Entries |
Document | Title | Date |
20080234294 | Cxcr4 Binding Molecules - This invention relates to the use of a CXCR binding molecules as described in the specification, in WHIM syndrome. | 09-25-2008 |
20080255156 | ADENOSINE A2A RECEPTOR ANTAGONISTS - Compounds having the structural formula I | 10-16-2008 |
20080255157 | 6-Aryl-7-halo-imidazo[1,2-a]pyrimidines as anticancer agents - This invention relates to certain 6-aryl-7-halo-imidazo[1,2-a]pyrimidines or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals by promotion of microtubule polymerization. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. | 10-16-2008 |
20090012102 | Imidazo[1,2-C]Pyrimidinylacetic Acid Derivatives - The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo[1,2-c]pyrimidinylacetic acid derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis. | 01-08-2009 |
20090042912 | DIPHENYLIMIDAZOLYL COMPOUNDS AS INHIBITORS OF beta-SECRETASE - The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid deposits or β-amyloid levels in a patient. | 02-12-2009 |
20090048271 | HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS - Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a heteroaryl five-membered ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed. | 02-19-2009 |
20090156617 | 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. | 06-18-2009 |
20090221612 | CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF - Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 09-03-2009 |
20090253716 | AMINO-IMIDAZOLONES FOR THE INHIBITION OF BETA-SECRETASE - The present invention provides an amino-imidazolone compound of formula I | 10-08-2009 |
20100004269 | 5-ANILINOIMIDAZOPYRIDINES AND METHODS OF USE - The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 01-07-2010 |
20100075993 | SMALL MOLECULE INHIBITORS AGAINST WEST NILE VIRUS REPLICATION - The invention provides flavivirus replication inhibitors of WNV and other flaviviruses, such as, for example, JEV, SLEV, AV, KV, JV, CV, YV, TBEV, DENV-1, DENV-2, DENV-3, DENV-4, YFV and MVEV. The invention further provides pharmaceutical compositions including one or more such flavivirus replication inhibitors. The invention further provides methods of treatment, prevention, inhibition or amelioration of one or more diseases associated with flavivirus replication including administering one or more such inhibitors or pharmaceutical compositions. | 03-25-2010 |
20100152205 | CXCR2 INHIBITORS - The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease. | 06-17-2010 |
20100160344 | NOVEL COMPOUNDS - This invention relates to imidazopyrimidine substituted piperidine derivatives and their use as pharmaceuticals. | 06-24-2010 |
20100160345 | NOVEL COMPOUNDS - This invention relates to imidazopyrazine substituted piperidine derivatives and their use as pharmaceuticals. | 06-24-2010 |
20100168135 | Method of Inducing Cleavage of Amyloid Precursor Protein to Form a Novel Fragment - The present invention provides a method of inducing cleavage of amyloid precursor protein to produce an approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein in a subject, the method comprising administering a heterocyclic compound or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof, wherein the approximately 17 kilodalton fragment includes the carboxyterminal amino acid sequence of amyloid precursor protein and amyloid-beta amino acid sequence. Also provided is a screening method for identifying compounds induce cleavage of amyloid precursor protein to produce the approximately 17 kilodalton carboxy-terminal fragment of amyloid precursor protein. | 07-01-2010 |
20100249151 | IMIDAZO 1, 2-A PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF DISEASES SUCH AS DIABETES - Novel compounds of the formula (I), in which W, T, R | 09-30-2010 |
20100298347 | SUBSTITUTED 2-NAPHTHOIC ACIDS AS ANTAGONISTS OF GPR105 ACTIVITY - Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome. | 11-25-2010 |
20100298348 | Method of Decreasing Ubiquitylated Protein Levels - The present invention provides a method of decreasing the level of ubiquitylated protein in a subject, the method comprising administering a heterocyclic compound disclosed herein or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof. | 11-25-2010 |
20110065728 | LIPOPROTEIN LIPASE-ACTIVATING COMPOSITIONS COMPRISING BENZENE DERIVATIVES - The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: | 03-17-2011 |
20110160226 | Substituted Triazolo-Pyrimidine Compounds - The present invention relates to substituted triazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 06-30-2011 |
20110172250 | ISOTOPICALLY ENRICHED PYRIMIDIN-5-YL ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS - Provided herein are | 07-14-2011 |
20110178106 | 5-QUINOLINONE AND IMIDAZOPYRIDINE COMPOUNDS AND USE THEREOF - 5-Quinolinone and Imidazopyrimidine compounds are provided that are useful for inhibiting the efflux of any therapeutic agent that is a MRP1 substrate. Also provided is a method for screening to identify additional MRP1 inhibitors. | 07-21-2011 |
20110207751 | HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS - Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a thiazole ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed. | 08-25-2011 |
20130065913 | NOVEL COMPOUNDS - Compounds of formula (I): | 03-14-2013 |
20130231354 | SUBSTITUTED AZAINDAZOLE COMPOUNDS - Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds. | 09-05-2013 |
20130296342 | LIPOPROTEIN LIPASE-ACTIVATING COMPOSITIONS COMPRISING BENZENE DERIVATES - The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: | 11-07-2013 |
20140094474 | ANDROGEN RECEPTOR MODULATING CARBOXAMIDES - Compounds of formula (I) or (II) | 04-03-2014 |
20140171452 | METHODS FOR TREATING DEPRESSION, NEURODEGENERATION, INHIBITING AMYLOID BETA DEPOSITION, DELAYING SENESCENCE, AND EXTENDING LIFE SPANS WITH HETEROCYCLIC COMPOUNDS - Disclosed is an antidepressant, neuroprotectant, amyloid β deposition inhibitor, or age retardant composition containing a heterocyclic compound having the general formula (I): | 06-19-2014 |
20140179714 | NOVEL COMPOUNDS - Compounds of formula (I): | 06-26-2014 |
20150126530 | Novel Substituted Imidazopyrimidines as Gpbar1 Receptor Modulators - The present invention relates to novel substituted imidazo[1,2-a]pyrimidine compounds of formula (I), their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further” relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals. (Formula I). | 05-07-2015 |
20160046604 | HETEROARYL SUBSTITUTED INDAZOLES - Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 02-18-2016 |
20160200714 | 3-SUBSTITUTED CYCLOPENTYLAMINE DERIVATIVES | 07-14-2016 |
20180022738 | 3-SUBSTITUTED CYCLOPENTYLAMINE DERIVATIVES | 01-25-2018 |
20190142837 | TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF | 05-16-2019 |