 |
20080306056 | PYRAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS - The present invention is directed to a compound of formula I, | 12-11-2008 |
20080312220 | Oxadiazole Derivatives with Crth2 Receptor Activity - Compounds of formula are CRTH2 ligands, useful for treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein R | 12-18-2008 |
20090005369 | Oxazolidinone Compounds and Compositions and Methods Related Thereto - The invention provides new oxazolidinones of formula (I), where R1, R2, R3 and R4 are independently selected from H, F and Cl; A is certain heterocycles optionally substituted; X is selected from O, S, NR8 and CR8R9; R8 and R9 having different meanings; Y is selected from O, S, SO, SO2, NO, NR11 and CR11R12; R11 and R12 having different meanings; and n is selected from 0 and 1. It also provides different processes for the preparation of such compounds. Oxazolidinones compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections. | 01-01-2009 |
20090005370 | ISOXAZOLE-IMIDAZOLE DERIVATIVES - The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A α5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use for enhancing cognition or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I | 01-01-2009 |
20090018122 | Aryloxy and Arylalkyleneoxy Substituted Imidazoquinolines - Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy or hydroxy 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. | 01-15-2009 |
20090018123 | Oxazolidinones Bearing Antimicrobial Activity Composition and Methods of Preparation - The present invention concerns recombinant DNA's comprising cDNA of genomic RNA of a Salmonidae alphavirus preceded by a spacer sequence, under the control of a suitable promoter. Said recombinant DNA's are useful for obtaining expression vectors, producing recombinant Salmonidae alphavirus, and for obtaining vaccines. | 01-15-2009 |
20090036434 | Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto - The present invention relates to certain substituted aryl and heteroaryl derivative of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. | 02-05-2009 |
20090036435 | Pharmaceutical Compounds - The invention provides a combination of an ancillary agent and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein the ancillary agent is selected from: a monoclonal antibody, an alkylating agent, an anticancer agent, a further CDK inhibitor and a hormone, hormone agonist, hormone antagonist or hormone modulating agent; X is a group R | 02-05-2009 |
20090036436 | 3-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS HAVING ANALGESIC AND/OR IMMUNO STIMULANT ACTIVITY - Compounds of Formulas 1 and 2 | 02-05-2009 |
20090054420 | BICYCLIC-SUBSTITUTED AMINES AS HISTAMINE-3 RECEPTOR LIGANDS - Compounds of formula (I) | 02-26-2009 |
20090069310 | Anti-inflammatory medicaments - Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds. | 03-12-2009 |
20090069311 | 5-AMINOINDOLE DERIVATIVES AS H3 INVERSE AGONISTS - The present invention relates to compounds of formula I | 03-12-2009 |
20090075986 | Anti-inflammatory medicaments - Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds. | 03-19-2009 |
20090093471 | Methods of Treating Nervous Disorders - The invention relates to compositions and methods for treating nervous disorders. More particularly, the invention relates to methods of treating amyloÊd beta peptide-related disorders, particularly Alzheimer's disease, using Rac1 inhibitors. The invention may be used in mammalian subjects, particularly human subjects, at various stages of the disease, including disease onset. The invention also provides methods of producing, identifying, selecting or optimising compounds for use in the treatment of amyloÊd beta peptide-related disorders, based on a determination of the ability of a test compound to inhibit Rac 1. | 04-09-2009 |
20090099160 | 4-(4-(Imidazol-4-Yl) Pyrimidin-2-Ylamino) Benzamides as CDK Inhibitors - Compounds of the formula (I): | 04-16-2009 |
20090105230 | Anti-inflammatory medicaments - Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds. | 04-23-2009 |
20090105231 | AMIDE DERIVATIVES AS ROCK INHIBITORS - This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease. | 04-23-2009 |
20090105232 | CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES - The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) | 04-23-2009 |
