3-Amino-1-p-chlorphenyl-1,2,4-triazol | 52512-67-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-Amino-1-p-chlorphenyl-1,2,4-triazol
• 英文别名: 1-(4-chloro-phenyl)-1H-[1,2,4]triazol-3-ylamine；1-(4-chlorophenyl)-1H-1,2,4-triazol-3-amine；1-(4-Chloro-phenyl)-1H-[1,2,4]triazol-3-ylamine；1-(4-chlorophenyl)-1,2,4-triazol-3-amine
• CAS: 52512-67-1
• 化学式: C₈H₇ClN₄
• 分子量: 194.623
• InChiKey: ZQNILSIUCMKROX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  56.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-bromo-2-(4-methyl-1H-imidazol-1-yl)benzonitrile 、 3-Amino-1-p-chlorphenyl-1,2,4-triazol 以The title compound was obtained as a colorless solid (Yield=18%)的产率得到5-[1-(4-chloro-phenyl)-1H-[1,2,4]triazol-3-ylamino]-2-(4-methyl-imidazol-1-yl)-benzonitrile
  参考文献：
  名称：

  Heterocyclic gamma secretase modulators

  摘要：

  本发明涉及用于治疗阿尔茨海默病、脑淀粉样血管病、遗传性淀粉样脑出血、荷兰型（HCHWA-D）、多发性梗塞性痴呆、拳击性痴呆和唐氏综合征的方法，其包括向患者施用公式I的化合物的治疗有效量，其中R1、R2、R3、V、W、Y和Z如本文所定义，或这些化合物的药物活性酸盐。本发明还涉及这些化合物的亚属和含有它们的药物组合物，以及它们的制造方法。

  公开号：

  US08288403B2
• 作为产物：
  描述：

  3-氨基-5-苯基-1,2,4-噁二唑 、 对氯苯胺 以The title compound was obtained as brownish solid (Yield=54%)的产率得到3-Amino-1-p-chlorphenyl-1,2,4-triazol
  参考文献：
  名称：

  Heterocyclic gamma secretase modulators

  摘要：

  本发明涉及用于治疗阿尔茨海默病、脑淀粉样血管病、遗传性淀粉样脑出血、荷兰型（HCHWA-D）、多发性梗塞性痴呆、拳击性痴呆和唐氏综合征的方法，其包括向患者施用公式I的化合物的治疗有效量，其中R1、R2、R3、V、W、Y和Z如本文所定义，或这些化合物的药物活性酸盐。本发明还涉及这些化合物的亚属和含有它们的药物组合物，以及它们的制造方法。

  公开号：

  US08288403B2

文献信息

• HETEROCYCLIC GAMMA SECRETASE MODULATORS
  申请人：Baumann Karlheinz

  公开号：US20100120874A1

  公开（公告）日：2010-05-13

  The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R 1 , R 2 , R 3 , V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.

  该发明涉及治疗阿尔茨海默病、脑淀粉样血管病、遗传性淀粉样脑出血、荷兰型（HCHWA-D）、多梗塞性痴呆、拳击性痴呆和唐氏综合征的方法，包括给予化合物I的治疗有效量，其中R1、R2、R3、V、W、Y和Z如本文所定义，或者是这些化合物的药用活性酸盐。该发明还涉及这些化合物的亚属和含有它们的药物组合物，以及它们的制备方法。
• Method for reducing a susceptibility to tumor formation induced by 3-deoxyglucosone and precursors thereof
  申请人：Brown R. Truman

  公开号：US20060089316A1

  公开（公告）日：2006-04-27

  Disclosed are methods of using various compounds, which are known to bind to 3-deoxyglucosone (3DG) or precursors thereof, in order to reduce a susceptibility to tumor formation and/or to prevent or delay onset of tumor formation induced by 3DG and its precursors. Also disclosed is the reduction of 3DG levels in high fructose corn syrop so that the high fructose corn syrup is less likely to induce tumor formation.

  公开了使用各种已知与3-脱氧葡萄糖酮（3DG）或其前体结合的化合物的方法，以减少对肿瘤形成的易感性和/或预防或延迟由3DG及其前体诱导的肿瘤形成。还公开了降低高果糖玉米糖浆中3DG水平的方法，以使高果糖玉米糖浆不太可能诱导肿瘤形成。
• US5318982A
  申请人：——

  公开号：US5318982A

  公开（公告）日：1994-06-07
• US8288403B2
  申请人：——

  公开号：US8288403B2

  公开（公告）日：2012-10-16
• [EN] HETEROCYCLIC GAMMA SECRETASE MODULATORS<br/>[FR] MODULATEURS DE LA GAMMA SECRÉTASE HÉTÉROCYCLIQUE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2010052199A1

  公开（公告）日：2010-05-14

  The invention relates to the use of compounds of formula wherein R1 is a five or six membered heteroaryl group, optionally substituted by one or two R'; R' is lower alkyl; R2 is hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or cyano; Z is N, C, O or S; V is N, C(R''), O or S; W is N, C(R''), O, or S; Y is N or C; with the proviso that only one of Z, V or W may be O or S; R'' is hydrogen, lower alkyl, lower alkyl substituted by halogen or hydroxy, or is C(O)O-R4; L is a bond, -(CR42)n-, -C(O)NR4-, -C(O)NR4CH2-, or -C(O)-; R4 may be the same or different and is hydrogen or lower alkyl; R3 is lower alkyl, phenyl, optionally substituted by one or more R''' or is cycloalkyl; R''' is halogen, cyano, lower alkyl, lower alkyl substituted by halogen or hydroxy, or is lower alkoxy or is C(O)O-R4; n is 1, 2 or 3; or to pharmaceutically active acid addition salts for the manufacture of medicaments for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.