(S)-1-(4-(trifluoromethyl)phenyl)pyrrolidin-3-amine | 202267-19-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (S)-1-(4-(trifluoromethyl)phenyl)pyrrolidin-3-amine
• 英文别名: 1-(4-trifluoromethyl)phenyl-(3S)-pyrrolidin-3-ylamine；(3S)-1-[4-(trifluoromethyl)phenyl]pyrrolidin-3-amine
• CAS: 202267-19-4
• 化学式: C₁₁H₁₃F₃N₂
• 分子量: 230.233
• InChiKey: JESYTMXMXNUFCV-VIFPVBQESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (S)-1-(4-(trifluoromethyl)phenyl)pyrrolidin-3-amine 、 trans-2-(1H-benzo[d]imidazol-2-yl)cyclopropane-1-carboxylic acid 在 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以14 mg的产率得到Trans-2-(1H-benzo[d]imidazol-2-yl)-N-((S)-1-(4-(trifluoromethyl)phenyl)pyrrolidin-3-yl)cyclopropane-1-carboxyamide
  参考文献：
  名称：

  EP3825303

  摘要：

  公开号：

文献信息

• USE OF T-TYPE CALCIUM CHANNEL BLOCKER FOR TREATING PRURITUS
  申请人：Nippon Chemiphar Co., Ltd.

  公开号：EP3950059A1

  公开（公告）日：2022-02-09

  A medicament for treating or preventing pruritus is provided. For the medicament for treating or preventing pruritus, a compound having a blocking action on Cav3.2T-type calcium channels represented by General Formulas (I) to (VI), a tautomer of the compound, a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an active ingredient.

  提供一种用于治疗或预防瘙痒的药物。用于治疗或预防瘙痒的药物中，使用具有对Cav3.2T型钙通道具有阻断作用的化合物，该化合物以一般式(I)至(VI)表示，该化合物的互变异构体、立体异构体、其药用可接受的盐或其溶剂为活性成分。
• Methods of treating insulin resistance syndrome and diabetes
  申请人：——

  公开号：US20030176390A1

  公开（公告）日：2003-09-18

  This invention is directed to methods of treating insulin resistance syndrome and diabetes in a patient in need thereof, comprising administering to said patient a pharmaceutically effective amount of a compound derived from adenosine and analogues thereof, or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable prodrug thereof, an N-oxide thereof, a hydrate thereof or a solvate thereof, or a pharmaceutical composition comprising such compound.

  本发明涉及治疗胰岛素抵抗综合征和糖尿病的方法，包括向需要治疗的患者施用从腺苷和其类似物衍生的化合物的药效量，或其药用盐、药用前药、N-氧化物、水合物或溶剂化合物，或包含该化合物的药物组合物。
• Compounds having antihypertensive, cardioprotective anti-ischemic and antilipolytic properties
  申请人：——

  公开号：US20020099030A1

  公开（公告）日：2002-07-25

  This invention relates to adenosine derivatives and analogues which possess biological activity and are useful as anti-hypertensive, cardioprotective, anti-ischemic, and antilipolytic agents, to pharmaceutical compositions including such compounds, and to their use in treating hypertension, myocardial ischemia, ameliorating ischemic injury and myocardial infarct size consequent to myocardial ischemia, and treating hyperlipidemia and hypercholesterolemia, and to methods and intermediates used in the preparation of such compounds.

  本发明涉及腺苷衍生物和类似物，具有生物活性，可用作抗高血压、心脏保护、抗缺血和抗脂解作用的药物，包括这些化合物的制药组合物，以及它们在治疗高血压、心肌缺血、改善缺血损伤和心肌梗死大小，治疗高脂血症和高胆固醇血症方面的用途，以及用于制备这些化合物的方法和中间体。
• Adenosine analogues for the treatment of insulin resistance syndrome and diabetes
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1258247A1

  公开（公告）日：2002-11-20

  The invention relates to the use of adenosine compounds described by formula I and certain derivatives thereof for producing a medicine for the treatment of the insulin resistance syndrome and diabetes. In the formula I K is N, N→O, or CH; Q is CH2 or O; R6 is hydrogen, alkyl, allyl, 2-methallyl, 2-butenyl, or cycloalkyl; E is O or S; Y is e.g. hydrogen, alkyl, aralkyl, aryl; n and p are independently 0, 1, 2, or 3, provided that n + p is at least 1; T is e.g hydrogen, alkyl, acyl, thioacyl, halo, carboxyl; R1, R2 and R3 are independently H, alkyl, or cycloalkyl; A is hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, or OR'; B is hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, or OR"; R' and R" are e.g independently hydrogen, alkyl, aralkyl or carbamoyl.

