专利号:US-2024182642-A1 优先权日:2022-11-23 标 题:Green synthesis of amino acid based poly(ester urea)s 发明人:OLSEN BRADLEY DAVID; FRANSEN KATHARINA 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods of synthesizing poly(ester urea)s.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 权利人:LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-8703747-B2 优先权日:2008-07-23 标题 :Aminophosphinic derivatives that can be used in the treatment of pain 发明人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE 权利人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE; PHARMALEADS 摘要:The present invention relates to a compound of the following general formula (I): R 1 —NH—CH(R 2 )—P(â•?O)(OR 3 )—CH 2 —C(R 4 )(R 5 )—CONH—CH(R 6 )—COOR 7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R 1 represents a —C(â•?O)—O—C(R 8 )(R 9 )—OC(â•?O)—R 10 group; R 2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R 3 represents a hydrogen atom or a —C(R 12 )(R 13 )—OC(â•?O)—R 14 group; R 4 and R 5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R 4 represents a hydrogen atom and R 5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R 6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R 7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, —CHMe—COOR 18 , —CHR 19 —OC(â•?O)OR 20 and —CHR 19 —OC(â•?O)OR 20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more avantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
专利号:US-7732436-B2 优先权日:2003-05-19 标 题 :Preparation of hymenialdisine derivatives and use thereof 发明人:TEPE JETZE J 权利人:UNIV MICHIGAN STATE 摘要:The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of cytokines interleukin-2 (IL-2) and tumor necrosis factor-α (TNF-α). The chemically-synthesized indoloazepines of the invention also inhibit production of IL-2 and TNF-α. The indoloazepines are useful for treating inflammatory diseases, particularly diseases associated with kinases NF-κB or GSK-3β activation or NF-κB activated gene expression products. The indoloazepines are useful for the treatment of cancer by the inhibition of kinases CHK1 and CHK2.
专利号:CN-102532199-A 优先权日:2012-02-29 标 题:Structure and Synthesis of Novel Benzyl Phosphoramidate Prodrugs of Nucleoside Compounds
参考标题:Facile One-Step Synthesis Of 2,5-Diketopiperazines 作者:Xianyu Sun,Rachita Rai,Alexander D. Mackerell,Alan I. Faden,Fengtian Xue |发布日期:2014.3 摘要:We Report A One-Step Protocol For The General Synthesis Of 2,5-Diketopiperazines From An Fmoc-Protected Amino Acid And An Amino Acid Ester. The Application Of The Method Is Highlighted By Rapid And Efficient Preparation Of Various 2,5-Diketopiperazines.