ZY-15850A free acid | 105799-77-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: ZY-15850A free acid
• 英文别名: 4-phenyl-4H-thieno[3,2-c]chromene-2-carboxylic acid
• CAS: 105799-77-7
• 化学式: C₁₈H₁₂O₃S
• 分子量: 308.4
• InChiKey: OKVWPULYXWCZQE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  74.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Tricyclic thieno derivatives, their preparation and pharmaceutical compositions containing them
  申请人：Zyma SA

  公开号：EP0193493A2

  公开（公告）日：1986-09-03

  Pharmaceutical preparations containing compounds of formula I wherein ring A is unsubstituted or substituted, R1 and Rz, independently of one another, each represents hydrogen, lower alkyl, aryl or heteroaryl, or R, and R2 together represent lower alkylene optionally interrupted by oxygen, sulfur or optionally substituted nitrogen, Y is methylene, methylene mono- or disubstituted by lower alkyl, oxygen, sulfur, sulfinyl or sulfonyl, X represents a bivalent radical -S-C[-B-(Z)n]=CH- the sulfur group S of which is bonded directly to the a- or to the β-position of the bicyclic ring system, B denotes a direct bond, alkylene or alkenylene; n is 1 or, in case B is alkylene or alkenylene, may be also 2 or 3; and Z represents free or functionally modified carboxy, masked carboxy that can be cleaved under physiological conditions, free or functionally modified formyl, acyl, free or functionally modified sulfo, free, etherified or esterified hydroxy, free, etherified or oxidised etherified mercapto, unsubstituted or substituted amino, ammonio, nitro or halogen; and novel compounds of formula I are disclosed. The latter are prepared by methods known per se.

  含有式 I 化合物的药物制剂 其中环 A 是未取代的或取代的，R1 和 Rz 各自独立地代表氢、低级烷基、芳基或杂芳基，或 R 和 R2 一起代表任选被氧、硫或任选取代的氮打断的低级亚烷基，Y 是亚甲基、X 代表二价基 -S-C[-B-(Z)n]=CH-，其中的硫基 S 直接键合到双环系统的 a 位或 β 位，B 表示直接键、亚烷基或烯基；n 是 1，如果 B 是亚烷基或烯基，也可以是 2 或 3；以及 Z 代表游离的或功能修饰的羧基、在生理条件下可裂解的掩蔽羧基、游离的或功能修饰的甲酰基、酰基、游离的或功能修饰的磺酰基、游离的、醚化的或酯化的羟基、游离的、醚化的或氧化的醚化巯基、未取代的或取代的氨基、氨基、硝基或卤素。后者是通过本身已知的方法制备的。
• COMPOSITIONS FOR TREATMENT OF CHRONIC INFLAMMATORY DISEASES
  申请人：SHAPIRO, Howard, K.

  公开号：EP0759750A1

  公开（公告）日：1997-03-05
• EP0759750A4
  申请人：——

  公开号：EP0759750A4

  公开（公告）日：1998-05-27
• Compositions and method for treatment of chronic inflammatory diseases
  申请人：Shapiro K. Howard

  公开号：US20050090553A1

  公开（公告）日：2005-04-28

  This invention defines novel compositions that can be used for clinical treatment of a class of chronic inflammatory diseases. Increased generation of carbonyl substances, namely aldehydes and ketones, occurs at sites of chronic inflammation and is common to the etiologies of all of the clinical disorders addressed herein. Such carbonyl substances are cytotoxic and additionally serve to perpetuate and disseminate the inflammatory process. This invention defines use of compositions, the orally administered required primary agents of which are primary amine derivatives of benzoic acid capable of covalently reacting with the carbonyl substances. p-Aminobenzoic acid (or PABA) is an example of the required primary agent of the present invention. PABA has a small molecular weight, is water soluble, has a primary amine group which reacts with carbonyl-containing substances and is tolerated by the body in relatively high dosages for extended periods. The method of the present invention includes administration of a composition comprising: (1) an orally consumed therapeutically effective amount of at least one required primary agent; (2) at least one required previously known medicament co-agent recognized as effective to treat a chronic inflammatory disease addressed herein administered to the mammalian subject via the oral route, other systemic routes of administration or via the topical route; and (3) optionally one or more additional orally consumed co-agent selected from the group consisting of antioxidants, vitamins, metabolites at risk of depletion, sulfhydryl co-agents, co-agents which may facilitate glutathione activity and nonabsorbable primary amine polymeric co-agents, so as to produce an additive or synergistic physiological effect of an anti-inflammatory nature.
• US4797414A
  申请人：——

  公开号：US4797414A

  公开（公告）日：1989-01-10