5-chlorothiosalicylic acid

• 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: 5-chlorothiosalicylic acid
• 英文别名: 5-chloro-2-hydroxybenzenecarbothioic S-acid
• 化学式: C₇H₅ClO₂S
• 分子量: 188.635
• InChiKey: PEFTZKTUWHPLQV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  38.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-chlorothiosalicylic acid 、 alpha-氯乙酰苯 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 生成 2-phenacylthio-5-chlorobenzoic acid
  参考文献：
  名称：

  Substituted benzoic acid hypolipemic agents

  摘要：

  多取代苯甲酸及其在哺乳动物中作为降血脂剂的应用。

  公开号：

  US03953595A1
• 作为产物：
  描述：

  methyl-5-chlorothiosalicylate 生成 5-chlorothiosalicylic acid
  参考文献：
  名称：

  Benzothiophenes and benzofurans and antiallergic use thereof

  摘要：

  描述了具有抗过敏活性的新型苯并噻吩和苯并呋喃衍生物，以及其制备方法、药物组合物和使用方法。该公开内容描述了衍生物的用途，用于预防嗜碱细胞和肥大细胞释放组胺和白三烯等介质，并防止中性粒细胞的呼吸爆发，提供在心血管疾病以及抗炎、银屑病和抗偏头痛治疗中有用的活性。

  公开号：

  US04703053A1

文献信息

• Anti-inflammatory and analgesic 3-hydroxybenzo[b]thiophene derivatives,
  申请人：Merck & Co., Inc.

  公开号：US04663344A1

  公开（公告）日：1987-05-05

  3-Hydroxybenzo[b]thiophene derivatives, such as 2-aralkyl, 2-alkyl and 2-alkenyl-3-hydroxybenzo[b]-thiophenes, were prepared by, among other methods, ring closure of 2-(2-carboxy-phenylthio)-.alpha.-substituted acetic acids. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory diseases and other prostaglandin and/or leukotriene mediated diseases.

  3-羟基苯并[b]噻吩衍生物，如2-芳基、2-烷基和2-烯基-3-羟基苯并[b]噻吩，可通过多种方法制备，其中包括2-(2-羧基苯硫基)-α-取代乙酸的环闭合。这些化合物被发现在治疗疼痛、发热、炎症、关节炎、哮喘、过敏性疾病、皮肤病、心血管疾病、牛皮癣、炎症性疾病和其他前列腺素和/或白三烯介导的疾病中具有用处。
• Non-malignant disease treatment with Ras antagonists
  申请人：Kloog Yoel

  公开号：US20050119237A1

  公开（公告）日：2005-06-02

  Disclosed is a method for inhibiting Ras-induced or mediated proliferation of cells associated with a non-malignant disease, disorder or pathological condition. The method entails administering to a patient a Ras antagonist in an amount effective to inhibit the proliferation. The invention is particularly applicable to diseases characterized by a proliferation of T-cells such as autoimmune disease, e.g., type 1 diabetes, lupus and multiple sclerosis, and pathological states such as graft rejection induced by the presentation of a foreign antigen such as a graft in response to a disease condition (e.g., kidney failure). Other non-malignant diseases characterized by proliferations of cells include cirrhosis of the liver and restenosis. Preferred Ras antagonists are S-trans-trans farnesylthiosalicylic acid (FTS) and structurally related compounds (or analogs) thereof.

  本发明公开了一种抑制与非恶性疾病、失调或病理状态相关的细胞Ras诱导或介导增殖的方法。该方法包括向患者施用有效量的Ras拮抗剂以抑制增殖。本发明特别适用于由T细胞增殖所特征的疾病，例如自身免疫疾病，例如1型糖尿病、狼疮和多发性硬化症，以及由疾病状态（例如肾衰竭）对外来抗原（例如移植物）的呈现引起的移植排斥等病理状态。其他由细胞增殖所特征的非恶性疾病包括肝硬化和再狭窄。首选的Ras拮抗剂是S-转-转-法尼基硫酸水杨酸（FTS）及其结构相关化合物（或类似物）。
• Spiro compounds, process for their preparation and pharmaceutical compositions containing them
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0026000A1

  公开（公告）日：1981-04-01

  Newspirocompoundsoftheformula: wherein n is an integer of 1 to 4, and X is halogen, lower alkyl, nitro, amino which may be substituted, hydroxyl which may be substituted, acyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may be substituted, sulfamoyl which may be substituted, lower alkylthio or lower alkylsulfonyl, or two of X at the 5- and 6-positions together form -CH=CH-CH=CH-, exhibit inhibitory activity to thrombocyte aggregation and are useful for the prophylaxis or treatment of cardiovascular disturbance such as thrombosis.

