专利号:US-6608202-B1 优先权日:2001-08-21 标题:Process of synthesis of a tricyclic ketone intermediate 发明人:DORAN HENRY J; O'NEILL PAT M; WILLIAMS ROBERT P 权利人:SCHERING CORP 摘要:In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen,and intermediates therefor from easily available starting materials by a simple route.
专利号:US-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-9085535-B2 优先权日:2009-07-27 标 题 :Method and substances for the preparation of N-substituted pyridinium compounds 发明人:HEINDL DIETER; GEBAUER PETER 权利人:HEINDL DIETER; GEBAUER PETER; ROCHE DIAGNOSTICS OPERATIONS 摘要:Methods for the synthesis of N-substituted carboxylated pyridinium compounds by reaction of a pentamethine precursor with a primary amine are provided. In this reaction an N-substituted alkoxycarbonyl pyridinium heterocycle is formed.
专利号:US-2003144314-A1 优先权日:2001-08-21 标 题 :Process of synthesis of a tricyclic ketone intermediate
专利号:EP-3567040-B1 优先权日:2013-06-24 标 题 :Method for the preparation of intermediates useful for the synthesis of [1,2,4]-triazolo[4,3-a]pyridines
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