- 2,5-Disubstituted pyridines as potent GPR119 agonists
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A series of 2-piperazinyl-5-alkoxypyridines were synthesized and screened against human GPR119 receptor. Through SAR analysis, compounds containing 2-alkylsulfonylpiperazinyl-5-alkoxypyridines were discovered and found to be potent agonists of the human GPR119 receptor.
- Wu, Yulin,Kuntz, Judith D.,Carpenter, Andrew J.,Fang, Jing,Sauls, Howard R.,Gomez, Daniel J.,Ammala, Carina,Xu, Yun,Hart, Shane,Tadepalli, Sarva
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scheme or table
p. 2577 - 2581
(2010/06/19)
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- PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE
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Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. [Insert Formula Ic and Id]
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Page/Page column 142-143
(2008/12/06)
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- NOVEL INHIBITORS OF PROTEIN KINASE
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The present invention relates to novel compounds for inhibition of angiogenesis receptor tyrosine kinases, in particular, VEGF receptor 2 kinase ("KDR") activity, and preparations for preparation of them, and the use of them, and pharmaceutical compositions containing them at a therapeutically effective amount. The compounds according to the present invention are useful for the treatment and prevention of diseases resulting from the undesired KDR activity, for example, angiogenesis-related diseases such as cancers, psoriasis, rheumatoid arthritis, diabetic retinopathy, etc.
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Page/Page column 56
(2010/11/27)
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- CARBAMATE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS
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The invention provides novel benzoimidazolone-carboxamide-derived carbamate 5-HT4 receptor agonist compounds of formula (I): wherein R1, R2, R3, R4, a, and b are defined in the disclosure. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 14
(2008/06/13)
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- 4-AMINOQUINOLINE-3-CARBOXAMIDE DERIVATIVES AS PDE4 INHIBITORS
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Compounds of formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.
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Page/Page column 39
(2010/02/11)
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- THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).
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Page 298-299
(2008/06/13)
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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