专利号:US-9573934-B2 优先权日:2011-01-26 标题 :Methods and compositions for the synthesis of multimerizing agents 发明人:LI FENG; WANG YIHAN 权利人:ARIAD PHARMA INC 摘要:The invention features methods and compositions for the synthesis of multimerizing agents.
专利号:US-6177572-B1 优先权日:1997-08-20 标题 :Solid and liquid-phase synthesis of benzoxazoles and benzothiazoles and their use 发明人:WANG FENGJIANG 权利人:SEPRACOR INC 摘要:Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.
专利号:US-5942632-A 优先权日:1995-07-28 标题:Solid phase synthesis method 发明人:WANG GARY T 权利人:ABBOTT LAB 摘要:A solid phase synthesis method and intermediates useful in the process are disclosed for the preparation of diamino diol and diamino alcohol inhibitors of HIV protease.
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-8853228-B2 优先权日:2007-06-04 标 题:Heterocyclic analogs of propargyl-linked inhibitors of dihydrofolate reductase 发明人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE 权利人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE; UNIV CONNECTICUT 摘要:The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
专利号:US-8426432-B2 优先权日:2007-06-04 标 题 :Inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties 发明人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO 权利人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO; UNIV CONNECTICUT 摘要:The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
参考标题:Synthesis Of Halogenated Trimetoquinol Derivatives And Evaluation Of Their .Beta.-Agonist And Thromboxane A2 (Txa2) Antagonist Activities 作者:K. M. Markovich,V. Tantishaiyakul,A. Hamada,D. D. Miller,K. J. Romstedt,G. Shams,Y. Shin,P. F. Fraundorfer,K. Doyle,D. R. Feller |发布日期:1992.2 摘要:Activities While Imparting Weak Antagonist Activity On Beta 1 Receptors. On Txa2 Systems, Both 4 And 7 Possessed Significantly Decreased Inhibitory Activity Compared To Tmq. The Synthetic Approaches To The Synthesis Of 8-(Trifluoromethyl)-Tmq (8) Are Also Described. The Enantiomers Of The 8-Fluoro Derivative (3) Of Tmq Were Separated On A Preparative Chiralcel Od Column And Evaluated On Beta-Adrenergic Systems