  本发明涉及式 I 所述腺苷化合物及其某些衍生物用于生产治疗胰岛素抵抗综合征和糖尿病的药物。 及其某些衍生物用于生产治疗胰岛素抵抗综合征和糖尿病的药物。 在式 I 中 K 是 N、N→O 或 CH； Q 是 CH2 或 O； R6 是氢、烷基、烯丙基、2-甲基烯丙基、2-丁烯基或环烷基； E 是 O 或 S； Y 是氢、烷基、芳烷基或芳基； n 和 p 独立地为 0、1、2 或 3，条件是 n + p 至少为 1； T 例如是氢、烷基、酰基、硫代酰基、卤代酰基、羧基； R1、R2 和 R3 独立地是氢、烷基或环烷基； A 是氢、烷基、羟烷基、烷氧基烷基或 OR'； B 是氢、烷基、羟烷基、烷氧基烷基或 OR"； R'和 R "例如独立地为氢、烷基、芳烷基或氨基甲酰基。
• T-TYPE CALCIUM CHANNEL BLOCKER
  申请人：Nippon Chemiphar Co., Ltd.

  公开号：EP3825303A1

  公开（公告）日：2021-05-26

  To provide a novel T-type calcium channel blocker. A compound represented by the following General Formula (I), a tautomer or a stereoisomer of the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound, the tautomer, the stereoisomer, or the salt is used as a T-type calcium channel blocker. wherein A represents a phenyl which may have a substituent, a 4-membered to 6-membered heteroaryl ring composed of one to three identical or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom and carbon atoms as ring-constituting atoms, or a heterocondensed ring composed of the heteroaryl ring and either a benzene ring or a 6-membered heteroaryl ring composed of one to two nitrogen atoms and carbon atoms, wherein the heteroaryl ring or the heterocondensed ring may have a substituent and is bonded to a nitrogen atom of the adjacent cyclic amino by means of a carbon atom constituting these rings; B represents a phenyl which may have a substituent, a 5-membered or 6-membered heteroaryl ring composed of one to three identical or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom and carbon atoms as ring-constituting atoms, or a heterocondensed ring composed of the heteroaryl ring and either a benzene ring or a 6-membered heteroaryl ring composed of one to two nitrogen atoms and carbon atoms, wherein the heteroaryl ring or the heterocondensed ring may have a substituent and is bonded to the adjacent cyclopropyl ring by means of a carbon atom constituting these rings; R1 and R2, which may be identical or different, each represent a hydrogen atom, a halogen atom, or the like; R3 represents a hydrogen atom, a halogen atom, or the like; n and m, which may be identical or different, each represent 0 or 1; and p represents 1 or 2.

  提供一种新型 T 型钙通道阻滞剂。 由以下通式（I）代表的化合物、该化合物的同系物或立体异构体、该化合物的药学上可接受的盐，或该化合物、同系物、立体异构体或盐的溶液可用作 T 型钙通道阻滞剂。 其中 A 代表可能具有取代基的苯基、由 1 至 3 个相同或不同的杂原子组成的 4 元至 6 元杂芳基环，这些杂原子选自氧原子、硫原子、氮原子和碳原子作为构环原子、或由杂芳基环和苯环或由一至两个氮原子和碳原子组成的 6 元杂芳基环组成的杂缩合环，其中杂芳基环或杂缩合环可具有取代基，并通过构成这些环的碳原子与相邻环状氨基的氮原子键合； B 代表可能具有取代基的苯基、由 1 至 3 个相同或不同的杂原子组成的 5 元或 6 元杂芳基环，这些杂原子选自氧原子、硫原子、氮原子和作为构环原子的碳原子、或由杂芳环和苯环或由一至两个氮原子和碳原子组成的六元杂芳环组成的杂缩合环，其中杂芳环或杂缩合环可具有取代基，并通过构成这些环的碳原子与相邻的环丙基环键合； R1 和 R2 可以相同或不同，各自代表氢原子、卤素原子或类似物； R3 代表氢原子、卤素原子或类似原子； n 和 m 可以相同或不同，各自代表 0 或 1；p 代表 1 或 2。