专利号:US-4876280-A 优先权日:1988-03-10 标题 :Arylcyclohexane and arylcyclohexene analogs of mevalonolactone derivatives and their use 发明人:DAMON II ROBERT E 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein R1 is hydrogen, C1-3alkyl, n-butyl, i-butyl or t-butyl, R2 is hydrogen or C1-3alkyl, R3 is hydrogen or C1-3alkyl, R4 is hydrogen, C1-3alkyl, n-butyl, i-butyl or t-butyl, R5 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, fluoro, chloro, trifluoromethyl, phenoxy or benzyloxy, R6 is hydrogen, C1-3alkyl, C1-3alkoxy, fluoro, chloro, trifluoromethyl, phenoxy or benzyloxy, with the provisos that not more than one of R5 and R6 is trifluoromethyl, not more than one of R5 and R6 is phenoxy, and not more than one of R5 and R6 is benzyloxy, or R5 and R6 are attached to adjacent carbon atoms and taken together form a radical of the formula -CH=CH-CH=CH-, R6a is hydrogen, C1-2alkyl, fluoro or chloro, X is -CH2CH2- or wherein R7 is hydrogen or C1-3alkyl, and R8 is hydrogen, R9 or M, wherein R9 is a physiologically acceptable ester group, and M is a pharmaceutically acceptable cation, and the broken line represents a double ( pi ) bond or two hydrogen atoms (one on each carbon atom), the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:US-2003092064-A1 优先权日:2001-04-05 标题 :System for the synthesis of spatially separated libraries of compounds and methods for the use thereof 发明人:READER JOHN C 权利人:MILLENNIUM PHARM INC 摘要:Featured is an apparatus useful for preparing combinatorial libraries of compounds in a parallel fashion so that the individual compounds of the library are spatially separate and the position of each compound of the library in the apparatus is known. Moreover, the apparatus is useful for the preparation of combinatorial libraries of compounds where the library is constructed from three or more building blocks, e.g., three, four, five, six or seven building blocks, resulting in a three, four, five, six or seven dimensional combinatorial library. Also featured are related methods for the preparation of three, four, five, six or seven dimensional combinatorial libraries of compounds using the apparatus of the present invention.
专利号:US-9085605-B2 优先权日:2010-05-27 标 题:Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate 发明人:LIU GANG; ZHAO NAN; MA YAO 权利人:LIU GANG; ZHAO NAN; MA YAO; SHENZHEN SALUBRIS PHARM CO LTD 摘要:The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-2008214565-A1 优先权日:2003-04-07 标 题:Oxazolidinone Derivatives as Antimicrobials 发明人:MEHTA ANITA; RUDRA SONALI; RAO AJJARAPU VENKATA SUBRAHMANYA RAJO; YADAV AJAY SINGH; RATTAN ASHOK 权利人:MEHTA ANITA; RUDRA SONALI; RAO AJJARAPU VENKATA SUBRAHMANYA RAJO; YADAV AJAY SINGH; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones of formula I and H and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
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