2-Amino-5-chloro-N-(4-(morpholine-4-sulfonyl)-phenyl)-benzamide | 254877-58-2

• 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: 2-Amino-5-chloro-N-(4-(morpholine-4-sulfonyl)-phenyl)-benzamide
• 英文别名: 2-amino-5-chloro-N-(4-morpholin-4-ylsulfonylphenyl)benzamide
• CAS: 254877-58-2
• 化学式: C₁₇H₁₈ClN₃O₄S
• 分子量: 395.867
• InChiKey: MCDVJJASZBJIHD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-Amino-5-chloro-N-(4-(morpholine-4-sulfonyl)-phenyl)-benzamide 、 2-三氟甲基苯磺酰氯 生成 5-Chloro-N-(4-(morpholine-4-sulfonyl)-phenyl)-2-(2-trifluoromethyl-phenylsulfonylamino)-benzamide
  参考文献：
  名称：

  Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them

  摘要：

  本发明涉及以下式I的化合物，其中A1、A2、R1、R2、R3、X和n如权利要求中所定义，这些化合物是有价值的药用活性化合物，可用于治疗和预防疾病，例如心血管疾病，如高血压、心绞痛、心力衰竭、血栓形成或动脉粥样硬化。式I的化合物能够调节体内环鸟苷酸单磷酸（cGMP）的产生，并且通常适用于治疗和预防与破坏cGMP平衡有关的疾病。此外，本发明还涉及制备式I化合物的方法，它们用于治疗和预防上述疾病以及用于制备用途的药物，以及包含式I化合物的药物制剂。

  公开号：

  US06335334B1
• 作为产物：
  描述：

  5-Chloro-N-(4-(morpholine-4-sulfonyl)-phenyl)-2-nitro-benzamide 在 sodium hydrosulfite 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 1.0h， 以55%的产率得到2-Amino-5-chloro-N-(4-(morpholine-4-sulfonyl)-phenyl)-benzamide
  参考文献：
  名称：

  Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them

  摘要：

  本发明涉及以下式I的化合物，其中A1、A2、R1、R2、R3、X和n如权利要求中所定义，这些化合物是有价值的药用活性化合物，可用于治疗和预防疾病，例如心血管疾病，如高血压、心绞痛、心力衰竭、血栓形成或动脉粥样硬化。式I的化合物能够调节体内环鸟苷酸单磷酸（cGMP）的产生，并且通常适用于治疗和预防与破坏cGMP平衡有关的疾病。此外，本发明还涉及制备式I化合物的方法，它们用于治疗和预防上述疾病以及用于制备用途的药物，以及包含式I化合物的药物制剂。

  公开号：

  US06335334B1

文献信息

• [EN] SULFUR SUBSTITUTED SULFONYLAMINOCARBOXYLIC ACID N-ARYLAMIDES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM<br/>[FR] N-ARYLAMIDES D'ACIDE SULFONYLAMINOCARBOXYLIQUE A SUBSTITUTION SOUFRE, PREPARATION ET UTILISATION DE CES DERNIERS, PREPARATIONS PHARMACEUTIQUES CONTENANT CES COMPOSES
  申请人：HOECHST MARION ROUSSEL DE GMBH

  公开号：WO2000002851A1

  公开（公告）日：2000-01-20

  The present invention relates to compounds of formula (I), wherein A?1, A2, R1, R2, R3¿, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of formula (I) are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of formula (I), to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of formula (I).

  本发明涉及式（I）化合物，其中A1，A2，R1，R2，R3，X和n如权利要求所定义，这些化合物是有价值的药物活性化合物，用于治疗和预防疾病，例如心血管疾病，如高血压，心绞痛，心力衰竭，血栓或动脉硬化。式（I）化合物能够调节体内环磷鸟苷酸（cGMP）的产生，并且通常适用于治疗和预防与cGMP平衡紊乱有关的疾病。本发明还涉及制备式（I）化合物的方法，它们用于治疗和预防上述疾病以及制备药物，以及包含式（I）化合物的制药制剂。
• SULFUR SUBSTITUTED SULFONYLAMINOCARBOXYLIC ACID N-ARYLAMIDES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM
  申请人：SCHINDLER Ursula

  公开号：US20120108573A1

  公开（公告）日：2012-05-03

  The present invention relates to compounds of the formula I wherein A 1 , A 2 , R 1 , R 3 , X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula fare capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.

  本发明涉及公式I的化合物，其中A1、A2、R1、R3、X和n如权利要求中所定义，这些化合物是有价值的药物活性化合物，用于治疗和预防疾病，例如心血管疾病，如高血压、心绞痛、心力衰竭、血栓或动脉硬化。公式F的化合物能够调节体内环磷酸鸟苷单磷酸（cGMP）的产生，通常适用于治疗和预防与扰乱cGMP平衡有关的疾病。本发明还涉及制备公式I化合物的方法，以及它们用于治疗和预防上述疾病和制备药物的用途，以及包含公式I化合物的制药制剂。
• Use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides in the treatment of pain
  申请人：RUDOLPHI Karl

  公开号：US20110021505A1

  公开（公告）日：2011-01-27

  The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R 1 to R 6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.

  本发明涉及使用式I中的磺酰基取代的2-磺酰氨基苯甲酸N-苯基酰胺，其中A和R1至R6具有声明中所示的含义，用于治疗疼痛并制造用于治疗疼痛的药物。
• Sulfur substituted sulfonylaminocarboxylic acid N-heteroarylamides, their preparation, their use and pharmaceutical preparations comprising them
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP1614678A2

  公开（公告）日：2006-01-11

  The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.

  本发明涉及式 I 的化合物 其中 A1、A2、R1、R2、R3、X 和 n 如权利要求书中所定义，是治疗和预防疾病（例如高血压、心绞痛、心功能不全、血栓或动脉粥样硬化等心血管疾病）的有价值的药物活性化合物。式 I 的化合物能够调节体内环磷酸鸟苷（cGMP）的生成，通常适用于治疗和预防与 cGMP 平衡失调有关的疾病。此外，本发明还涉及式 I 化合物的制备工艺、其在治疗和预防上述疾病中的用途以及为此目的制备药物的工艺，以及包含式 I 化合物的药物制剂。
• USE OF SULFONYL-SUBSTITUTED 2-SULFONYLAMINOBENZOIC ACID N-PHENYLAMIDES IN THE TREATMENT OF PAIN
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP2207541A1

  公开（公告）日：2010-07-21