5-(1,4-Diazepan-1-ylsulfonyl)-4-methylisoquinoline;dihydrochloride

• 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: 5-(1,4-Diazepan-1-ylsulfonyl)-4-methylisoquinoline;dihydrochloride
• 化学式: C15H21Cl2N3O2S
• 分子量: 378.3
• InChiKey: WPITZCCQSIFELD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.37
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  70.7
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Preventives/remedies for kidney diseases
  申请人：——

  公开号：US20030096843A1

  公开（公告）日：2003-05-22

  A compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)-cyclohexane, has a renal interstitial fibrosis inhibitory action in renal interstitial fibrosis model mice and various other actions, and therefore, is useful as an agent for the prophylaxis or treatment of renal diseases.

  具有Rho激酶抑制活性的化合物，例如（+）-trans-4-(1-氨乙基)-1-(4-吡啶基氨甲酰基)-环己烷，对于肾间质纤维化模型小鼠具有肾间质纤维化抑制作用和其他各种作用，因此，可用作预防或治疗肾脏疾病的药物。
• Antitumor effect potentiators
  申请人：——

  公开号：US20030165576A1

  公开（公告）日：2003-09-04

  When used concurrently with an antitumor agent, a compound having a Rho kinase inhibitory activity, such as (R)-(+)-N-(4-pyridyl)-4-(1-aminoethyl)benzamide, reinforces an antitumor effect of the antitumor agent and is useful as an antitumor effect potentiator. Particularly, a compound having a Rho kinase inhibitory activity used with an antitumor agent in combination can reduce the dose of the antitumor agent, which in turn affords provision of a sufficient effect and/or reduction of side effects.

  当与抗肿瘤药物同时使用时，具有Rho激酶抑制活性的化合物，如(R)-(+)-N-(4-吡啶基)-4-(1-氨乙基)苯甲酰胺，可以增强抗肿瘤药物的抗肿瘤效果，并且可用作抗肿瘤效应增强剂。特别是，与抗肿瘤药物联合使用具有Rho激酶抑制活性的化合物可以降低抗肿瘤药物的剂量，从而提供足够的疗效和/或减少副作用。
• 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。
• ISOQUINOLINE DERIVATIVES AND DRUGS
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0885888A1

  公开（公告）日：1998-12-23

  The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof, wherein R1 represents alkyl, alkenyl, alkynyl, alkoxy, hydroxy, cyano, or halogen; R2 represents hydrogen, hydroxy, or halogen; R3 represents hydrogen, alkyl, or amidino; Ring A represents a 5 to 11-membered cyclic amino group which may be substituted, which cyclic amino group may be bridged between two carbon atoms in optional positions. The compound of this invention is useful for the prevention or treatment of cerebral tissue impairment due to the vasospasm following cerebral hemorrhage.

  本发明涉及下式通式[I]的化合物或其药用盐或其溶液、 其中 R1 代表烷基、烯基、炔基、烷氧基、羟基、氰基或卤素；R2 代表氢、羟基或卤素；R3 代表氢、烷基或脒基；环 A 代表可被取代的 5 至 11 元环氨基，该环氨基可在任选位置的两个碳原子之间桥接。 本发明的化合物可用于预防或治疗脑出血后血管痉挛引起的脑组织损伤。
• 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。