CAS: 53234-55-2; 5-Cyanopicolinic Acid

相似化合物

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CAS号76196-66-2 5-氰基-吡啶-2-羧酸甲酯 | CAS号3222-48-8 5-氰基-2-甲基吡啶 | CAS号7757-82-6 元明粉 | CAS号24242-18-0 pyridine 2-carb... | CAS号65346-04-5 5-氰基-2-吡啶甲酰胺 | CAS号29682-15-3 5-溴吡啶-2-羧酸甲酯 | CAS号100-54-9 3-氰基吡啶

5-氰基-吡啶-2-羧酸甲酯置于乙醇,Sodium Hydroxide,盐酸,水体系中,用 乙醇 作为反应溶剂,化学反应 0.17H,反应生成 5-氰基-2-吡啶羧酸
参考文献:Fused Aminodihydrothiazine Derivatives
标题:Fused Aminodihydrothiazine Derivatives
摘要:一个由以下通用公式表示的化合物:或其药用可接受的盐或其溶剂化物,其中环a是c6-14芳基或类似物,L是-nreco-或类似物(其中re是氢原子或类似物),环b是c6-14芳基或类似物,X是c1-3烷基烯基或类似物,Y是单键或类似物,Z是c1-3烷基烯基或类似物,R1和r2各自独立地是氢原子或类似物,而r3,R4,R5和r6各自独立地是氢原子,卤原子或类似物,具有aβ产生抑制作用或bace1抑制作用,并且可用作由aβ引起的以阿尔茨海默型痴呆为特征的神经退行性疾病的预防或治疗剂.

专利信息

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.

专利号:US-2016090360-A1
优先权日:2013-04-26
标题:Synthesis of bace inhibitors
发明人：FETTES ALEC; MARTY HANS-PETER; SCALONE MICHELANGELO
权利人:HOFFMANN LA ROCHE
摘要:The present invention provides a one step carbonylation of a compound of formula II in the presence of water to afford a compound of formula (I), useful in processes to manufacture BACE inhibitors.

专利号:US-RE41998-E
优先权日:1990-02-26
标题 :Compositions and methods of treatment of sympathetically maintained pain
发明人：CAMPBELL JAMES N
权利人:ARCLON THERAPEUTICS INC
摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

专利号:CA-2909136-A1
优先权日:2013-04-26
标题 :Synthesis of bace inhibitors