专利号:US-8835476-B2 优先权日:2005-03-04 标 题:Synthesis of novel antimicrobials 发明人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 权利人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 摘要:The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
专利号:US-5648502-A 优先权日:1992-11-23 标 题 :Regioselective synthesis of 4-chloro-2-thiophenecarboxylic acid 发明人:BURGESS LAURENCE E; SCHULTE GARY R 权利人:PFIZER 摘要:4-Chloro-2-thiophenecarboxylic acid is made by forming a compound of formula (Ia), disclosed herein, wherein R 3 is (C 1 -C 6 ) alkyl, phenyl, or benzyl; converting the compound to a compound of formula (IVa), disclosed herein, and removing the silyl group R 3 Si--. The product is useful as an intermediate in making pharmaceutical products.
专利号:US-6407103-B2 优先权日:1998-04-21 标 题:Indeno [1,2-c] pyrazol-4-ones and their uses 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-5278337-A 优先权日:1992-10-14 标 题:Enantiomeric resolution of aryl-substituted aliphatic carboxylic acids 发明人:MANIMARAN THANIKAVELU; STAHLY G PATRICK; HERNDON JR R CARL 权利人:ETHYL CORP 摘要:A process for obtaining a substantially pure enantiomer of an aryl-substituted aliphatic carboxylic acid is described. The process utilizes first an enantiomerically enriched mixture the of aryl-substituted aliphatic carboxylic acid obtained from kinetic resolution, diastereomeric crystallization or asymmetric synthesis processes. This enriched mixture is reacted with a base producing a salt that has the following properties: n 1) has at least one eutectic point; n 2) a composition that is not at the eutectic point; and n 3) a eutectic composition that is closer to the racemic composition than is the eutectic composition of said aryl-substituted carboxylic acid. n Substantially pure, enantiomeric salt is separated, leaving a mother liquor comprising the solvent and aryl-substituted aliphatic carboxylic acid enriched in the other enantiomer.
专利号:US-4471139-A 优先权日:1982-05-24 标题 :Processes for making 3-methylthiophene-2-carboxaldehyde and intermediates therefor 发明人:ANDREWS GLENN C 权利人:PFIZER 摘要:Processes for preparing isomerically pure 3-methylthiophene-2-carboxaldehyde, an intermediate for synthesis of anthelmintic agents, by reaction of mercaptoacetaldehyde or the dimer, or a polymer thereof, or a dialkylacetal thereof in the presence of a base with (1) methyl vinyl ketone or an alpha- or beta-oxidized derivative of methyl vinyl ketone to form a 3-oxobutylmercaptoacetaldehyde or dialkyl acetal thereof, or an alpha- or beta-substituted derivative thereof which is then converted to 3-methylthiophene-2-carboxaldehyde via appropriate steps including, if necessary, treatment with acid, followed, if necessary, by enamine catalyzed cyclization and, in the case of using methyl vinyl ketone as reactant, a dehydrogenation step; or (2) 3-butyn-2-one to produce a mixture of isomeric 3-oxobut-1-enylmercaptoacetaldehyde or dialkyl acetals thereof which is cyclized to 3-methylthiophene-2-carboxaldehyde. n A further aspect of this invention is an improved process for making dialkyl acetals of 2-mercaptoacetaldehyde which comprises reacting an alkyl vinyl ether with sulfur chloride to produce a bis(2-chloro-2-alkoxy ethyl)disulfide which is then treated with an alcohol to afford a bis(2,2-dialkoxyethyl)disulfide which is reduced under alkaline conditions to 2-mercaptoethyl acetaldehyde alkali metal salt which can be alkylated to a thioether, a valuable intermediate.
专利号:WO-9412505-A1 优先权日:1992-11-23 标题 :Regioselective synthesis of 4-chloro-2-thiophenecarboxylic acid