trans-2-Methyl-cyclohexylamin

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: trans-2-Methyl-cyclohexylamin
• 英文别名: (2R)-2-methylcyclohexan-1-amine
• 化学式: C₇H₁₅N
• 分子量: 113.203
• InChiKey: FEUISMYEFPANSS-ULUSZKPHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  8
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  trans-2-Methyl-cyclohexylamin 、 4-chloro-5-(pyridin-2-ylethynyl)-1H-pyrrolo[2,3-b]pyridine 在 tris-(dibenzylideneacetone)dipalladium(0) 、 sodium t-butanolate 、 1,3-双(2,6-二异丙基苯基)氯化咪唑鎓 作用下， 以 1,4-二氧六环 为溶剂， 以41%的产率得到N-((2R)-2-methylcyclohexyl)-5-(pyridin-2-ylethynyl)-1H-pyrrolo[2,3-b]pyridin-4-amine
  参考文献：
  名称：

  一种二吡咯并吡啶结构的化合物、制备方法和医药用途

  摘要：

  本发明公开了一种二吡咯并吡啶结构的化合物、制备方法和医药用途。本发明提供的二吡咯并吡啶结构的化合物对JAK家族蛋白具有明显的抑制活性，为有效的JAK抑制剂，因此具备开发成抑制JAK进而治疗疾病的药物的前景。

  公开号：

  CN113292561A

文献信息

• 2-AMINOBENZAMIDE DERIVATIVE
  申请人：Astellas Pharma Inc.

  公开号：EP1955697A1

  公开（公告）日：2008-08-13

  To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.

  提供一种基于对辣椒素受体 VR1 激活的抑制作用，用于治疗或预防痛觉痛、神经病 理痛、癌痛、头痛、膀胱功能紊乱等的新型优良制剂。 本发明是通过确认一种苯甲酰胺衍生物，其特征在于该衍生物具有一个苯环，在该苯环中，一个单环缩合在氨基基团的氮原子上，并且在所述氨基基团的邻近位置上具有一个被环基取代的低级烷基氨基或氨基，该衍生物对 VR1 的活化具有很强的抑制作用，并在此基础上具有很好的药理作用，并发现该衍生物可以成为治疗或预防 VR1 相关疾病（如痛觉疼痛）的一种很好的药物、神经性疼痛、癌痛、头痛、膀胱功能紊乱等。
• NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
  申请人：FUJIFILM Corporation

  公开号：EP2589592A1

  公开（公告）日：2013-05-08

  An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl g roup, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R4 and R5 e ach independently represent a hydrogen atom; and R2 and R4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.

  本发明的目的是提供一种化合物和药物组合物，其具有优异的抑制 Syk 的活性。本发明提供了一种烟酰胺衍生物，由以下式（I）表示 其中 R1 代表卤素原子；R2 代表 C1-12 烷基、C2-12 烯基、C2-12 炔基、C3-8 环烷基、芳基、ar-C1-6 烷基或杂环基，每个基团可选择具有至少一个取代基；R3 代表芳基或杂环基，每个基团可选择具有至少一个取代基；以及 R4 和 R5 分别独立地代表一个氢原子；R2 和 R4 可与它们结合的氮原子一起形成一个环状氨基，该氨基可选择具有至少一个取代基）或其盐，以及一种用于治疗 Syk 相关疾病的药物组合物，该药物组合物包含烟酰胺衍生物或其盐。
• 4,6,7-TRISUBSTITUTED 1,2-DIHYDROPYRROL[3,4-C]PYRIDIN/PYRIMIDIN-3-ONE DERIVATIVE AND USE
  申请人：Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

  公开号：EP3689871A1

  公开（公告）日：2020-08-05

  The present disclosure relates to 4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives, and their preparations and medicinal use. Specifically, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof, wherein the definition of each group is as described in the specification and claims.

  本公开涉及4,6,7-三取代的1,2-二氢吡咯并[3,4-c]吡啶/嘧啶-3-酮衍生物及其制剂和药用。具体地说，本公开公开了式(I)化合物或其药学上可接受的盐、立体异构体、溶媒或原药及其制备方法和用途，其中各组的定义如说明书和权利要求书中所述。
• Benzopyrazole compound used as RHO kinase inhibitor
  申请人：MEDSHINE DISCOVERY INC.

  公开号：US11345678B2

  公开（公告）日：2022-05-31

  The invention relates to a benzopyrazole compound used as RHO kinase inhibitor, a pharmaceutical composition and uses thereof for preparing an RHO kinase inhibiting drug, and more specifically to said compound of formula (I-1), a pharmaceutically acceptable salt and isomer thereof.

  本发明涉及一种用作 RHO 激酶抑制剂的苯并吡唑化合物、制备 RHO 激酶抑制药物的药物组合物及其用途，更具体地说，涉及所述式（I-1）化合物、其药学上可接受的盐和异构体。
• 2,4,6-TRIAMINO-1,3,5-TRIAZINE DERIVATIVE
  申请人：Astellas Pharma Inc.

  公开号：EP1479397B1

  公开（公告）日：2011-06-08