20090137572 | 2-substituted-4-heteroaryl-pyrimidines useful for the treatment of proliferative disorders - The present invention relates to selected substituted pyrimidines their preparation, pharmaceutical compositions containing them and their use as inhibitors of one or more protein kinases, and hence their use in the treatment of proliferative disorders, viral disorders and/or other disorders. | 05-28-2009 |
20090137573 | 1,3-Disubstituted 4-methyl-1H-pyrrole-2-carboxamides and their Use in Medicaments - 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I | 05-28-2009 |
20090137574 | Combination Therapy Using an 11Beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitor and an Antihypertensive Agent for the Treatment of Metabolic Syndrome and Related Diseases and Disorders - Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders. | 05-28-2009 |
20090143371 | ISOXAZOLE-PYRIDINE DERIVATIVES - The present invention is concerned with isoxazole-pyridine derivatives of formula I | 06-04-2009 |
20090163482 | TETRALINES ANTAGONISTS OF THE H-3 RECEPTOR - This invention is directed to a compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of formula (I) a process of en preparation of a compound of formula (I), a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above. | 06-25-2009 |
20090170838 | Bicycloheteroaryl compounds as P2X7 modulators and uses thereof - Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: | 07-02-2009 |
20090197875 | ARYL-ISOXAZOLO-4-YL-OXADIAZOLE DERIVATIVES - The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula | 08-06-2009 |
20090215758 | Use of 2,5-Disubstituted Thiazol-4-One Derivatives in Drugs - The invention relates to 2,5-disubstituted thiazol-4-one derivatives and to their use in the production of drugs, to methods for producing them and to drugs containing said compounds. | 08-27-2009 |
20090215759 | MODULATORS FOR AMYLOID BETA - The invention relates to compounds of formula | 08-27-2009 |
20090221564 | Heterocyclic Compounds and Their Use in the Treatment of Cardiovascular Disease - Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R | 09-03-2009 |
20090253688 | Semicarbazide derivatives as kinase inhibitors - The present invention relates to semicarbazide derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. | 10-08-2009 |
20090264422 | METHOD OF TREATING DISEASE STATES USING SUBSTITUTED PYRAZOLE COMPOUNDS - Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer. | 10-22-2009 |
20090275567 | 2-HETEROCYCLOAMINO-4-IMIDAZOLYLPYRIMIDINES AS AGENTS FOR THE INHIBITION OF CELL PROLIFERATION - Compounds of formula (I): | 11-05-2009 |
20090281094 | Derivatives of 1--4-methylpiperazine, synthesis process and uses thereof - The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds. | 11-12-2009 |
20090281095 | THIOMORPHOLINE COMPOUND AND PROCESS FOR PREPARING THE SAME - The present invention discloses a thiomorpholine compound represented by the formula [I]: | 11-12-2009 |
20090298815 | Benzene Sulfonamide Thiazole and Oxazole Compounds - The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 12-03-2009 |
20090306059 | CYCLIC AMINE DERIVATIVE HAVING SUBSTITUTED ALKYL GROUP - A compound having the general formula (I), pharmacologically acceptable salts thereof or prodrugs thereof: | 12-10-2009 |
20090318430 | MEDICAL USE OF CYCLIN DEPENDENT KINASES INHIBITORS - The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (0): | 12-24-2009 |
20100029625 | Therapeutic Agent for Restenosis - A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: | 02-04-2010 |
20100029626 | Cyclic sulfones useful as mitochondrial sodium-calcium exchangers - The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases. | 02-04-2010 |
20100048543 | PYRIMIDINE COMPOUNDS HAVING TIES (TEK) INHIBITORY ACTIVITY - The invention relates to a compound of the Formula I | 02-25-2010 |
20100087425 | Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors - This invention discloses novel gamma secretase inhibitors of the formula: | 04-08-2010 |
20100099667 | BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 04-22-2010 |
20100113434 | CARBAMATE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis. | 05-06-2010 |
20100113435 | INHIBITORS OF 11-BETA-HYDROXY STERIOD DEHYDROGENASE TYPE 1 - The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme. | 05-06-2010 |
20100120757 | PYRAZOLONE DERIVATIVES AS PDE4 INHIBITORS - The compounds of a certain formula 1, | 05-13-2010 |
20100130485 | Cyclopropyl Amines as Modulators of the Histamine H3 Receptor - Certain cyclopropyl amines are histamine H | 05-27-2010 |
