专利号:US-11655255-B2 优先权日:2022-10-17 标题 :Method for catalytic asymmetric synthesis of phosphorus-stereogenic (P-stereogenic) nucleoside derivative and catalyst used therein 发明人:ZHANG WANBIN; WANG MO; ZHANG LU; HUO XIAOHONG; ZHANG ZHENFENG; YUAN QIANJIA; CHEN JIANZHONG 权利人:SPH NO 1 BIOCHEMICAL & PHARMACEUTICAL CO LTD; UNIV SHANGHAI JIAOTONG 摘要:A method for catalytic asymmetric synthesis of a phosphorus-stereogenic (P-stereogenic) nucleoside derivative of formula (3) and a catalyst used therein. The P-stereogenic nucleoside derivative (3) can be hydrolyzed to obtain remdesivir. Specifically, a nucleoside and phosphoryl chloride are subjected to asymmetric reaction under the catalysis of a chiral bicyclic imidazole catalyst in the presence of a base to produce the P-stereogenic nucleoside derivative of formula (3)
专利号:WO-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 权利人:LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-9035061-B2 优先权日:2010-07-13 标题:Process for preparing a biphenyl-2-ylcarbamic acid 发明人:COLSON PIERRE-JEAN 权利人:COLSON PIERRE-JEAN; THERAVANCE BIOPHARMA R & D IP LLC 摘要:The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.
专利号:US-2023085986-A1 优先权日:2022-10-17 标 题:Method for catalytic asymmetric synthesis of phosphorus-stereogenic (p-stereogenic) nucleoside derivative and catalyst used therein