专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:WO-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:US-5521179-A 优先权日:1991-04-18 标题 :Heterocyclic amides 发明人:BERNSTEIN PETER R; SHAW ANDREW; THOMAS ROYSTON M; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.
专利号:US-7122549-B2 优先权日:2000-11-03 标题:Saframycins, analogues and uses thereof 发明人:MYERS ANDREW G; PLOWRIGHT ALLEYN T 权利人:HARVARD COLLEGE 摘要:In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof. n n n n n n n n n n In another aspect, the present invention provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. In yet another aspect, the present invention provides methods for treating cancer comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof.
专利号:US-8420851-B2 优先权日:2006-10-31 标 题:Selective TR-β 1 agonist 发明人:RAVAL SAURIN; RAVAL PREETI; LOHRAY BRAJ BHUSHAN; LOHRAY VIDYA BHUSHAN; PATEL PANKAJ R 权利人:RAVAL SAURIN; RAVAL PREETI; LOHRAY BRAJ BHUSHAN; LOHRAY VIDYA BHUSHAN; PATEL PANKAJ R; CADILA HEALTHCARE LTD 摘要:The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta (TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.
参考文献:10.1055/s-2007-984534 摘要:Papot S, Thomas M, Gesson J. Efficient Regio- and Stereoselective Synthesis of 1-β-O-Glucuronyl Carbamates and Carbonates from Unprotected 1,2,3,4-Hydroxyl Glucuronates. Synlett. 2007 Jul;2007(12):1966–8. doi: 10.1055/s-2007-984534. 参考文献:10.3390/ijms13010665 摘要:D'Souza MJ, Knapp JA, Fernandez-Bueno GA, Kevill DN. Use of Linear Free Energy Relationships (LFERs) to elucidate the mechanisms of reaction of a γ-methyl-β-alkynyl and an ortho-substituted aryl chloroformate ester. Int J Mol Sci. 2012;13(1):665–82.