(4-bromo-2,6-dimethylphenyl)hydrazine hydrochloride | 174826-34-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (4-bromo-2,6-dimethylphenyl)hydrazine hydrochloride
• 英文别名: (4-bromo-2,6-dimethylphenyl)hydrazine;hydrochloride
• CAS: 174826-34-7
• 化学式: C₈H₁₁BrN₂*ClH
• 分子量: 251.554
• InChiKey: SZTXNGAWBPIHMK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.77
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  38
• 氢给体数：
  3
• 氢受体数：
  2

安全信息

• 储存条件：
  2-8°C

反应信息

• 作为反应物：
  描述：

  (4-bromo-2,6-dimethylphenyl)hydrazine hydrochloride 在 tris-(dibenzylideneacetone)dipalladium(0) 、 三丁基膦 、 水 、 potassium hydroxide 、 1,1'-azodicarbonyl-dipiperidine 、 2-二-叔丁膦基-2',4',6'-三异丙基联苯 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲醇 、 水 为溶剂， 反应 58.0h， 生成 N-[4-[(1S)-1-[3,5-二甲基-4-[4-(三氟甲基)-1H-吡唑-1-基]苯氧基]丁基]苯甲酰基]-beta-丙氨酸
  参考文献：
  名称：

  The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus

  摘要：

  A novel and potent small molecule glucagon receptor antagonist for the treatment of diabetes mellitus is reported. This candidate, (S)-3-[4-(1-{3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy}butyl)benzamido]propanoic acid, has lower molecular weight and lipophilicity than historical glucagon receptor antagonists, resulting in excellent selectivity in broad-panel screening, lower cytotoxicity, and excellent overall in vivo safety in early pre-clinical testing. Additionally, it displays low in vivo clearance and excellent oral bioavailability in both rats and dogs. In a rat glucagon challenge model, it was shown to reduce the glucagon-elicited glucose excursion in a dose-dependent manner and at a concentration consistent with its rat in vitro potency. Its properties make it an excellent candidate for further investigation. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2013.03.014
• 作为产物：
  描述：

  4-溴-2,6-二甲基苯胺 在 盐酸 、 sodium nitrite 、 tin(ll) chloride 作用下， 以 水 为溶剂， 反应 19.5h， 以61%的产率得到(4-bromo-2,6-dimethylphenyl)hydrazine hydrochloride
  参考文献：
  名称：

  羧酸类衍生物、其制备方法及其在医药上的用途

  摘要：

  本发明涉及一种羧酸类衍生物、其制备方法及其在医药上的应用。具体而言，本发明涉及一种通式(I)所示的羧酸类衍生物、其制备方法及其可药用的盐，以及它们作为治疗剂，特别是作为胰高血糖受体拮抗剂的用途，其中通式(I)中的各取代基的定义与说明书中的定义相同。

  公开号：

  CN107759522B

文献信息

• GLUCAGON RECEPTOR MODULATORS
  申请人：Aspnes Gary Erik

  公开号：US20120202834A1

  公开（公告）日：2012-08-09

  The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R 1 , R 2 , R 3 , A 1 , A 2 , A 3 , A 4 , L, B 1 , B 2 , B 3 and B 4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

  本发明提供了一种式（I）的化合物或其药学上可接受的盐，其中R1、R2、R3、A1、A2、A3、A4、L、B1、B2、B3和B4如本文所定义。已发现式I的化合物可作为葡萄糖胰高血糖素拮抗剂或逆向激动剂。因此，式I的化合物及其药物组成物对于治疗由葡萄糖胰高血糖素介导的疾病、紊乱或症状是有用的。
• METAL COMPLEX AND LIGHT EMITTING DEVICE USING THE SAME
  申请人：Sumitomo Chemical Company, Limited

  公开号：US20170166599A1

  公开（公告）日：2017-06-15

  Provided is a metal complex excellent in light emission stability. The metal complex is represented by the formula (1): wherein M represents an iridium atom or the like, n 1 represents an integer of 1 to 3, n 2 represents an integer of 0 to 2, E 2 to E 4 represent a nitrogen atom or a carbon atom where two selected from among E 2 to E 4 are nitrogen atoms and the remaining one is a carbon atom, R 1 represents an aryl group or the like, R 2 and R 3 represent a hydrogen atom, an alkyl group, an aryl group or the like, the ring B represents a triazole ring, the ring A represents an aromatic hydrocarbon ring or the like, and A 1 -G 1 -A 2 represents an anionic bidentate ligand.

