专利号:US-4154745-A 优先权日:1977-05-02 标题:Isobenzofuran route to anthracycloquinones 发明人:KENDE ANDREW S; TSAY YUH-GENG 权利人:RESEARCH CORP 摘要:There is provided a novel method of synthesizing certain tetracyclic quinones. In particular, there is provided a novel route to the synthesis of (±)-7-deoxydaunomycinone and analogs thereof which includes the provision of novel tetrahydronaphthoquinones and tetracyclic quinone intermediates. The compounds of the present invention are provided through a route comprising a Diels-Alder addition of certain isobenzofurans to certain novel tetrahydronaphthoquinones. The products of the synthetic route provided herein may be converted into compounds of known antibiotic and antineoplastic activity.
专利号:US-2015315143-A1 优先权日:2014-05-01 标题 :N-Heterocyclic Carbene-Catalyzed Synthesis of 2-Aryl Indoles
专利号:US-9527812-B2 优先权日:2014-05-01 标题 :N-heterocyclic carbene-catalyzed synthesis of 2-aryl indoles 发明人:SCHEIDT KARL A; HOVEY JR MICHAEL TODD; CHECK CHRISTOPHER 权利人:UNIV NORTHWESTERN 摘要:Transition metal-free catalytic methods for access to 2-arylindole compounds.
专利号:US-8461107-B2 优先权日:2008-04-28 标题:HCV NS3 protease inhibitors 发明人:LIVERTON NIGEL J; MCCAULEY JOHN A; BUTCHER JOHN W; GILBERT KEVIN F; MCINTYRE CHARLES J; RUDD MICHAEL T 权利人:LIVERTON NIGEL J; MCCAULEY JOHN A; BUTCHER JOHN W; GILBERT KEVIN F; MCINTYRE CHARLES J; RUDD MICHAEL T; MERCK SHARP & DOHME 摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
专利号:US-9133224-B2 优先权日:2010-11-29 标 题:Macrocyclic kinase inhibitors 发明人:CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W 权利人:CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W; OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.
专利号:US-10669274-B2 优先权日:2017-03-31 标 题 :Azaphenalene-3-one derivative, preparation method therefor, and application therof 发明人:ZHANG HAO; WANG XIAODONG; XU WEILIANG; XU WEIZHENG 权利人:SUZHOU KANGRUN PHARMACEUTICALS INC 摘要:Disclosed are an azaphenalene-3-one derivative, its preparation method and its application, in the field of pharmaceutical synthesis. The derivative has the following Formula (I), wherein R is H, 2-fluoroethylamino, 2,2,2-trifluoroethylamino, diethylamino, pyrrolidinyl, imidazolyl, piperidinyl, morphinolinyl, 4-methylaminopiperidinyl, 4-dimethylaminopiperidinyl, (1-methylpiperidin-4-yl)methylamino, (1-phenylpiperidin-4-yl)methylamino, (1-benzylpiperidin-4-yl)methylamino, or 7-fluoro-3,4-dihydroisoquinoline-2(1H)-yl. The preparation method of the azaphenalene-3-one derivative is simple, the yield is high, post-treatment is easy, and purity is high. The derivative has high inhibitory activity against PARP enzyme. It establishes a foundation for researching better anti-tumor drugs using PARP inhibitors.