CAS: 180683-37-8; (S)-1-((2S,4R)-4-Benzyl-2-Hydroxy-5-(((1S,2R)-2-Hydroxy-2,3-Dihydro-1H-Inden-1-yl)Amino)-5-Oxopentyl)-N-(Tert-Butyl)-4-(Pyridin-3-Ylmethyl)Piperazine-2-Carboxamide Hydrate

专利信息

专利号:US-6818633-B2
优先权日:2001-06-29
标题:Antiviral compounds and methods for synthesis and therapy
发明人：BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN
权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING
摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

专利号:US-5612484-A
优先权日:1995-05-18
标题:Process for making HIV protease inhibitors
发明人：ASKIN DAVID; SAGER JESS; ROSSEN KAI; VOLANTE RALPH P; REIDER PAUL J
权利人:MERCK & CO INC
摘要:A process for making a clinically efficacious HIV protease inhibitor Compound J eliminates one step in its synthesis, by an improved, alternative synthesis of the 2(S)-4-picolyl-2-piperazine-t-butyl-carboxamide intermediate.

专利号:US-10736911-B2
优先权日:2015-12-29
标题 :Use of a DHODH inhibitor in combination with an inhibitor of pyrimidine salvage
发明人：DEANS RICHARD; OKESLI AYSE; MORGENS DAVID; KHOSLA CHAITAN; BASSIK MICHAEL C
权利人:UNIV LELAND STANFORD JUNIOR
摘要:Compounds and methods are provided for the treatment of pathogenic virus infections or cancer. The formulations combine an inhibitor of de novo pyrimidine synthesis, and an inhibitor of a pyrimidine salvage pathway enzyme.

专利号:WO-0053577-A9
优先权日:1999-03-12
标 题:Hydrazide inhibitors of hiv-1 integrase
发明人：NEAMATI NOURI; POMMIER YVES; LIN ZHAIWEI; BURKE TERRENCE
权利人:US GOV HEALTH & HUMAN SERV; NEAMATI NOURI; POMMIER YVES; LIN ZHAIWEI; BURKE TERRENCE
摘要:The design, synthesis and antiviral activity of novel mercaptosalicylhydrazides are disclosed, which inhibit human immunodeficiency virus type-1 integrase (HIV-1 IN), an essential enzyme for effective viral replication. Examples of the compounds are N,N'-bis(2-mercaptobenzoyl)hydrazide, N,N'-bis(2,2'-dithiosalicyl)hydrazide, and N,N'-bis(2-mercaptobenzyl)-2,2'-dithiosalicylhydrazide. These compounds are effective against the integrase catalytic core domain, inhibit integrase binding to HIV LTR DNA, and inhibit integrase in preassmbled integrase-DNA complexes. The disclosed mercaptosalicylhydrazides are 300 fold less cytotoxic than other known salicylhydrazides, and exhibit antiviral activity. They are also active in Mg+2-based assays, while integrase inhibition by salicylhydrazides is strictly Mn+2-dependent. The mercaptosalicylhydrazides have no detectable effect on other retroviral targets, including reverse transcriptase, protease, and virus attachment, and exhibit no detectable activity against human topoisomerase I at concentrations that effectively inhibited integrase. The mercaptosalicylhydrazides of the invention are therefore selective inhibitors of HIV-1 integrase, are useful in therapeutic compositions for the treatment of HIV disease, and can also be used to find related antiviral drugs.

专利号:CA-2794671-C
优先权日:2010-03-31
标题:Stereoselective synthesis of phosphorus containing actives

专利号:RU-2669919-C1
优先权日:2015-09-04
标题 :Pan-genomic inhibitors of the hepatitis c virus protein ns5a, pharmaceutical compositions, intermediates for the synthesis of inhibitors, and methods for their preparation and use