H1152

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: H1152
• 英文别名: HMN-1152；(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazine；4-methyl-5-[(2-methyl-1,4-diazepan-1-yl)sulfonyl]isoquinoline
• 化学式: C₁₆H₂₁N₃O₂S
• 分子量: 319.428
• InChiKey: AWDORCFLUJZUQS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  70.7
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• ISOQUINOLINESULFONAMIDE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
  申请人：Hidaka, Hiroyoshi

  公开号：EP1074545A1

  公开（公告）日：2001-02-07

  This invention relates to isoquinolinesulfonamide derivatives represented by the following formula (1): wherein A represents a linear or branched alkylene group, R1 represents a hydrogen atom, an hydroxyl, alkoxy or alkyl group or the like, R2 represents a hydrogen atom, an alkyl group or the like, R3 represents a hydrogen atom, an alkyl group or the like, and R4 and R5 may be the same or different and individually represent hydrogen atoms or lower alkyl groups; N-oxides and salts thereof; and solvates thereof. This invention is also concerned with pharmaceutical compositions, which contain the derivatives, N-oxides, salts, or solvates. These derivatives, N-oxides, salts, and solvates have viral proliferation inhibiting activities and are useful as AIDS therapeutics.

  本发明涉及下式（1）所代表的异喹啉磺酰胺衍生物： 其中 A 代表直链或支链亚烷基，R1 代表氢原子、羟基、烷氧基或烷基或类似基团，R2 代表氢原子、烷基或类似基团，R3 代表氢原子、烷基或类似基团，R4 和 R5 可以相同或不同，且各自代表氢原子或低级烷基；其 N-氧化物和盐；以及其溶解物。本发明还涉及含有这些衍生物、N-氧化物、盐或溶液的药物组合物。这些衍生物、N-氧化物、盐和溶液具有抑制病毒增殖的活性，可用作艾滋病治疗药物。
• REMEDY FOR GLAUCOMA COMPRISING Rho KINASE INHIBITOR AND PROSTAGLANDINS
  申请人：SANTEN PHARMACEUTICAL CO., LTD.

  公开号：EP1541151A1

  公开（公告）日：2005-06-15

  A subject of the present invention is to find utility of a combination of a Rho kinase inhibitor and prostaglandins as a therapeutic agent for glaucoma. Actions of reducing intraocular pressure are complemented and/or enhanced each other by combining the Rho kinase inhibitor with prostaglandins. For the administration mode, each drug can be administered in combination or in mixture.

  本发明的一个主题是发现 Rho 激酶抑制剂和前列腺素的组合作为青光眼治疗剂的效用。通过将 Rho 激酶抑制剂与前列腺素结合使用，可相互补充和/或增强降低眼内压的作用。在给药方式上，每种药物可以联合给药，也可以混合给药。
• REMEDY FOR GLAUCOMA COMPRISING Rho KINASE INHIBITOR AND &bgr;-BLOCKER
  申请人：SANTEN PHARMACEUTICAL CO., LTD.

  公开号：EP1568382A1

  公开（公告）日：2005-08-31

  A subject of the present invention is to find utility of a co mbination of a Rho kinase inhibitor having a novel action and a β-blocker as a therapeutic agent for glaucoma. Actions of reduci ng intraocular pressure are complemented and/or enhanced each other by combining the Rho kinase inhibitor with the β-blocker. For the administration mode, each drug can be administered in combination or in mixture.

  本发明的一个主题是发现一种具有新作用的 Rho 激酶抑制剂和一种 β-受体阻滞剂的组合作为青光眼治疗剂的效用。通过将 Rho 激酶抑制剂和 β-受体阻滞剂联合使用，降低眼内压的作用可以相互补充和/或增强。在给药方式上，每种药物可以联合给药，也可以混合给药。
• Rho/Rock/PI3/Akt kinase inhibitors for the treatment of diseases associated with protozoan parasites.
  申请人：UNIVERSITE PIERRE ET MARIE CURIE (PARIS VI)

  公开号：EP1891958A1

  公开（公告）日：2008-02-27

  The present invention relates to the use of a Rho/ROCK/Pl3K/Akt pathway modulator for the manufacture of a medicament intended for the prevention or the treatment of pathologies associated with an infection by a protozoan parasite.

  本发明涉及使用 Rho/ROCK/Pl3K/Akt 通路调节剂制造用于预防或治疗与原生动物寄生虫感染有关的病症的药物。
• Therapeutic agent for glaucoma comprising rho kinase inhibitor and prostaglandin
  申请人：Santen Pharmaceutical Co., Ltd

  公开号：EP2314299A1

  公开（公告）日：2011-04-27

  A subject of the present invention is to find utility of a combination of a Rho kinase inhibitor and prostaglandins as a therapeutic agent for glaucoma. Actions of reducing intraocular pressure are complemented and/or enhanced each other by combining the Rho kinase inhibitor with prostaglandins. For the administration mode, each drug can be administered in combination or in mixture.

  本发明的一个主题是发现 Rho 激酶抑制剂和前列腺素的组合作为青光眼治疗剂的效用。通过将 Rho 激酶抑制剂与前列腺素结合使用，可相互补充和/或增强降低眼内压的作用。在给药方式上，每种药物可以联合给药，也可以混合给药。