专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-7728135-B2 优先权日:2005-01-06 标 题:Synthesis of CCR5 receptor antagonists 发明人:SHI XIONGWEI; ZHU MAN; LEONG WILLIAM; DAHANUKAR VILAS; ZAVIALOV ILIA A; PROIETTI CECELIA; ZHAO SHANNON; LEE HONG-CHANG; LIU YI; NGUYEN HOA N; WU WENXUE; D SA BOSCO; LIANG FENG; TRAN LOC THANH 权利人:SCHERING CORP 摘要:The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.
专利号:US-10766921-B2 优先权日:2016-05-18 标 题 :Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY 权利人:NZP UK LTD 摘要:The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.
专利号:US-2012095211-A1 优先权日:2010-09-22 标 题 :Substituted proline inhibitors of hepatitis c virus replication 发明人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D 权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC 摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.
专利号:US-9227965-B2 优先权日:2011-09-22 标题 :Processes and intermediates for preparing a macrocyclic protease inhibitor of HCV 发明人:HORVATH ANDRAS; DEPRÉ DOMINIQUE PAUL MICHEL; ORMEROD DOMINIC JOHN 权利人:JANSSEN PHARMACEUTICALS INC 摘要:Disclosed is a process for the preparation of a cinchonidine salt of formula (IV) via an aqueous solution of a racemic 4-hydroxy-1,2-cyclopentanedicarboxylic acid, which is subjected to cyclization without removing water, by the addition of a water-miscible organic solvent to the aqueous solution and, again without removing water, adding cinchonidine to the aqueous-organic solvent solution so as to obtain the cinchonidine salt of the lactone acid. The cinchonidine salt is allowd to crystallize so as to obtain the enantiomerically purified crystalline lactone acid cinchonidine salt (IV). The enantiomerically pure salt is an intermediate in the synthesis of HCV inhibitor compound of formula (I).
专利号:US-2019284227-A1 优先权日:2016-05-18 标题:Intermediates for the Synthesis of Bile Acid Derivatives, in Particular of Obeticholic Acid
摘要:Duan, J.; Chen, H.; Hong, X.; Harmata, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 255. 摘要:Chemler, S. R.; Kennedy-Ellis, J. J., Science of Synthesis: Special Topics, (2022) 1, 68.