专利号:US-4806655-A 优先权日:1986-07-03 标题:Process for the stereospecific synthesis of indole derivatives 发明人:WAGNON JEAN; PLOUZANE CLAUDE; TONNERRE BERNARD; NISATO DINO 权利人:SANOFI SA 摘要:The present invention relates to a process for the stereo-specific synthesis of indole derivatives of formula: ##STR1## which consists in using 3-tosyloxy-1,2-O-isopropylidenepropane-1,2-diol (II) in an optically pure form in order to introduce the asymetric carbon C* of compound (I). Compound (II) is condensed with a suitable primary amine in order to prepare an oxazolidinone and condensation with a suitable phenol, and the oxazolidinone ring is then opened to form an indole compound (I).
专利号:US-2015031898-A1 优先权日:2012-03-09 标题 :Process for preparation of prostaglandin f2 alpha analogues 发明人:DAMS IWONA; KUTNER ANDRZEJ; CHODYNSKI MICHAL; KRUPA MALGORZATA; PIETRASZEK ANITA; ZEZULA MARTA; CMOCH PIOTR; KOSINSKA MONIKA 权利人:INST FARMACEUTYCZNY 摘要:A convergent synthesis of the prostaglandin F 2α analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ω-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate.
专利号:US-8445510-B2 优先权日:2010-05-14 标题 :Fused bicyclic kinase inhibitors 发明人:MULVIHILL MARK J; STEINIG ARNO G; CREW ANDREW PHILIP; JIN MEIZHONG; KLEINBERG ANDREW; LI AN-HU; WANG JING 权利人:MULVIHILL MARK J; STEINIG ARNO G; CREW ANDREW PHILIP; JIN MEIZHONG; KLEINBERG ANDREW; LI AN-HU; WANG JING; OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula I, as shown below and defined herein: n n n n n n n n n n pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.
专利号:US-7501430-B2 优先权日:2006-04-17 标题:RAF inhibitors and their uses 发明人:LAPIERRE JEAN-MARC; NAMDEV NIVEDITA D; ASHWELL MARK A; FRANCE DENNIS S; WU HUI; HUTCHINS PATRICK M; TANDON MANISH; LIU YANBIN; LINK JEFF S; ALI SYED M; BRASSARD CHRIS J; NICEWONGER ROBB B; FILIKOV ANTON; CARAZZA REBECCA J 权利人:ARQULE INC 摘要:The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAF V600E . The compounds are useful for the treatment of cell proliferative disorders such as cancer.