  式中 n 为 1 至 4 的整数，X 为卤素、低级烷基、硝基、可被取代的氨基、可被取代的羟基、酰基、羧基、低级烷氧基羰基、可被取代的氨基甲酰基、可被取代的氨基磺酰基、低级烷硫基或低级烷基磺酰基，或位于 5 位和 6 位的两个 X 共同形成-CH=CH-CH=CH-，具有抑制血小板聚集的活性，可用于预防或治疗血栓等心血管疾病。
• Benzothiophenes and benzofurans having antiallergic activity
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP0187487A1

  公开（公告）日：1986-07-16

  There is disclosed a compound having the following general formula (I) or a pharmaceutically acceptable salt thereof, wherein: R', R4, and R5 are each, independently, H, an alkyl having from one to twelve carbon atoms, an alkoxy having from one to twelve carbon atoms, a hydroxy, an aryl, a nitro group, an amino group, a substituted amino group, a mercapto radical, an alkylthio radical having from one to four carbon atoms, an alkylsulphinyl radical having from one to four carbon atoms, an alkylsulphonyl radical having from one to four carbon atoms, an arylthio radical, an arylsulphinyl radical, an arylsulphony radical or a halogen, R1 being further chosen from a methylenedioxy radical attached to adjacent carbon atoms of the benzene ring; R2 is an alkoxy having from one to twelve carbon atoms, an arylmethoxy, an amino group, a substituted amino group, a mercapto group, an alkylthio having from one to four carbon atoms, an alkylsulphinyl having from one to four carbon atoms, an alkylsulphonyl having from one to four carbon atoms, an arylthio, an arylsulphinyl, or an arylsulphonyl; and R3 is A or B X is oxygen or S(O)q wherein q is zero, one, or two. Also disclosed is a process for preparing the compounds, compositions comprising the compounds and pharmaceutical uses of the compounds. The novel benzothiophene and benzofuran derivatives have antiallergic activity. The disclosure describes the use of derivatives for prevention of the release of mediators including histamine and leukotrienes from basophils and mast cells, and prevent respiratory burst in neutrophils providing activity useful in cardiovascular disorders as well as in antiinflammatory, psoriasis, and antimigraine treatment.

  本发明公开了具有以下通式（I）的化合物 或其药学上可接受的盐，其中 R'、R4 和 R5 各自独立地为 H、具有 1 至 12 个碳原子的烷基、具有 1 至 12 个碳原子的烷氧基、羟基、芳基、硝基、氨基、取代氨基、巯基、具有 1 至 4 个碳原子的烷硫基R1是连接到苯环相邻碳原子上的亚甲基二氧基，R2是具有一至四个碳原子的烷氧基，R3是具有一至四个碳原子的亚甲基二氧基，R4是具有一至四个碳原子的亚甲基二氧基，R5是具有一至四个碳原子的亚甲基二氧基，R6是具有一至四个碳原子的亚甲基二氧基，R7是具有一至四个碳原子的亚甲基二氧基，R8是具有一至四个碳原子的亚甲基二氧基，R9是具有一至四个碳原子的亚甲基二氧基； R2 是具有一至十二个碳原子的烷氧基、芳基甲氧基、氨基、取代氨基、巯基、具有一至四个碳原子的烷硫基、具有一至四个碳原子的烷基亚砜基、具有一至四个碳原子的烷基磺酰基、芳基硫基、芳基亚砜基或芳基磺酰基；和 R3 是 A 或 B X 是氧或 S(O)q，其中 q 为 0、1 或 2。 还公开了制备这些化合物的工艺、包含这些化合物的组合物以及这些化合物的药物用途。 新型苯并噻吩和苯并呋喃衍生物具有抗过敏活性。该公开描述了这些衍生物在防止嗜碱性粒细胞和肥大细胞释放包括组胺和白三烯在内的介质，以及防止中性粒细胞呼吸爆发方面的用途，其活性可用于心血管疾病以及抗炎、牛皮癣和抗偏头痛治疗。
• Inhibitors of leukotriene A4 hydrolase
  申请人：CELTAXSYS, INC.

  公开号：US10399986B2

  公开（公告）日：2019-09-03

  The present invention is directed to compounds encompassed by the Formula (I): pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.

  本发明涉及式 (I) 所包含的化合物： 其药物组合物、抑制LTA-4水解酶的方法，以及治疗通过抑制LTA4h活性而得到改善的疾病和紊乱的方法。此类疾病和病症的非限制性实例包括炎症性和自身免疫性疾病和病症。