86239-00-1Relevant articles and documents
TGR5 AGONISTS
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Page/Page column 163, (2011/06/26)
TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY
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Page/Page column 153, (2012/01/30)
The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprise
BENZENE OR THIOPHENE DERIVATIVE AND USE THEREOF AS VAP-1 INHIBITOR
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Page/Page column 129-130, (2009/12/27)
The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors
Asaki, Tetsuo,Sugiyama, Yukiteru,Hamamoto, Taisuke,Higashioka, Masaya,Umehara, Masato,Naito, Haruna,Niwa, Tomoko
, p. 1421 - 1425 (2007/10/03)
A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against the Bc
NOVEL IMIDAZOLES WITH ANTI-INFLAMMATORY ACTIVITY
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, (2008/06/13)
Compounds of formula I wherein: one of X or Y represents N and the other represents C; R1 represents hydrogen, methyl, halogen, cyano, nitro, -CHO, -COCH3 or -COOR4; R2 represents optionally-substituted aryl or heteroaryl; R3 represents C1-8 alkyl, C1-8 haloalkyl or -NR4R6; R4 represents hydrogen, C1-8 alkyl or arylC0-8 alkyl; R6 represents hydrogen, C1-8 alkyl, arylC1-8 alkyl, -COR8 or -COOR8; R8 represents C1-8 alkyl or C1-8 haloalkyl; aryl in the above definitions represents phenyl or naphthyl; and heteroaryl in the above definitions represents pyridine, pyrazine, pyrimidine or pyridazine, which can be optionally fused to a benzene ring. These compounds are useful as cyclooxygenase-2 inhibitors.
Aromatic Retinoic Acid Analogues. 2. Synthesis and Pharmacological Activity
Dawson, Marcia I.,Chan, Rebecca,Hobbs, Peter D.,Chao, Wan-ru,Schiff, Leonard J.
, p. 1282 - 1293 (2007/10/02)
Aromatic analogues of (E)-1-(4-carboxyphenyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1-yl)butadiene (1b) and its ethyl ester (1a) were synthesized as potential chemopreventive agents for the treatment of epithelial cancer and such skin diseases as psoriasis and cystic acne.The phenyl ring of 1 was replaced by 2-fluorophenyl, 2-methoxyphenyl, thienyl, furanyl, and pyridyl groups.The 1-fluorobutadiene analogue of 1 was also synthesized.With exception for the furanyl analogue, these compounds demonstrated good activity in reversing keratinization in hamster tracheal organ culture and in inhibiting the induction of ornithine decarboxylase in mouse epidermis by a tumor promoter.