CAS: 24242-20-4; 5-Aminopicolinic Acid

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848308-47-4 30651-24-2 55338-73-3

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📜2-溴-5-硝基吡啶置于盐酸,Ammonium Hydroxide,硫化氢体系中,化学反应 1.58H,反应生成5-氨基-2-吡啶羧酸
参考文献:Comparison Of Two Synthetic Methods To Obtain [18F] N-(2-Aminoethyl)-5-Fluoropyridine-2-Carboxamide,A Potential Mao-B Imaging Tracer For Pet
标题:Comparison Of Two Synthetic Methods To Obtain [18F] N-(2-Aminoethyl)-5-Fluoropyridine-2-Carboxamide,A Potential Mao-B Imaging Tracer For Pet
摘要:化合物ro 19-6327,即n-(2-氨基乙基)-5-氯吡啶-2-甲酰胺,已知能可逆且特异性地抑制单胺氧化酶b(mao-B).其123I标记的碘类似物n-(2-氨基乙基)-5-碘吡啶-2-甲酰胺(ro 43-0463)已成功通过单光子发射断层扫描(spet)在人体志愿者中进行了研究.因此,我们开发了相应的氟类似物n-(2-氨基乙基)-5-氟吡啶-2-甲酰胺与18F的合成及放射性标记,以进行正电子发射断层扫描(pet)研究与mao-B相关的神经精神疾病.为此,我们采取了两种合成途径以实现18F放射性标记的亲电法和亲核法.当考虑到前体合成,束流时间,比活度和放射化学纯度等因素时,亲核法显示出优势.
Doi:10.1002/jlcr.2580361005

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:CN-117897379-A
优先权日:2021-08-30
标 题:Process for the synthesis of naphthyridine derivatives and intermediates thereof

专利号:US-11530205-B2
优先权日:2017-04-28
标题:GLP-1 receptor modulators
发明人：TAMIYA JUNKO; TURNBULL PHILIP; ENUGURTHI BRAHMACHARY; HUANG LIMING; YEAGER ADAM R; FOWLER THOMAS; IACOBINI GREG P; CRITTALL MATTHEW RICHARD
权利人:RECEPTOS LLC
摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as products containing such compounds, and methods of their use and synthesis. Such compounds have the structure of Formula (I) below: (I) or pharmaceutically acceptable salts thereof, wherein A, J, W 1 , Y, Z, R 1 , R 2 , R 3 and R 4 are as defined herein.