丙替嗪酸 | 13799-03-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 中文名称: 丙替嗪酸
• 中文别名: 甲吩噻嗪丙酸；2-(7-甲氧基-10-甲基吩噻嗪-2-基)丙酸；甲嗪丙酸
• 英文名称: 7-methoxy-α,10-dimethyl-10H-phenothiazine-2-acetic acid
• 英文别名: protizinic acid；PRT062607；PRT；2-(7-methoxy-10-methyl-10H-phenothiazin-2-yl)-propionic acid；2-(7-methoxy-10-methylphenothiazin-2-yl)propanoic acid
• CAS: 13799-03-6
• 化学式: C₁₇H₁₇NO₃S
• 分子量: 315.393
• InChiKey: VSQMKHNDXWGCDB-UHFFFAOYSA-N

物化性质

• 熔点：
  124-125 °C
• 沸点：
  524.6±50.0 °C(Predicted)
• 密度：
  1.285±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  75.1
• 氢给体数：
  1
• 氢受体数：
  5

安全信息

• 海关编码：
  2934300000

制备方法与用途

普罗替尼酸是一种口服活性的非甾体抗炎药，具备抗炎和解热的作用。它能够抑制磷脂酶A2（PLA2）的活性，其IC50值为210微摩尔。

文献信息

• Kappa agonist compounds and pharmaceutical formulations thereof
  申请人：——

  公开号：US20030144272A1

  公开（公告）日：2003-07-31

  Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae I, II, IIA, III, IIIA, IIIB, IIIB-i, IV and IVA have the structure: 1 2 wherein R 1 , R 2 , R 3 , R 4 ; and X, X 4 , X 5 , X 7 , X 9 ; Y, Z and n are as described in the specification.

  提供具有kappa阿片受体激动剂活性的化合物，含有这些化合物的组合物以及使用它们作为镇痛剂的方法。 具有以下结构的化合物I、II、IIA、III、IIIA、IIIB、IIIB-i、IV和IVA： 1 2 其中 R 1 ，R 2 ，R 3 ，R 4 ；和 X，X 4 ，X 5 ，X 7 ，X 9 ； Y，Z和n如规范中所述。
• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
  申请人：Cerulean Pharma Inc.

  公开号：US20130196906A1

  公开（公告）日：2013-08-01

  Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of a disease or disorder, e.g., autoimmune disease, inflammatory disease, central nervous system disorder, cardiovascular disease, or metabolic disorder. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.

  提供了关于使用CDP-治疗剂偶联物治疗疾病或紊乱的方法，例如自身免疫疾病、炎症性疾病、中枢神经系统紊乱、心血管疾病或代谢紊乱。还提供了CDP-治疗剂偶联物、包含CDP-治疗剂偶联物的颗粒以及包含CDP-治疗剂偶联物的组合物。
• [EN] ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS<br/>[FR] ANTI-INFECTIEUX A BASE D'ISOTHIAZOLOQUINOLONES ET DE SELS CORRESPONDANTS
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2005019228A1

  公开（公告）日：2005-03-03

  The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

  本发明提供了具有抗菌活性的公式(I)和公式(II)的化合物及盐类：本发明还提供了用于制造公式(I)和公式(II)化合物的新的合成中间体。变量A1、R2、R3、R5、R6、R7、A8和R9在此文中定义。本文披露的某些公式(I)和公式(II)化合物是细菌DNA合成和细菌复制的强效和选择性抑制剂。本发明还提供了含有一种或多种公式(I)或公式(II)化合物以及一种或多种载体、辅料或稀释剂的抗菌组合物，包括药物组合物。这样的组合物可以只含有公式(I)或公式(II)的化合物作为唯一的活性成分，也可以含有公式(I)或公式(II)的化合物与一种或多种其他活性成分的组合。本发明还提供了用于治疗动物微生物感染的方法。
• DIAZENIUMDIOLATED NON-STEROIDAL ANTI-INFLAMMATORY DRUGS, COMPOSITIONS THEREOF, AND RELATED METHODS
  申请人：Velázquez Carlos A.

  公开号：US20090186859A1

  公开（公告）日：2009-07-23

  Disclosed are compounds that release nitric oxide, e.g., a compound of Formula (I) wherein R 1-10 , X, and n are as described herein, which are NSAID derivatives comprising a diazeniumdiolate moiety N 2 O 2 − . The compounds are chemopreventive agents with gastric-sparing, analgesic, cardioprotective, and/or anti-inflammatory properties. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed is a method of preventing or treating cancer or treating inflammation or an inflammation-related condition in a mammal comprising administering an effective amount of a compound of the invention to the mammal.

  披露了释放一氧化氮的化合物，例如，式(I)的化合物，其中R1-10、X和n如本文所述，这些化合物是非甾体抗炎药（NSAID）衍生物，包含亚硝基二醇基团N2O2−。这些化合物是具有胃保护、镇痛、心脏保护和/或抗炎特性的化学预防剂。还披露了一种药物组合物，包括本发明的化合物和药用载体。还披露了一种预防或治疗癌症或治疗炎症或炎症相关状况的方法，包括向哺乳动物施用本发明的化合物的有效量。
• HYDROGEN SULFIDE DERIVATIVES OF NON-STEROIDAL ANTI-INFLAMMATORY DRUGS
  申请人：WALLACE JOHN

  公开号：US20080004245A1

  公开（公告）日：2008-01-03

  The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H 2 S) releasing moiety to produce novel anti-inflammatory compounds having reduced side effects.

  本发明涉及具有改善的抗炎性质的非甾体抗炎药（NSAIDs）衍生物，用于治疗炎症、疼痛和发热。更具体地说，非甾体抗炎药与释放硫化氢（H2S）的基团结合，以产生具有减少副作用的新的抗炎化合物。