357263-39-9Relevant articles and documents
ANNELATED PYRIDAZINES FOR THE TREATMENT OF TUMORS DRIVEN BY INAPPROPRIATE HEDGEHOG SIGNALLING
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Page/Page column 69, (2009/04/25)
The present invention relates generally to compounds represented in Formula (I), pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.
PIPERAZINE DERIVATIVES
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Page/Page column 30, (2008/06/13)
The present invention relates to a crystalline form of 5-{(1S)-2-[(2R)-4-benzoyl-2-methyl-piperazin-1-yl]-1-methyl-2-oxo-ethoxy}-4-methoxy-pyridine-2-carboxylic acid methylamide, processes for the preparation thereof, compositions containing the crystalli
Discovery of 4-benzoyl-1-[(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2-(R) -methylpiperazine (BMS-378806): A novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions
Wang, Tao,Zhang, Zhongxing,Wallace, Owen B.,Deshpande, Milind,Fang, Haiquan,Yang, Zheng,Zadjura, Lisa M.,Tweedie, Donald L.,Huang, Stella,Zhao, Fang,Ranadive, Sunanda,Robinson, Brett S.,Gong, Yi-Fei,Ricarrdi, Keith,Spicer, Timothy P.,Deminie, Carol,Rose, Ronald,Wang, Hwei-Gene Heidi,Blair, Wade S.,Shi, Pei-Yong,Lin, Pin-Fang,Colonno, Richard J.,Meanwell, Nicholas A.
, p. 4236 - 4239 (2007/10/03)
Indole derivative 1 interferes with the interaction of the HIV surface protein gp120 with the host cell receptor CD4. The 4-fluoro derivative 2 exhibited markedly enhanced potency and was bioavailable in the rat, dog, and cynomolgus monkey when administered orally as a solution formulation. However, aqueous suspensions of 2 were poorly bioavailable, indicative of dissolution-limited absorption. The 7-azaindole derivative 3, BMS-378806, exhibited improved pharmaceutical properties while retaining the HIV-1 inhibitory profile of 2.