357262-90-9Relevant articles and documents
TARGETED BIFUNCTIONAL DEGRADERS
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, (2021/04/17)
The present invention provides, in one aspect, bifunctional compounds that can be used to promote or enhance degradation of certain circulating proteins. In another aspect, the present invention provides bifunctional compounds that can be used to promote or enhance degradation of certain autoantibodies. In certain embodiments, treatment or management of a disease and/or disorder requires degradation, removal, or reduction in concentration of the circulating protein or the autoantibody in the subject. Thus, in certain embodiments, administration of a compound of the invention to the subject removes or reduces the circulation concentration of the circulating protein or the autoantibody, thus treating, ameliorating, or preventing the disease and/or disorder. In certain embodiments, the circulating protein is TNF.
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.