Highly selective rho-kinase inhibitor
    1.
    发明申请
    Highly selective rho-kinase inhibitor 审中-公开
    高选择性rho激酶抑制剂

    公开(公告)号:US20090306053A1

    公开(公告)日:2009-12-10

    申请号:US11919176

    申请日:2006-04-24

    摘要: The present invention relates to a compound having a highly selective Rho-kinase inhibiting activity and being useful as a therapeutic agent for a disease such as hypertension, pulmonary hypertension, cerebral vasospasm, cardiac angina, cardiac failure, arteriosclerosis, glaucoma, dysuria, asthma, or erectile dysfunction, and a drug containing the compound.Provided is a homopiperazine derivative represented by General Formula (1), an acid addition salt thereof, or a solvate of the derivative or the salt: (wherein R1 represents an amino acid residue; R2 represents a hydrogen atom or an alkyl group; R3 represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogen atom, a nitrile group, or a hydroxyl group; and R4 represents a hydrogen atom, a halogen atom, or a hydroxyl group).

    摘要翻译: 本发明涉及具有高选择性Rho-激酶抑制活性的化合物,可用作高血压,肺动脉高压,脑血管痉挛,心绞痛,心力衰竭,动脉硬化,青光眼,排尿困难,哮喘等疾病的治疗剂。 或勃起功能障碍,以及含有该化合物的药物。 本发明提供通式(1)表示的高哌嗪衍生物,其酸加成盐或其衍生物或盐的溶剂化物:其中,R1表示氨基酸残基,R2表示氢原子或烷基,R3表示 氢原子,烷基,烯基,炔基,烷氧基,卤素原子,腈基或羟基; R4表示氢原子,卤素原子或羟基)。

    4-haloisoquinoline derivative and drug containing the same
    2.
    发明申请
    4-haloisoquinoline derivative and drug containing the same 审中-公开
    4-卤代异喹啉衍生物和含有它们的药物

    公开(公告)号:US20070088021A1

    公开(公告)日:2007-04-19

    申请号:US11518141

    申请日:2006-09-11

    IPC分类号: A61K31/551

    CPC分类号: A61K31/551 C07D401/12

    摘要: The present invention relates to compounds which have a potent Rho-kinase inhibitory action and which are useful as therapeutic agents for treating diseases, such as hypertension, pulmonary hypertension, cerebral vasospasm, angina pectoris, cardiac failure, arteriosclerosis, glaucoma, dysuria, asthma, and erectile failure, and drugs containing the compounds. The present invention provides a 4-haloisoquinoline derivative represented by formula (1): an acid-added salt thereof, or a solvate of any of the foregoing, in which X is halogen, such as fluoro, chloro, bromo and iodo.

    摘要翻译: 本发明涉及具有强Rho激酶抑制作用的化合物,其可用作治疗疾病的治疗剂,例如高血压,肺动脉高压,脑血管痉挛,心绞痛,心力衰竭,动脉硬化,青光眼,排尿困难,哮喘, 和勃起功能障碍,以及含有化合物的药物。 本发明提供由式(1)表示的4-卤代异喹啉衍生物:其酸加成盐,或上述任何一种的溶剂合物,其中X为卤素,如氟,氯,溴和碘。

    6-Quinazolinesulfonyl derivatives and process for preparation thereof
    5.
    发明授权
    6-Quinazolinesulfonyl derivatives and process for preparation thereof 失效
    6-喹唑啉磺酰基衍生物及其制备方法

    公开(公告)号:US4510307A

    公开(公告)日:1985-04-09

    申请号:US293192

    申请日:1981-08-17

    摘要: A 6-quinazolinesulfonyl derivative of Formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or a C.sub.1-12 alkyl group:R.sub.2 is a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.4-10 cycloalkyl group, an aryl group or an aralkyl group; andR.sub.1 and R.sub.2 may be linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring together with the adjacent nitrogen atom; andR.sub.3 is a ##STR2## group wherein R.sub.4 is a C.sub.1-8 alkyl group; a --HN(CH.sub.2).sub.n NH.sub.2 group wherein n is an integer of 2 to 10; or a ##STR3## group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.