20100144721 | INHIBITORS OF C-MET AND USES THEREOF - The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 06-10-2010 |
20100144722 | NOVEL HETEROCYCLIC COMPOUNDS AS GATA MODULATORS - Novel heterocyclic compounds, sstereoisomers thereof and/or pharmaceutically acceptable salts of formula (I) and its stereoisomers are provided. Additionally, methods of forming novel heterocyclic compounds, stereoisomers thereof and/or pharmaceutically acceptable salts of formula (I) and its stereoisomers are provided. | 06-10-2010 |
20100144723 | 1-(BIPHENYL-4-YLMETHYL)IMIDAZOLIDINE-2,4-DIONE - The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I | 06-10-2010 |
20100144724 | 1-(4-(PYRIDIN-2-YL)BENZYL)IMIDAZOLIDINE-2,4-DIONE DERIVATIVES - The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I | 06-10-2010 |
20100160301 | MICROANGIOPATHY TREATMENT AND PREVENTION - The present invention relates to the use of selective factor Xa inhibitors, in particular of oxazolidinones of the formula (I) | 06-24-2010 |
20100160302 | NOVEL DIPEPTIDYL PEPTIDASE IV INHIBITORS AND PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined. The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia. | 06-24-2010 |
20100168088 | PYRROLIDINE DERIVATIVES AS NK-3 RECEPTOR ANTAGONISTS - The present invention relates to a compound of formula I | 07-01-2010 |
20100168089 | UTILIZATION OF TACE INHIBITORS FOR THE TREATMENT OF ACNE - An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne. | 07-01-2010 |
20100173899 | DIPEPTIDE ANALOGS AS COAGULATION FACTOR INHIBITORS - Disclosed are novel dipeptide analogs compounds of Formula (I), (II) or (III): | 07-08-2010 |
20100179137 | PYRIDONE COMPOUND - [Solving Means] The present inventors have conducted extensive studies on an EP4 receptor agonist, and as a result, found that a novel pyridone compound characterized in that the 1-position in the pyridone ring is substituted with a group having an acidic group such as a carboxyl group and the 6-position is bonded with an aromatic ring group via lower alkyl, lower alkylene, ether, or thioether, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action and a blood flow increasing action in the hindlimb of a rat, it is useful as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease. | 07-15-2010 |
20100179138 | Isozazole Compounds As Inhibitors Of Heat Shock Proteins - Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: | 07-15-2010 |
20100184753 | Ion Channel Modulators and Methods of Uses - In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels. | 07-22-2010 |
20100190779 | VIRAL POLYMERASE INHIBITORS - Compounds of formula I: | 07-29-2010 |
20100190780 | SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved. | 07-29-2010 |
20100190781 | SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved. | 07-29-2010 |
20100197671 | PHENYL AMINO PYRIMIDINE COMPOUNDS AND USES THEREOF - The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. | 08-05-2010 |
20100197672 | PYRROLE COMPOUNDS AS INHIBITORS OF MYCOBACTERIA, SYNTHESIS THEREOF AND INTERMEDIATES THERETO - The present invention relates to a compound having the general formula (3): synthesis, intermediates and uses thereof. | 08-05-2010 |
20100210633 | CARBOXAMIDE COMPOUNDS AND THEIR USE - Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein. | 08-19-2010 |
20100227855 | HELIX 12 DIRECTED NON-STEROIDAL ANTIANDROGENS - Compounds having the structure (or their salts): | 09-09-2010 |
20100234365 | COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1). | 09-16-2010 |
20100249117 | FACTOR XA INHIBITORS - The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 09-30-2010 |
20100261715 | CARBAMATE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis. | 10-14-2010 |
20100267706 | Compounds, Compositions and Methods Comprising Pyridazine Derivatives - The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1 or 2 or encompassed by formulas I, Ia, II, III, and IV) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 10-21-2010 |
20100280019 | ISOXAZOLES - The present invention is concerned with novel isoxazole derivatives of formula I | 11-04-2010 |
20100280020 | ISOXAZOLES - The present invention is concerned with novel isoxazole derivatives of formula I | 11-04-2010 |
20100286131 | VIRAL POLYMERASE INHIBITORS - Compounds of formula I: | 11-11-2010 |
