2-氯-4-(甲基氨基)-苯甲酸 | 3975-62-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 2-氯-4-(甲基氨基)-苯甲酸
• 英文名称: 2-Chlor-4-methylamino-benzoesaeure
• 英文别名: 2-chloro-4-methylamino-benzoic acid；2-Chloro-4-(methylamino)benzoic acid
• CAS: 3975-62-0
• 化学式: C₈H₈ClNO₂
• 分子量: 185.61
• InChiKey: SELSOKMSAZQJOJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE<br/>[FR] DÉRIVÉS DE PIPÉRIDINE EN TANT QU'AGONISTES DES RÉCEPTEURS BÊTA X DU FOIE, COMPOSITIONS ET UTILISATION ASSOCIÉES
  申请人：MERCK SHARP & DOHME

  公开号：WO2018068296A1

  公开（公告）日：2018-04-19

  Piperidine compounds of the Formular: (I) and pharmaceutically acceptable salts thereof, wherein X, Y, R 1, R 2, R 3, L, R 4, L 1, Q and R 5 are as defined herein. The compounds and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

  吡啶类化合物的化学式：(I)及其药用可接受盐，其中X、Y、R1、R2、R3、L、R4、L1、Q和R5的定义如本文所述。这些化合物及包含其化合物的药用可接受组合物可用作肝X-β受体（LXRβ）激动剂，可能用于治疗或预防与之相关的病理。这些病理包括但不限于炎症性疾病和胆固醇和脂质代谢缺陷所特征的疾病，例如阿尔茨海默病。
• [EN] AZAINDOLE DERIVATIVES AS TYROSINE KINASE INHIBITORS<br/>[FR] DÉRIVÉS AZA-INDOLIQUES UTILISÉS COMME INHIBITEURS DE TYROSINE KINASES
  申请人：PRINCIPIA BIOPHARMA INC

  公开号：WO2012158785A1

  公开（公告）日：2012-11-22

  The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.

  本公开提供了一些化合物和药用盐，它们是酪氨酸激酶抑制剂，特别是BLK、BMX、EGFR、HER2、HER4、ITK、JAK3、TEC、Btk和TXK，因此适用于治疗通过抑制酪氨酸激酶治疗的疾病，如癌症和炎症性疾病（如关节炎等）。还提供了含有这些化合物和药用盐的药物组合物，以及制备这些化合物和药用盐的过程。
• Therapeutic agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient
  申请人：Akada Yasushige

  公开号：US20060040985A1

  公开（公告）日：2006-02-23

  An agent for preventing/treating respiratory diseases contains, as an active ingredient, a compound represented by following Formula (I): wherein A is a group represented by L-W [wherein L is a bond or CH 2 ; and W is O, SOn (wherein n is 0 to 2), or —NR 7 — (wherein R 7 is hydrogen or lower alkyl)]; each of G 1 and G 2 is (CH 2 )r (wherein r is 0 to 2), provided that when n is 1, G 1 and G 2 may be bridged by lower alkylene; Y is a lower alkylene or (substituted) benzylidene; Z is a bond or O, provided that when Z is a bond, Y may form a 5- or 6-membered ring with carbon on the benzene ring; R 1 is, for example, NO 2 , a lower alkoxycarbonyl, (substituted) carbamoyl, (protected) hydroxyl group, (protected) carboxyl, or (protected) N-hydroxycarbamoyl; each of R 2 and R 3 is hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy or NO 2 ; each of R 4 and R 5 is, for example, hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy, CN, or lower alkylsulfonyl; and R 6 is hydrogen or lower alkyl, a salt thereof or a solvate of them. It has excellent antitussive activity when used as an agent for preventing/treating respiratory diseases such as lung cancer, common cold syndrome, pulmonary tuberculosis, pneumonia, acute bronchitis or chronic bronchitis.

  一种用于预防/治疗呼吸系统疾病的药剂，其活性成分为以下式(I)所表示的化合物：其中A是由L-W表示的基团[其中L是键或CH2; W是O，SO n（其中n为0至2），或—NR7—（其中R7是氢或较低烷基）]；G1和G2分别为(CH2)r（其中r为0至2），但当n为1时，G1和G2可以由较低的烷基桥接；Y是较低的烷基或（取代的）苯甲亚基；Z是键或O，但当Z为键时，Y可以与苯环上的碳形成5-或6-成员环；R1为NO2、较低的烷氧羰基、（取代的）氨基甲酰基、（保护的）羟基、（保护的）羧基或（保护的）N-羟基氨基甲酰基；R2和R3分别为氢、卤素、（卤代的）较低烷基、（卤代的）较低烷氧基或NO2；R4和R5分别为氢、卤素、（卤代的）较低烷基、（卤代的）较低烷氧基、CN或较低烷基磺酰基；R6为氢或较低烷基，其盐或溶剂也可以使用。当用作预防/治疗肺癌、普通感冒综合症、肺结核、肺炎、急性支气管炎或慢性支气管炎等呼吸系统疾病的药剂时，具有优异的止咳活性。
• AZAINDOLE DERIVATIVES AS TYROSINE KINASE INHIBITORS
  申请人：Principia Biopharma Inc.

  公开号：US20140073626A1

  公开（公告）日：2014-03-13

  The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.

  本公开提供了一些化合物和药学上可接受的盐，它们是酪氨酸激酶抑制剂，特别是BLK，BMX，EGFR，HER2，HER4，ITK，JAK3，TEC，Btk和TXK，因此可用于治疗通过抑制酪氨酸激酶治疗的疾病，例如癌症和炎症性疾病，如关节炎等。还提供了含有这些化合物和药学上可接受的盐的药物组合物和制备这些化合物和药学上可接受的盐的方法。
• [EN] DIHYDROPYRIMIDINE COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF<br/>[FR] COMPOSÉ DE DIHYDROPYRIMIDINE, SON PROCÉDÉ DE PRÉPARATION ET SON APPLICATION<br/>[ZH] 一种二氢嘧啶类化合物、其制备方法及应用
  申请人：SHANGHAI VISONPHARMA CO LTD

  公开号：WO2022121844A1

  公开（公告）日：2022-06-16

  公开了一种二氢嘧啶类化合物、其制备方法及应用。提供了一种如式I所示的二氢嘧啶类化合物或其药学上可接受的盐。该二氢嘧啶类化合物具有较好的抗HBV活性、以及较低的细胞毒性，可用于制备治疗和/或预防HBV感染的药物。