CAS: 30651-24-2; 5-Nitro-2-Pyridinecarboxylic Acid

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2-溴-5-硝基吡啶置于copper(L) Cyanide体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 0.25H,反应生成 5-硝基-2-吡啶羧酸
参考文献: Derivatives Of Quinolines And Quinoxalines As Protein Tyrosine Kinase Inhibitors[fr] Dérivés De Quinoléines Et De Quinoxalines En Tant Qu'Inhibiteurs De Protéine Tyrosine Kinases
标题: Derivatives Of Quinolines And Quinoxalines As Protein Tyrosine Kinase Inhibitors[fr] Dérivés De Quinoléines Et De Quinoxalines En Tant Qu'Inhibiteurs De Protéine Tyrosine Kinases
摘要:该发明涉及式(i)的化合物,其中取代基如规范中定义的那样,以自由形式或作为药用盐,溶剂合物,酯,其n-氧化物的形式存在;其制备方法;含有这种化合物的药物,特别是用于治疗一个或多个蛋白酪氨酸激酶介导的疾病.

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-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:US-10308595-B2
优先权日:2013-02-15
标 题:Albicidin derivatives, their use and synthesis
发明人：SUESSMUTH RODERICH; KRETZ JULIAN; SCHUBERT VIVIEN; PESIC ALEXANDER; HUEGELLAND MANUELA; ROYER MONIQUE; COCIANCICH STEPHANE; ROTT PHILIPPE; KERWAT DENNIS; GRAETZ STEFAN
权利人:UNIV BERLIN TECH
摘要:Antibiotically active compounds characterized by general formula (I), wherein X1, BB, BC, BD, BE and X2 are building blocks with D1, D2, D3, D4 or D5 being linkers which include carbon, sulphur, nitrogen, phosphor and/or oxygen atoms and which are covalently connecting the moities BA and BB, BB and BC, BC and BD, BD and BE and BE and BF, respectively, and wherein in particular the building block BC comprises an amino acid derivative. The compounds for use in a method of treatment of diseases, in particular for use in a method of treatment of bacterial infections are also disclosed.

专利号:CN-105732488-B
优先权日:2016-03-28
标 题 :A kind of method of pyridine-2-formic acid decarboxylation synthesis 2-(2-chloroethoxy) ethoxypyridine ether compound