20100286132 | PYRIDINES - The present invention is concerned with isoxazole-pyridines of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as pharmaceuticals. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease. | 11-11-2010 |
20100305111 | SUBSTITUTED PIPERIDINES - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular diseases and tumour diseases. | 12-02-2010 |
20100324032 | COMPOUNDS AND USES THEREOF IN MODULATING AMYLOID BETA - Novel compounds, compositions, and kits are provided. Methods of modulating Aβ levels, and methods of treating a disease associated with aberrant Aβ levels are also provided. | 12-23-2010 |
20110003799 | 3,4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASE AND GLYCOGEN SYNTHASE KINASE-3 MODULATORS - The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. | 01-06-2011 |
20110034449 | N-SUBSTITUTED HYDROXYPYRIMIDINONE CARBOXAMIDE INHIBITORS OF HIV INTEGRASE - N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: | 02-10-2011 |
20110046121 | INHIBITORS OF FOCAL ADHESION KINASE - The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions. | 02-24-2011 |
20110082134 | 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia - The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Formula (Ia) that are modulators of metabolism. | 04-07-2011 |
20110098285 | BICYCLIC-SUBSTITUTED AMINES AS HISTAMINE-3 RECEPTOR LIGANDS - Compounds of formula (I) | 04-28-2011 |
20110105483 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperprolif erative disorders, such as cancer, in a subject in need thereof. | 05-05-2011 |
20110105484 | FILAMIN A-BINDING ANTI-INFLAMMATORY ANALGESIC - A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within. | 05-05-2011 |
20110105485 | Alpha-(N-Sulfonamido)Acetamide Derivatives as Beta-Amyloid Inhibitors - There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) | 05-05-2011 |
20110105486 | THIAZOLE DERIVATIVES - Wherein n is an integer of from 0 to 3; R | 05-05-2011 |
20110112080 | OXAZOLINE DERIVATIVES - The invention relates to compounds of formula I | 05-12-2011 |
20110112081 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 05-12-2011 |
20110130393 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 06-02-2011 |
20110136796 | IDO Inhibitors - Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R | 06-09-2011 |
20110136797 | CYCLOPROPYL AMINES AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain cyclopropyl amines are histamine H | 06-09-2011 |
20110160196 | FACTOR XA INHIBITORS - The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 06-30-2011 |
20110166129 | 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. | 07-07-2011 |
20110172215 | Benzene Sulfonamide Thiazole And Oxazole Compounds - The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 07-14-2011 |
20110178074 | ANTIPATHOGENIC BENZAMIDE COMPOUNDS - The present invention is related to methods of treating bacterial infections in mammals using antipathogenic benzamide compounds having the formula | 07-21-2011 |
20110190280 | Thiazole And Oxazole Kinase Inhibitors - The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 08-04-2011 |
20110201602 | PROTEIN KINASE MODULATORS AND METHOD OF USE - The present invention relates to chemical compounds having a general formula I | 08-18-2011 |
20110201603 | Novel Acylaminobenzamide Derivatives - The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an aromatic ring group of Q1 to Q7 described in the detailed description, G | 08-18-2011 |
20110237573 | N- (HETERO)ARYL, 2- (HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS - The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A | 09-29-2011 |
20110245239 | ORGANIC COMPOUNDS - Novel isoxazoline compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for use on non-human animals. | 10-06-2011 |
20110251187 | HETEROCYCLIC COMPOUND - The present invention relates to a compound represented by | 10-13-2011 |
20110288080 | Nitrofuran Compounds for the Treatment of Cancer and Angiogenesis - The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds. | 11-24-2011 |
20110288081 | PYRIMIDINE COMPOUNDS AND USES THEREOF - This invention features pyrimidine compounds of formula (I): | 11-24-2011 |
20110306606 | NOVEL 2,6-SUBSTITUTED-3-NITROPYRIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME - The present invention relates to a novel 2,6-substituted-3-nitropyridine derivative compound, a method for preparing the same, and a pharmaceutical composition including the same for prevention and treatment of osteoporosis. The 2,6-substituted-3-nitropyridine derivative compound of the present invention increases osteoblast activity and effectively inhibits the differentiation of osteoclasts, and thus can be usefully used for the prevention and treatment of osteoporosis. | 12-15-2011 |
