40473-01-6 = 86873-60-1 反应条件:1.1 Reagents: Butyllithium Solvents: Diethyl Ether,Hexane; 2 H,-78 °C1.2 2 H,-78 °C; -78 °C -> Rt 标题:2-Aminomethylphenylamine As A Novel Scaffold For Factor Xa Inhibitor 作者:Mochizuki,Akiyoshi; Et Al 参考文献:Bioorganic & Medicinal Chemistry 日期:2011 卷标:19(5) 页码:1623-1642]
2138-22-9 = 86873-60-1 反应条件:1.1 -1.2 Reagents: Ammonia Solvents: Water 标题:Catechol 2,3-Dioxygenase-Catalyzed Synthesis Of Picolinic Acids From Catechols 作者:Asano,Yasuhisa; Et Al 参考文献:Bioscience 日期:1994 卷标:58(11) 页码:2954-6]
1072-98-6 = 86873-60-1 反应条件:1.1 Reagents: Bromine,Hydrogen Bromide Solvents: Water; -5 - 0 °C1.2 Reagents: Sodium Nitrite Solvents: Water; 3 H,0 °C -> 15 °C1.3 Reagents: Sodium Hydroxide,Sodium Thiosulfate Solvents: Diethyl Ether,Water2.1 Reagents: Butyllithium Solvents: Diethyl Ether,Hexane; 2 H,-78 °C2.2 2 H,-78 °C; -78 °C -> Rt 标题:2-Aminomethylphenylamine As A Novel Scaffold For Factor Xa Inhibitor 作者:Mochizuki,Akiyoshi; Et Al 参考文献:Bioorganic & Medicinal Chemistry 日期:2011 卷标:19(5) 页码:1623-1642]
6960-22-1 = 86873-60-1 反应条件:1.1 Reagents: Sodium Hypochlorite2.1 Reagents: Sodium Nitrite,Hydrochloric Acid,Cuprous Chloride3.1 Reagents: Permanganic Acid (Hmno4),Potassium Salt (1:1) 标题:Preparation Of Some 4- And 5-Substituted Pyridine-2-Carboxylic Acids As Fusaric Acid Analogs 作者:Oehlke,J.; Et Al 参考文献:Pharmazie 日期:1983 卷标:38(9) 页码:591-6]
86873-60-1 = 86873-60-1 反应条件:1.1 Solvents: Acetonitrile,Water; Overnight,Ph 9.5,Rt1.2 Reagents: Ethanol1.3 Reagents: Molybdenum Hexacarbonyl,Cesium Hydroxide Catalysts: Palladate(1-),[2′-(Amino-Kn)[1,1′-Biphenyl]-2-Yl-Kc]Chloro[2′-(Dicyclohexylphos... Solvents: 1-Methoxy-2-Propanol,Water; 15 H,80 °C 标题:Palladium-Catalyzed Hydroxycarbonylation Of (Hetero)Aryl Halides For Dna-Encoded Chemical Library Synthesis 作者:Li,Jian-Yuan; Et Al 参考文献:Bioconjugate Chemistry 日期:2019 卷标:30(8) 页码:2209-2215]
72093-07-3 = 86873-60-1 反应条件:1.1 Reagents: Permanganic Acid (Hmno4),Potassium Salt (1:1) 标题:Preparation Of Some 4- And 5-Substituted Pyridine-2-Carboxylic Acids As Fusaric Acid Analogs 作者:Oehlke,J.; Et Al 参考文献:Pharmazie 日期:1983 卷标:38(9) 页码:591-6]
3430-14-6 = 86873-60-1 反应条件:1.1 Reagents: Sodium Nitrite,Hydrochloric Acid,Cuprous Chloride2.1 Reagents: Permanganic Acid (Hmno4),Potassium Salt (1:1) 标题:Preparation Of Some 4- And 5-Substituted Pyridine-2-Carboxylic Acids As Fusaric Acid Analogs 作者:Oehlke,J.; Et Al 参考文献:Pharmazie 日期:1983 卷标:38(9) 页码:591-6]
21684-59-3 = 86873-60-1 反应条件:1.1 Reagents: Ammonia2.1 Reagents: Sodium Hypochlorite3.1 Reagents: Sodium Nitrite,Hydrochloric Acid,Cuprous Chloride4.1 Reagents: Permanganic Acid (Hmno4),Potassium Salt (1:1) 标题:Preparation Of Some 4- And 5-Substituted Pyridine-2-Carboxylic Acids As Fusaric Acid Analogs 作者:Oehlke,J.; Et Al 参考文献:Pharmazie 日期:1983 卷标:38(9) 页码:591-6]
3222-47-7 = 86873-60-1 反应条件:1.1 -2.1 Reagents: Ammonia3.1 Reagents: Sodium Hypochlorite4.1 Reagents: Sodium Nitrite,Hydrochloric Acid,Cuprous Chloride5.1 Reagents: Permanganic Acid (Hmno4),Potassium Salt (1:1) 标题:Preparation Of Some 4- And 5-Substituted Pyridine-2-Carboxylic Acids As Fusaric Acid Analogs 作者:Oehlke,J.; Et Al 参考文献:Pharmazie 日期:1983 卷标:38(9) 页码:591-6
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-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:EP-3515880-B1 优先权日:2017-03-17 标题:Methods and compositions for synthesis of encoded libraries 发明人:LI JIN; MORGAN BARRY A; Wan jinqiao; DOU DENGFENG; LIU GUANSAI; CHANG YONG; CHEN QIUXIA; WANG XING; XU YANSHAN; HU DONGYAN; LIU JIAN; CHENG XUEMIN 权利人:HITGEN INC