专利号:US-7514559-B2 优先权日:2004-03-22 标题 :Catalyst for synthesis of 2- and 4-picolines 发明人:DUTTA PASHUPATI; ROY SUBHASH CHANDRA; ROY SHYAM KISHORE; GOSWAMI TARUN KANTI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides a catalyst composite for the synthesis of 2- and 4-picolines and a process for the preparation thereof and use thereof for the synthesis of 2- and 4-Picolines.
专利号:US-6844434-B2 优先权日:2001-01-18 标题 :Synthesis of temozolomide and analogs 发明人:KUO SHEN-CHUN 权利人:SCHERING CORP 摘要:This invention relates to a novel process for the synthesis of temozolomide, an antitumor compound, and to intermediates useful in this novel process.
专利号:US-2013012706-A1 优先权日:2010-03-01 标 题 :Methods and Intermediates for the Synthesis of 4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazines 发明人:HUMMERSONE MARC GEOFFERY; COUSIN DAVID 权利人:PHARMINOX LTD; HUMMERSONE MARC GEOFFERY; COUSIN DAVID 摘要:The present invention provides a compound of general formula (II), or a salt or solvate thereof: n n n n n n n n n n n n wherein n A is independently -A 1 , -A 2 , -A 3 , -A 4 , -A 5 , -A 6 , or -A 7 , wherein:n -A 1 is independently C 5-12 heteroaryl, and is optionally substituted; -A 2 is independently thioamido or substituted thioamido; -A 3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A 4 is independently hydroxamic acid or hydroxamate; -A 5 is independently carboxamide or substituted carboxamide; -A 6 is independently aliphatic C 2-6 alkenyl, and is optionally substituted; and -A 7 is independently carboxy or C 1-4 alkyl-carboxylate;n nand its use in the synthesis of temozolomide and analogues thereof.
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:WO-9101724-A1 优先权日:1989-07-27 标题 :Renal-selective prodrugs for 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 depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors 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-Y-glutamyl fusaric acid is preferred.
专利号:WO-9201667-A1 优先权日:1990-07-25 标题 :Renal-selective prodrugs for control of renal sympathetic 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 kydney. 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-η-glutamyl fusaric acid hydrazide [represented in formula (a)] is preferred.