20110319400 | PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN - Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: | 12-29-2011 |
20120004216 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 01-05-2012 |
20120004217 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - A compound of formula: | 01-05-2012 |
20120010200 | Biaryl Heterocyclic Compounds And Methods Of Making And Using The Same - The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents. | 01-12-2012 |
20120022052 | SMALL MOLECULE INHIBITORS OF KYNURENINE-3-MONOOXYGENASE - The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof. | 01-26-2012 |
20120028970 | HETEROARYLTHIOMETHYL PYRIDINE DERIVATIVE - The present invention relates to a compound represented by a formula (I): wherein X is a group represented by or the like; Y is a group represented by or the like; and Ar | 02-02-2012 |
20120046280 | NOVEL HETEROPYRROLE ANALOGS ACTING ON CANNABINOID RECEPTORS - Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed. | 02-23-2012 |
20120065196 | AMIDE COMPOUNDS - The present invention provides compounds represented by the formula (Ie): | 03-15-2012 |
20120077806 | Deubiquitinase Inhibitors and Methods for Use of the Same - Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds. | 03-29-2012 |
20120083489 | BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISTS - The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes. | 04-05-2012 |
20120094986 | ANTICANCER DERIVIATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - The invention relates to nicotinamide derivatives which can be used as anticancer drugs. | 04-19-2012 |
20120122857 | HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases. | 05-17-2012 |
20120135985 | Substituted piperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular diseases and tumour diseases. | 05-31-2012 |
20120142677 | Pyrrolidine Compounds Which Modulate The CB2 Receptor - Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. (I) | 06-07-2012 |
20120149694 | Substituted piperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders. | 06-14-2012 |
20120149695 | DIHYDROPYRIMIDINE COMPOUNDS AND PREPARATION METHODS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - Disclosed are dihydropyrimidine compounds and preparation methods, pharmaceutical compositions and uses thereof. Specifically, the compounds described herein in general formula (I), or their isomers, pharmaceutically acceptable salts or hydrates are provided, wherein each variable has the meaning as defined in the description. Also provided are a process for preparing the compounds of the general formula (I), the use of the compounds, an isomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof as a medicament, in particular as a medicament for the treatment and/or prevention of Hepatitis B. | 06-14-2012 |
20120149696 | ETHYLENE DIAMINE MODULATORS OF FATTY ACID HYDROLASE - Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed. | 06-14-2012 |
20120172356 | SERUM BIOMARKERS FOR CHAGAS DISEASE - The present invention provides protein-based biomarkers and biomarker combinations that are useful in qualifying Chagas disease status in a patient. In particular, the biomarkers of this invention are useful to classify a subject sample as infected with Chagas disease or non-infected. The biomarkers can be detected by SELDI mass spectrometry. | 07-05-2012 |
20120184538 | ISOXAZOLO-PYRIDINE DERIVATIVES - The present invention is concerned with isoxazole-pyridine derivatives of formula I | 07-19-2012 |
20120208803 | PYRROLIDINE DERIVATIVES AS NK2 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula I | 08-16-2012 |
20120252796 | COMPOUNDS FOR THE TREATMENT OF DYSLIPIDEMIA AND RELATED DISEASES - The present invention relates to compounds of the general formula (I), | 10-04-2012 |
20120252797 | Isoxazole Compounds As Inhibitors Of Heat Shock Proteins - Isoxazoles of formula (A) or (B) | 10-04-2012 |
20120295896 | OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I) and (IA): | 11-22-2012 |