  提供的是一种在发光稳定性方面表现出色的金属配合物。该金属配合物由以下式表示：其中M代表铱原子或类似物，n1代表1到3的整数，n2代表0到2的整数，E2到E4代表氮原子或碳原子，其中E2到E4中选取两个为氮原子，另一个为碳原子，R1代表芳基或类似物，R2和R3代表氢原子、烷基、芳基或类似物，环B代表三唑环，环A代表芳香烃环或类似物，A1-G1-A2代表一个阴离子双齿配体。
• COMPOSITION AND LIGHT-EMITTING DEVICE USING THE SAME
  申请人：Sumitomo Chemical Company, Limited

  公开号：US20180354978A1

  公开（公告）日：2018-12-13

  A composition containing phosphorescent compounds represented by formula (1) and formula (2) are provided. M 1 and M 2 each represent an iridium atom, n 1 and n 3 each denote an integer of 1 or more; n and n 4 each denote an integer of 0 or more, n 1 +n 2 and n 3 +n 4 are each 2 or 3, E L represents a hydrogen atom or a nitrogen atom, R 2 represents an aromatic hydrocarbon ring, E 1 , E 2 , E 11A , and E 12A represent a nitrogen atom, R 11A , R 12A , and R 13A represent an aryl group, ring L 1 represents a 6-membered aromatic heterocyclic ring, ring L 2 represents an aromatic hydrocarbon ring, at least ring L 1 or ring L 2 has a group represented by formula (1-T), A 1 -G 1 -A 2 and A 3 -G 2 -A 4 each represent an anionic bidentate ligand, A 1 , A 2 , A 3 and A 4 each represent a nitrogen atom, G 1 and G 2 each represent a single bond, and R 1T represents an alkyl group. —R 1T (1-T)

  提供了一个包含磷光化合物的组合物，其表示为公式（1）和公式（2）。M1和M2分别代表一个铱原子，n1和n3分别表示大于或等于1的整数；n和n4分别表示大于或等于0的整数，n1+n2和n3+n4分别为2或3，EL代表一个氢原子或一个氮原子，R2代表一个芳香烃环，E1、E2、E11A和E12A代表一个氮原子，R11A、R12A和R13A代表一个芳基团，环L1代表一个6元芳香杂环，环L2代表一个芳香烃环，至少环L1或环L2具有一个由公式（1-T）表示的基团，A1-G1-A2和A3-G2-A4分别代表一个阴离子双齿配体，A1、A2、A3和A4分别代表一个氮原子，G1和G2分别代表一个单键，R1T代表一个烷基团。—R1T(1-T)
• Substituted pyrazoles as corticotropin-releasing factor (CRF) antagonists
  申请人：Pfizer Inc.

  公开号：US05968944A1

  公开（公告）日：1999-10-19

  The compounds of the formula wherein A, R.sub.1, R.sub.3, X.sub.1, Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.

  该公式中的化合物，其中A，R.sub.1，R.sub.3，X.sub.1，Y和Z的定义如本文所述，具有促肾上腺皮质激素释放因子（CRF）拮抗剂活性。它们在治疗由CRF引起的疾病，如压力和焦虑相关障碍方面非常有用。
• Glucagon receptor modulators
  申请人：Pfizer Inc.

  公开号：US08859591B2

  公开（公告）日：2014-10-14

  The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

  本发明提供了公式（I）的化合物或其药学上可接受的盐，其中R1、R2、R3、A1、A2、A3、A4、L、B1、B2、B3和B4的定义如本文所述。发现公式I的化合物可作为胰高血糖素拮抗剂或反向激动剂。因此，公式I的化合物及其药物组合物对于治疗由胰高血糖素介导的疾病、疾病或病况是有用的。