专利号:US-12275733-B2 优先权日:2016-11-07 标 题:Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders 发明人:GRETZKE DIRK; RITZELER OLAF; HEINELT UWE; WEHNER VOLKMAR; SCHMIDT FRIEDEMANN 权利人:SANOFI SA 摘要:The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
专利号:US-2023357257-A1 优先权日:2020-12-28 标 题 :Novel process for the synthesis of noroxymorphone from morphine 发明人:GORBACHEV DMITRY; LAM HON WAI; SAXENA AAKARSH; SAXENA NAVIN SATYAPAL 权利人:NAVIN SAXENA RESEARCH & TECH PVT LTD 摘要:The present invention relates to a novel, efficient, pot- and atom-economical, and industrially applicable process for converting morphine to noroxymorphone using reagents and solvents of lesser toxicity and lower cost with respect to those used in the prior art.
专利号:US-11518726-B2 优先权日:2017-10-11 标题 :Synthesis of bicyclo[2.2.2]octane derivatives 发明人:HU YUE RACHEL; HEMBRE ROBERT THOMAS; TUSTIN GERALD CHARLES; LIU ZHUFANG; ADAMS STEVEN J 权利人:EASTMAN CHEM CO 摘要:Provided is a process for the preparation of certain 1,4-bicyclo[2.2.2]octane derivatives. The new synthetic procedure involves treating 1,4-dimethylene cyclohexane with an oxidizing agent in the presence of a transition metal catalyst to afford an oxo-substituted bicyclo[2.2.2]octane species. This intermediate structure can then be further derivatized. The processes of this disclosure thus affords a novel and simplified means for the commercial production of a wide variety of bicyclo[2.2.2]octane derivatives.
专利号:US-7582771-B2 优先权日:2003-09-03 标题:Process for the synthesis of cPLA2 inhibitors 发明人:DEHNHARDT CHRISTOPH M; MEGATI SREENIVASULU; MICHALAK RONALD S; RAVEENDRANATH PANOLIL; REN JIANXIN; WU CHARLES C; WU YANGZHONG 权利人:WYETH CORP 摘要:A process for making the compound of formula (I) n nwherein Ac represents acetate; X represents O or CH 2 ; Y represents C 1 -C 6 alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF 3 , OCF 3 , OH, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 thioalkyl, NH 2 , N(C 1 -C 6 alkyl) 2 , NH(C 1 -C 6 alkyl), NC(O)—(C 1 C 6 alkyl), and NO 2 . In his process, a compound of formula (II)n n nis reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).
专利号:US-12378246-B2 优先权日:2019-04-11 标 题:Synthetic options towards the manufacture of (6R,10S)-10-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6H)-pyrimidinyl} - 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(metheno)pyrazolo[4,3-b][1,7]diazacyclotetradecin-5(6H)-one 发明人:CUNIERE NICOLAS; FAN YU; KOLOTUCHIN SERGEI; MUKHERJEE SUBHA; SIMMONS ERIC M; SINGH AMARJIT; WEI CAROLYN S; XIAO YI; YUAN CHANGXIA; ZHENG BIN; WAGSCHAL SIMON ALBERT; BROGGINI DIEGO FERNANDO DOMENICO; CAO DUY CHI TRUNG; CHERNICHENKO KOSTIANTYN; LEMAIRE SEBASTIEN FRANCOIS EMMANUEL; BEN HAÃ?M CYRIL 权利人:BRISTOL MYERS SQUIBB CO; JANSSEN PHARMACEUTICA NV 摘要:Highly efficient methods are provided for preparing key intermediates in the synthesis of Compound (I), which are broadly applicable and can provide selected components having a variety of substituents groups.
专利号:US-7030281-B2 优先权日:2002-03-21 标题 :Synthesis of 3,3,-dimethylbutyraldehyde by the reduction of 3,3,-dimethylbutyric acid 发明人:PRAKASH INDRA; AUGUSTINE ROBERT L; TANIELYAN SETRAK K 权利人:NUTRASWEET CO 摘要:A process for the production of 3,3-dimethylbutyraldehyde is disclosed. The 3,3-dimethylbutyraldehyde is obtained by the reduction of 3,3-dimethylbutyric acid using trimethylacetic anhydride and a phosphine. The 3,3-dimethylbutyric acid is preferably obtained by a process in which tert-butanol and vinylidene chloride are reacted in the presence of sulfuric acid. The disclosed process has improved cost and yield.
摘要:Tobe, Y.; Takeda, T., Science of Synthesis, (2010) 45, 1344. 摘要:Koo, S., Science of Synthesis, (2010) 45, 1356. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 572. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 591. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 594.