20120309750 | 5-MEMBERED HETEROCYCLE DERIVATIVES AND MANUFACTURING PROCESS THEREOF - Disclosed are a novel 5-membered heterocycle derivatives of Formula I, a tautomer, pharmaceutically acceptable salt, prodrug thereof and a pharmaceutical use thereof. The 5-membered heterocycle derivatives of Formula I, a tautomer, pharmaceutically acceptable salt, prodrug thereof and compositions containing them are useful for treating a tumor. | 12-06-2012 |
20120322795 | BIARYLAMIDE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 12-20-2012 |
20130005716 | DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS - Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD. | 01-03-2013 |
20130005717 | 3-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS HAVING ANALGESIC AND/OR IMMUNO STIMULANT ACTIVITY - Compounds of Formulas 1 and 2 | 01-03-2013 |
20130018048 | OXAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH - The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease. | 01-17-2013 |
20130023526 | Isoxazolines as Therapeutic Agents - The present invention provides compound of Formula (I) | 01-24-2013 |
20130023527 | 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia - The present invention relates to certain | 01-24-2013 |
20130035331 | THIAZOLE AND OXAZOLE KINASE INHIBITORS - The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors. | 02-07-2013 |
20130109682 | CYCLIC ETHER COMPOUNDS USEFUL AS KINASE INHIBITORS | 05-02-2013 |
20130123246 | MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF USING THE SAME - The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. | 05-16-2013 |
20130131052 | Amelioration Of The Development Of Cataracts And Other Ophthalmic Diseases - Ophthalmically acceptable compositions used in arresting the development of cataracts or macular degeneration comprising a pharmaceutically acceptable carrier or diluent and a compound having the formula: | 05-23-2013 |
20130131053 | ISOXAZOLINE DERIVATIVES AS PESTICIDES - The invention relates to new isoxazoline compounds of formula | 05-23-2013 |
20130158018 | Heteroaryl Nitrile Compounds Useful as Inhibitors of Cathepsin-S - Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same. | 06-20-2013 |
20130158019 | PYRIMIDINE COMPOUNDS THAT INHIBIT ANAPLASTIC LYMPHOMA KINASE - Compounds of Formula I are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula I have the following structure: | 06-20-2013 |
20130165431 | INHIBITORS OF SYK AND JAK PROTEIN KINASES - The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 06-27-2013 |
20130172329 | NOVEL SOLID FORMS - The instant invention relates to novel solid forms of the compound of formula (I) | 07-04-2013 |
20130190302 | MODULATORS OF AMYLOID BETA - The invention relates to compounds of formula | 07-25-2013 |
20130210814 | Cycloalkyl Substituted Pyrimidinediamine Compounds And Their Uses - The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers. | 08-15-2013 |
20130252948 | Substituted piperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular diseases and tumour diseases. | 09-26-2013 |
20130267509 | THIAZOLE DERIVATIVES - Method of treating central nervous systems disease by administering | 10-10-2013 |
20130281443 | INHIBITORS OF FOCAL ADHESION KINASE - The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions. | 10-24-2013 |
20130289025 | PYRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 10-31-2013 |
20130289026 | Isoxazole Compounds As Inhibitors Of Heat Shock Proteins - Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: | 10-31-2013 |
20130296310 | THIAZOLE AND OXAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 11-07-2013 |
20130303526 | Pyridine Compounds and the Uses Thereof - The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R | 11-14-2013 |
20130310373 | PYRIMIDINE COMPOUND | 11-21-2013 |
20130324522 | INSECT ODORANT RECEPTOR ANTAGONISTS - Insect repellent compositions are disclosed which are antagonists of insect odorant receptors. These compositions are useful as insect repellents and confusants. These insect repellent compositions may be suitable for topical application. Also disclosed are methods for interfering with the ability of an insect to detect odors. This is accomplished by exposing an insect to an olfactory-disrupting concentration of a compound. | 12-05-2013 |
20130331382 | Pyridinone and Pyridazinone Derivatives - The present invention provides for compounds of formula (I) | 12-12-2013 |
20130331383 | NITROFURAN COMPOUNDS FOR THE TREATMENT OF CANCER AND ANGIOGENESIS - The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds. | 12-12-2013 |
