专利号:US-7179919-B2 优先权日:2004-03-18 标 题 :Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:SONG JINHUA J; TAN ZHULIN; YEE NATHAN K; SENANAYAKE CHRIS HUGH; XU JINGHUA; GALLOU FABRICE 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:A process for stereoselective synthesis of a compound of Formula (I) n nwherein R 1 , R 2 , R 3 , R 4 , and R 5 are as described herein.
专利号:US-7425629-B2 优先权日:2005-09-30 标 题:Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:SONG JINHUA J; REEVES JONATHAN T; ROSCHANGAR FRANK; TAN ZHULIN; YEE NATHAN K 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:A process for stereoselective synthesis of a compound of Formula (I) n nwherein R 1 , R 2 , R 3 , R 4 , and R 5 are as described herein.
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-2005209488-A1 优先权日:2004-03-18 标 题 :Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
专利号:US-2007100142-A1 优先权日:2005-09-30 标 题 :Stereoselective Synthesis of Certain Trifluoromethyl-Substituted Alcohols
专利号:US-6136982-A 优先权日:1999-01-22 标 题:Synthesis of 3-amino-2-chloro-4-methylpyridine from acetone and ethyl cyanoacetate 发明人:GROZINGER KARL 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:A method for making 3-amino-2-chloro-4-methylpyridine from acetone and ethyl cyanoacetate, as depicted in the following reaction scheme. ##STR1##
参考标题: Proteasome Activity Enhancing Compounds Composés Renforçant L'Activité Des Protéasomes 摘要:The Present Invention Is Directed To Compounds Having The Formula (I), (II), (III), (Iv), And (V), Compositions Thereof, The Methods Of Synthesis Of The Compouds Of Interest, And To Methods For The Treatment Of A Condition Associated With A Dysfunction In Proteostasis, Such As Cancer, Inflammatory Conditions, Neurodegeneration, Metabolic Conditions, Comprising Administering An Effective Amount Of A Compound Of The Invention.