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:WO-2011114184-A1 优先权日:2010-03-15 标题 :Amides of heterocyclic compounds as trpa1 inhibitors 发明人:CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; WAGHMARE NAYAN TATERAO; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL 权利人:GLENMARK PHARMACEUTICALS SA; CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; WAGHMARE NAYAN TATERAO; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL 摘要:Amides of heterocyclic compounds as Transient Receptor Potential subfamily A (TRPA) modulators are provided In particular, compounds described herein are useful for treating or preventing diseases, conditions and/ or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1) Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. (I).
专利号:US-7982049-B2 优先权日:2001-10-30 标 题:α-form or β-form crystal of acetanilide derivative 发明人:KAWAZOE SOUICHIROU; SAKAMOTO KENICHIROU; AWAMURA YUJI; MARUYAMA TATSUYA; SUZUKI TAKAYUKI; ONDA KENICHI; TAKASU TOSHIYUKI 权利人:ASTELLAS PHARMA INC 摘要:To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.
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.
专利号:US-4500716-A 优先权日:1981-11-19 标题 :Intermediate products for the preparation of Z-cephalosporins 发明人:KINAST GUENTHER 权利人:BAYER AG 摘要:Highly active substantially pure Z-isomers of cephalosporins are produced by the following synthesis: ##STR1## in which R 1 , R 4 and R 5 ae various organic radicals, n R 2 is alkoxycarbonyl, n Y is Cl, Br or --O--SO 2 --R 5 , and n X is a conventional cephalosporin substituent. n Many of the intermediates are new, especially in pure Z-form.
参考标题:Synthetic Chemical Diversity: Solid Phase Synthesis Of Libraries Of C2 Symmetric Inhibitors Of Hiv Protease Containing Diamino Diol And Diamino Alcohol Cores 作者:Gary T. Wang,Sam Li,Norman Wideburg,Grant A. Krafft,Dale J. Kempf |发布日期:1995.8 摘要:Structure--Activity Relationship (Sar) Studies. To Expand The Scope Of Solid Phase Synthesis Beyond The Capability Of The Traditional Method Of Solid Phase Synthesis For Peptides, A Strategy Was Developed For Bi-Directional Solid Phase Synthesis Starting With Diamino Alcohol Or Diamino Diol Core Structures. The Strategy Relies On Using Bifunctional Linkers To Modify The Core Structures, Simultaneously Protecting
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摘要:National Toxicology Program, Institute of Environmental Health Sciences, National Institutes of Health (NTP). 1992. National Toxicology Program Chemical Repository Database. Research Triangle Park, North Carolina. 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2018).