10H-phenothiazine-2-carbothioamide | 95708-16-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 英文名称: 10H-phenothiazine-2-carbothioamide
• CAS: 95708-16-0
• 化学式: C₁₃H₁₀N₂S₂
• 分子量: 258.368
• InChiKey: HEURGSITSQEMFD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  95.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  10H-phenothiazine-2-carbothioamide 、 碘甲烷 以 丙酮 为溶剂， 反应 15.0h， 以85%的产率得到Methyl 10H-phenothiazine-2-carbimidothioate hydroiodide
  参考文献：
  名称：

  AMIDINE DERIVATIVES AND THEIR APPLICATIONS AS A MEDICAMENT

  摘要：

  这项发明涉及一般式（I）的胍衍生物，其具有钙蛋白酶的抑制活性和/或氧化反应活性的捕捉活性。

  公开号：

  US20090018120A1
• 作为产物：
  描述：

  10H-吩噻嗪-2-羧酸酰胺 在 劳森试剂 、 吡啶 作用下， 以 1,4-二氧六环 为溶剂， 反应 1.5h， 生成 10H-phenothiazine-2-carbothioamide
  参考文献：
  名称：

  Heterocyclic compounds and their use as medicines

  摘要：

  本发明涉及一种新的杂环衍生物，具有对卡尔帕因的抑制活性和/或对反应性氧化物种的捕获活性，其化学式中A、X、Y、R1、R2和Het代表可变基团。本发明还涉及它们的制备方法，含有它们的药物制剂以及它们作为治疗目的的用途，特别是作为卡尔帕因的抑制剂和/或对反应性氧化物种的陷阱，有选择性或非选择性地使用。

  公开号：

  US06747024B1

文献信息

• COMPOSITION CONTAINING AMIDINE DERIVATIVES OR CARBOXAMIDE DERIVATIVES AND STEROIDS, AS A MEDICAMENT
  申请人：Pignol Bernadette

  公开号：US20090149430A1

  公开（公告）日：2009-06-11

  The present invention relates to a composition containing at least one amidine derivative or carboxamide derivative of general formula (I) or (A) in combination with at least one compound chosen from steroids, corticoids or corticosteroids, wherein said composition is suitable for the preparation of a medicament.

  本发明涉及一种含有至少一种氨基甲酸酰胺衍生物或一般式(I)或(A)的羧酰胺衍生物的组合物，与至少一种来自类固醇、皮质类固醇或皮质类固醇的化合物结合在一起，所述组合物适用于制备药物。
• Heterocyclic compounds and their use as medicines
  申请人：Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)

  公开号：US06747024B1

  公开（公告）日：2004-06-08

  The present invention relates to new heterocyclic derivatives having an inhibitory activity on calpains and/or a trapping activity on reactive oxygen species, of formula in which A, X, Y, R1, R2 and Het represent variable groups. The invention also relates to their preparation methods, the pharmaceutical preparations containing them and their use for therapeutic purposes, in particular as inhibitors of calpains and/or traps of reactive oxygen species, selectively or non-selectively.

  本发明涉及一种新的杂环衍生物，具有对卡尔帕因的抑制活性和/或对反应性氧化物种的捕获活性，其化学式中A、X、Y、R1、R2和Het代表可变基团。本发明还涉及它们的制备方法，含有它们的药物制剂以及它们作为治疗目的的用途，特别是作为卡尔帕因的抑制剂和/或对反应性氧化物种的陷阱，有选择性或非选择性地使用。
• Phenothiazine derivatives, their preparation and pharmaceutical
  申请人：Rhone-Poulenc Sante

  公开号：US04985419A1

  公开（公告）日：1991-01-15

  Phenothiazine derivatives of formula: ##STR1## in which Y is hydrogen or halogen, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl, cycloalkyl-alkyl, hydroxyalkyl or acetyloxyalkyl radicals or form, together with the nitrogen atom to which they are attached, an optionally substituted, saturated or partially unsaturated 4- to 7-membered heterocycle; and either X is oxygen, sulphur or: N-R.sub.4, R is cycloalkyl, phenyl or --CH.sub.2 R.sub.3, R.sub.3 is H, alkyl (1 to 5 C), alkenyl or alkynyl (2 to 4 C), cycloalkyl (3 to 6 C), phenyl, substituted phenyl or a heterocyclic radical, R.sub.4 is H or --CN, except that X is not oxygen if, simultaneously, R.sub.3 is H or alkyl, R.sub.1 and R.sub.2 are alkyl or NR.sub.1 R.sub.2 forms an unsubstituted heterocycle, and Y is H; or X is: N-R.sub.4 and R.sub.4 forms, with R and the neighbouring atoms, an optionally substituted imidazolyl or imidazolinyl radical or a hexahydrobenzimidazolyl radical, in their isomeric forms and mixtures thereof and their acid addition salts are useful as analgesics and diuretics.

  公式为：##STR1## 其中Y为氢或卤素，R.sub.1和R.sub.2可以相同也可以不同，表示烷基，环烷基-烷基，羟基烷基或醋氧基烷基基团，或者与它们所连接的氮原子一起形成一个可选的取代的饱和或部分不饱和的4-至7-成员杂环；而X为氧、硫或：N-R.sub.4，R为环烷基、苯基或--CH.sub.2 R.sub.3，R.sub.3为H、烷基（1至5个碳）、烯基或炔基（2至4个碳）、环烷基（3至6个碳）、苯基、取代苯基或杂环基，R.sub.4为H或--CN，但如果同时R.sub.3为H或烷基，R.sub.1和R.sub.2为烷基或NR.sub.1 R.sub.2形成未取代的杂环，则X不为氧，Y为H；或X为：N-R.sub.4，R.sub.4与R和相邻原子一起形成可选的取代咪唑基或咪唑啉基基团或六氢苯并咪唑基基团，它们的异构体和混合物及其酸加合物可用作镇痛剂和利尿剂。
• Heterocyclic compounds and their use as medicaments
  申请人：SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIEQUES (S.C.R.A.S.)

  公开号：US20040180936A1

  公开（公告）日：2004-09-16

  The present invention relates to new heterocyclic derivatives having an inhibitory activity on calpains and/or a trapping activity on reactive oxygen species, of formula 1 in which A, X, Y, R1, R 2 and Het represent variable groups. The invention also relates to their preparation methods, the pharmaceutical preparations containing them and their use for therapeutic purposes, in particular as inhibitors of calpains and/or traps of reactive oxygen species, selectively or non-selectively.

  本发明涉及一种具有对钙蛋白酶的抑制活性和/或对反应性氧化物的捕获活性的新杂环衍生物，其化学式为1，其中A、X、Y、R1、R2和Het表示可变基团。本发明还涉及它们的制备方法、含有它们的药物制剂以及它们的治疗用途，特别是作为钙蛋白酶的抑制剂和/或反应性氧化物的捕获剂，具有选择性或非选择性。
• Composition containing amidine derivatives or carboxamide derivatives and steroids, as a medicament
  申请人：Pignol Bernadette

  公开号：US08642591B2

  公开（公告）日：2014-02-04

  The present invention relates to a composition containing at least one amidine derivative or carboxamide derivative of general formula (I) or (A) in combination with at least one compound chosen from steroids, corticoids or corticosteroids, wherein said composition is suitable for the preparation of a medicament.

  本发明涉及一种组合物，其包含至少一种通式(I)或(A)的脲衍生物或羧酰胺衍生物，以及至少一种来自类固醇、皮质激素或类固醇激素的化合物，其中所述组合物适用于制备药物。