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:
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:
The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. 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 X and Y each independently represent a direct bond, NH, CH═CH, O, or S; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like, or R3 and R4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.
摘要翻译:本发明提供可用作新型药剂的异喹啉-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,其盐或其衍生物或盐的溶剂合物:其中X和Y各自独立地表示直接键,NH,CH = CH,O ,或S; R 1和R 2各自独立地表示氢原子,卤素原子,氰基,烷基等; R 3和R 4各自独立地表示氢原子,烷基等,或者R 3和R 4一起形成可以在两个碳原子之间桥接到任意位置的亚烷基或亚烯基; l,m和n表示1〜4的整数。
摘要:
The invention relates to an aminostilbazole derivative of the following formula or a hydrate thereof, and a salt thereof. ##STR1## wherein R.sup.1 and R.sup.2 each represents hydrogen etc.; R.sup.3, R.sup.4, R.sup.13, and R.sup.14 each represents hydrogen, C.sub.1-3 acyl, halogen, hydroxy etc.; R.sup.5 represents hydrogen or hydroxy-substituted C.sub.1-3 alkyl etc.; R.sup.6 represents benzenesulfonyl substituted by C.sub.1-3 alkoxy etc.; ring Y represents phenyl etc.; ring Z represents 4-pyridyl, its oxide etc. The compound is useful or the treatment of various malignant tumors.
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:
.omega.-Aminoalkanoic acid arylamides having the formula:R'(CH.sub.2).sub.n CONHRwherein R represents phenyl or naphthyl which can be substituted by halogen, nitro, alkyl, alkoxy, hydroxyl, acetoamino or alkoxycarbonyl; R' represents amino or acylated amino; and n is an integer of 4-8, exhibit blood platelet aggregation inhibiting effects.
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:
The present invention is directed to (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention has less hygroscopicity as compared with (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride anhydrous crystals and thus, exhibits excellent chemical stability.
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.
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.