20130345208 | ION CHANNEL MODULATORS AND METHODS OF USE - In general, the invention relates to novel 4-phenylpyrimidine compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels for the treatment of pain. | 12-26-2013 |
20140005180 | PHENYL AMINO PYRIMIDINE COMPOUNDS AND USES THEREOF | 01-02-2014 |
20140005181 | SMALL MOLECULE ANTAGONISTS OF THE APELIN RECEPTOR FOR THE TREATMENT OF DISEASE | 01-02-2014 |
20140031347 | 1,2,4-OXADIAZOLE DERIVATIVES AS DRUGS MODULATING THE GLP-1 PEPTIDE RECEPTOR - The present invention relates to the use of a compound of formula (I): | 01-30-2014 |
20140073634 | HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE - The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases. | 03-13-2014 |
20140094456 | ANTI-FIBROTIC PYRIDINONES - Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders. | 04-03-2014 |
20140107110 | ANTI-FIBROTIC PYRIDINONES - Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders. | 04-17-2014 |
20140107111 | USE OF SIGMA LIGANDS IN DIABETES TYPE-2 ASSOCIATED PAIN - The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms. | 04-17-2014 |
20140148448 | INHIBITORS OF C-FMS KINASE - The invention is directed to compounds of Formula I: | 05-29-2014 |
20140155391 | 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS - Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction. | 06-05-2014 |
20140221361 | C-19 MODIFIED TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY - Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: | 08-07-2014 |
20140275049 | SUBSTITUTED PYRAZOLE ANALOGS As RAR ANTAGONISTS - The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds. | 09-18-2014 |
20140275050 | 2,5-DISUBSTITUTED THIOMORPHOLINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 2,5-disubstituted thiomorpholine amide compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2,5-disubstituted thiomorpholine amide compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 09-18-2014 |
20140329806 | NOVEL SOLID FORMS - The instant invention relates to novel solid forms of the compound of formula (I) | 11-06-2014 |
20140371213 | 3,4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASE AND GLYCOGEN SYNTHASE KINASE-3 MODULATORS - The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. | 12-18-2014 |
20150045353 | FORMULATIONS CONTAINING GAMMA SECRETASE MODULATORS, METHODS FOR PREPARATION AND DELIVERY THEREOF - In accordance with the present invention, there are provided formulations of gamma secretase modulators (GSMs) which are suitable for oral delivery and have improved transport properties relative to prior art formulations thereof. Also provided are methods for the preparation of such improved formulations and uses thereof for the delivery of GSMs to subjects in need thereof. | 02-12-2015 |
20150072976 | SUBSTITUTED BENZAMIDES AND THEIR USES - Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use. | 03-12-2015 |
20150072977 | NITROCATECHOL DERIVATIVES AS COMT INHIBITORS - New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders. | 03-12-2015 |
20150087639 | Nitrogenous Heterocyclic Derivatives And Their Application In Drugs - The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis. | 03-26-2015 |
20150126499 | Triazole Compounds that Modulate HSP90 Activity - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound. | 05-07-2015 |
20150141413 | 5-AMINO[1,4]THIAZINES AS BACE 1 INHIBITORS - The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease. | 05-21-2015 |
20150297596 | ISOXAZOLINES AS THERAPEUTIC AGENTS - The present invention provides compound of Formula (I) | 10-22-2015 |
20160016921 | S-IMINO-S-OXO-IMINOTHIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein R | 01-21-2016 |
20160082014 | N-(HETERO)ARYL, 2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS - The present invention relates to methods for modulating the Wnt signaling pathway using compounds of Formula (1), | 03-24-2016 |
20160145251 | INHIBITORS OF MYOCARDIN-RELATED TRANSCRIPTION FACTOR AND SERUM RESPONSE FACTOR (MRTF/SRF)-MEDIATED GENE TRANSCRIPTION AND METHODS FOR USE OF THE SAME - Disclosed herein are inhibitors of gene transcription mediated by myocardin-related transcription factor and serum response factor, or both myocardin-related transcription factor and serum response factor (“MRTF/SRF”), and methods for their use in treating or preventing cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts thereof: | 05-26-2016 |
20160151380 | THERAPIES FOR DISEASES CAUSED BY ARTHROPOD-BORNE PARASITES | 06-02-2016 |