(S)-4-amino-6-methyl-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)thiochroman-7-carboxamide 1,1-dioxide | 361377-18-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: (S)-4-amino-6-methyl-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)thiochroman-7-carboxamide 1,1-dioxide
• 英文别名: (S)-4-amino-6-methyl-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)thiochromane-7-carboxamide 1,1-dioxide；(4S)-4-amino-6-methyl-1,1-dioxo-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-3,4-dihydro-2H-thiochromene-7-carboxamide
• CAS: 361377-18-6
• 化学式: C₁₈H₁₈N₄O₃S
• 分子量: 370.432
• InChiKey: COXPRQCAGOCGKS-AWEZNQCLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  26
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  126
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Amide compounds and use thereof
  申请人：——

  公开号：US20030158413A1

  公开（公告）日：2003-08-21

  The present invention relates to an amide compound of the formula 1 wherein R 1 is a hydrogen and the like, R 2 is a hydrogen and the like, X is SO 2 and the like, Y is the formula (III) and the like and a is 2, an isomer thereof or pharmaceutically acceptable salts thereof. The compound of the present invention shows a remarkable and selective Rho kinase inhibitory action, is free of problematic toxicity, shows fine oral absorption and drug kinetics (absorption, distribution, metabolism, excretion and the like of the drug), and shows superior properties (e.g., stability etc.) as a compound. Accordingly, it can be used as a therapeutic drug for various diseases in which Rho kinase is involved.

  本发明涉及一种式1的酰胺化合物，其中R1为氢等，R2为氢等，X为SO2等，Y为式（III）等，a为2，其异构体或其药学上可接受的盐。本发明的化合物显示出显著且选择性的Rho激酶抑制作用，不具有有毒性问题，显示出良好的口服吸收和药物动力学（药物的吸收、分布、代谢、排泄等），并且显示出优越的特性（例如稳定性等）作为一种化合物。因此，它可以作为治疗涉及Rho激酶的各种疾病的治疗药物。
• Visual function disorder improving agents
  申请人：——

  公开号：US20040106646A1

  公开（公告）日：2004-06-03

  The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-( 1 H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of a visual function disorder associated with various eye diseases caused by damage, defects, degeneration and the like in the retinal or optic nerve.

  本发明提供了一种含有具有Rho激酶抑制活性的化合物的视觉功能障碍改善剂，特别是(R)-(+)-N-(1H-吡咯[2,3-b]吡啶-4-基)-4-(1-氨基乙基)苯甲酰胺作为有效成分。该剂具有促进视网膜神经节细胞轴突延伸和视神经细胞再生的作用，可用于治疗与视网膜或视神经的损伤、缺陷、退化等引起的各种眼部疾病相关的视觉功能障碍。
• AMIDE COMPOUNDS AND USE THEREOF
  申请人：Mitsubishi Pharma Corporation

  公开号：EP1270570A1

  公开（公告）日：2003-01-02

  The present invention relates to an amide compound of the formula wherein R1 is a hydrogen and the like, R2 is a hydrogen and the like, X is SO2 and the like, Y is the formula (III) and the like and a is 2, an isomer thereof or pharmaceutically acceptable salts thereof. The compound of the present invention shows a remarkable and selective Rho kinase inhibitory action, is free of problematic toxicity, shows fine oral absorption and drug kinetics (absorption, distribution, metabolism, excretion and the like of the drug), and shows superior properties (e.g., stability etc.) as a compound. Accordingly, it can be used as a therapeutic drug for various diseases in which Rho kinase is involved.

  本发明涉及一种如下式的酰胺化合物 其中 R1 为氢等，R2 为氢等，X 为 SO2 等，Y 为式（III）等，a 为 2、其异构体或其药学上可接受的盐。本发明的化合物具有显著和选择性的 Rho 激酶抑制作用，无毒性问题，口服吸收和药物动力学（药物的吸收、分布、代谢、排泄等）良好，并显示出作为化合物的优越性能（如稳定性等）。因此，它可以作为一种治疗药物，用于治疗 Rho 激酶参与的各种疾病。
• VISUAL FUNCTION IMPROVING AGENTS
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP1378247A1

  公开（公告）日：2004-01-07

  The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of a visual function disorder associated with various eye diseases caused by damage, defects, degeneration and the like in the retinal or optic nerve.

  本发明提供了一种视功能紊乱改善剂，其有效成分含有具有 Rho 激酶抑制活性的化合物，特别是(R)-(+)-N-(1H-吡咯并[2,3-b]吡啶-4-基)-4-(1-氨基乙基)苯甲酰胺。这种药剂具有促进视网膜神经节细胞轴突延伸的作用和促进视神经细胞再生的作用，可用于治疗因视网膜或视神经系统损伤、缺损、变性等引起的与各种眼病相关的视觉功能障碍。
• COMBINATION THERAPY FOR PULMONARY ARTERIAL HYPERTENSION
  申请人：ROSCIGNO Robert

  公开号：US20090036465A1

  公开（公告）日：2009-02-05

  Methods for treatment of pulmonary hypertension include administration of a first amount of treprostinil and administration of a second amount of a Rho kinase inhibitor such that the first amount and the second amount form together an amount effective for pulmonary hypertension treatment. Kits for treatment pulmonary hypertension are also disclosed.