    摘要翻译: 式(I)的6-喹唑啉磺酰基衍生物:其中R1是氢原子或C1-12烷基:R2是氢原子,C1-12烷基,C4-10环烷基 ,芳基或芳烷基; R1和R2可以直接或通过氧原子连接,与相邻的氮原子一起形成5-至7-元杂环; 并且R 3是一个基团,其中R 4是C 1-8烷基; 其中n为2〜10的整数的-HN(CH 2)n NH 2基; 或组 及其药学上可接受的盐; 及其制备方法。 本发明的化合物对于血管平滑肌具有松弛作用,并且可用作血管扩张剂和低血压。

    Substituted isoquinoline derivative
    7.
    发明授权
    Substituted isoquinoline derivative 有权
    取代的异喹啉衍生物

    公开(公告)号:US08883792B2

    公开(公告)日:2014-11-11

    申请号:US13995300

    申请日:2011-12-21

    摘要: The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R1 and R2 each independently represent a hydrogen atom, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like; R5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms.

    摘要翻译: 本发明提供了可用作药物的新型异喹啉-6-磺酰胺衍生物。 本发明提供由式(1)表示的异喹啉-6-磺酰胺衍生物,其盐或衍生物或其盐的溶剂合物,其中R1和R2各自独立地表示氢原子等; R3和R4各自独立地表示氢原子,烷基等; R5表示氢原子,任选取代的烷基,任选取代的烯基,任选取代的炔基,任选取代的环烷基,任选取代的烷酰基等; A表示碳原子数2〜6的直链或支链亚烷基。

    Isoquinolinesulfonamide derivatives
    9.
    发明授权
    Isoquinolinesulfonamide derivatives 失效
    异喹啉磺酰胺衍生物

    公开(公告)号:US4709032A

    公开(公告)日:1987-11-24

    申请号:US919774

    申请日:1986-10-17

    摘要: This invention relates to novel isoquinolinesulfonamide derivatives of Formula (I): ##STR1## wherein A is a C.sub.0-10 alkylene group or a C.sub.0-10 alkylene group having a C.sub.1-10 alkyl group, a phenyl group, a substituted phenyl group or a phenylalkyl group; R.sub.1 and R.sub.2 each is a hydrogen atom; or R.sub.1 and R.sub.2 are linked directly to form an ethylene group unsubstituted or substituted with a C.sub.1-4 alkyl group;R.sub.3 and R.sub.4 each is a hydrogen atom, a C.sub.1-6 alkyl group or linked directly to form a C.sub.2-6 alkylene group; and the pharmaceutically acceptable acid addition salt thereof, and to a process for preparing them. The isoquinoline derivatives possess a relaxatory action for vascular smooth muscle and action for increasing blood flow and are useful as a vasodilator and a hypotensor.

    Substituted isoquinolinesulfonyl compounds
    10.
    发明授权
    Substituted isoquinolinesulfonyl compounds 失效
    取代的异喹啉磺酰基化合物

    公开(公告)号:US4678783A

    公开(公告)日:1987-07-07

    申请号:US813973

    申请日:1985-12-27

    摘要: An isoquinolinesulfonyl compound represented by the formula (I): ##STR1## wherein R.sup.1 : H, Cl, OHA : unsubstituted or substituted ethylene or alkyleneR.sup.2, R.sup.3 : H, alkyl, jointly forming unsubstituted or substituted ethylene or trimethyleneR.sup.4 : H, alkyl, amidinoor an acid salt thereof.They can be prepared, for example, by converting 1-R.sup.1 substituted-5-isoquinolinesulfonic acid to the corresponding sulfonyl chloride and subsequently reacting the chloride with a compound of formula ##STR2## They can be advantageously utilized as vasodilator, cerebral circulation ameliorator, antihypertensive agent and drugs for prevention and treatment of various circulatory organ diseases.

    摘要翻译: 由式(I)表示的异喹啉磺酰化合物:其中R1:H,Cl,OHA:未取代或取代的亚乙基或亚烷基R2,R3:H,烷基,共同形成未取代或取代的乙烯或三亚甲基R4 :H,烷基,脒基或其酸式盐。 它们可以例如通过将1-R1取代-5-异喹啉磺酸转化成相应的磺酰氯并随后使氯化物与式的化合物反应来制备。它们可以有利地用作血管扩张剂,脑循环改善剂,抗高血压药 用于预防和治疗各种循环器官疾病的药剂和药物。