313337-35-8Relevant academic research and scientific papers
Inhibitors of HIV-1 attachment. Part 7: Indole-7-carboxamides as potent and orally bioavailable antiviral agents
Yeung, Kap-Sun,Qiu, Zhilei,Xue, Quifen,Fang, Haiquan,Yang, Zheng,Zadjura, Lisa,D'Arienzo, Celia J.,Eggers, Betsy J.,Riccardi, Keith,Shi, Pei-Yong,Gong, Yi-Fei,Browning, Marc R.,Gao, Qi,Hansel, Steven,Santone, Kenneth,Lin, Ping-Fang,Meanwell, Nicholas A.,Kadow, John F.
, p. 198 - 202 (2013/02/25)
A series of substituted carboxamides at the indole C7 position of the previously described 4-fluoro-substituted indole HIV-1 attachment inhibitor 1 was synthesized and the SAR delineated. Heteroaryl carboxamide inhibitors that exhibited pM potency in the primary cell-based assay against a pseudotype virus expressing a JRFL envelope were identified. The simple methyl amide analog 4 displayed a promising in vitro profile, with its favorable HLM stability and membrane permeability translating into favorable pharmacokinetic properties in preclinical species.
Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives
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Page/Page column 33, (2010/02/05)
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. 1wherein: Z is 2Q is selected from the group consisting of: 3—W— is 4—represents a carbon-carbon bond or does not exist; and A is NR13R14.
INDOLE, AZAINDOLE AND RELATED HETEROCYCLIC UREIDO AND THIOUREIDO PIPERAZINE DERIVATIVES
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Page 73, (2010/02/06)
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with ureido and thioureido piperazine derivatives of Formula (I). These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula (I) are Formula (I) wherein:Y is O or S;Z is Formula (II); Q is selected from the group consisting of Formula (A) and Formula (B); m is 2;A is NRR; and-W- is Formula (C).
Antiviral indoleoxoacetyl piperazine derivatives
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, (2008/06/13)
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
