摘要:
3-Substituted-1,2-benzisoxazole derivative of the following formula: ##SPC1##Wherein R.sub.1 is hydrogen, hydroxy, nitro, alkyl, alkoxy, halogen or amino; R.sub.2 is hydroxyamino, amino, hydrazino, mono- or di- alkyl substituted amino, aralkylamino, acyloxyamino, morpholino, piperazine which is unsubstituted or substituted with alkyl, aralkyl or aryl at 4 position, or pyrrolidino, or R.sub.2 may combine with imino group and form together with the adjacent carbon atom a heterocyclic ring such as imidazoline or tetrahydropyrimidine; and n is an integer of 0 to 3, and its pharmaceutically acceptable acid addition salt, and preparation thereof. The present compounds show valuable pharmacological properties, such as anti-reserpine activity, central nervous depressing activity, anti-hypertensive activity and l-dopa potentiating activity.
摘要:
1,2-Diphenylethanolamine derivatives of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are each hydrogen, a halogen, nitro, hydroxy, an alkyl or methoxy; R.sub.3 is a group of the formula: ##SPC2##Wherein R.sub.4, R.sub.5 and R.sub.6 are each hydrogen, a halogen or methoxy and n is an integer of 0 to 3, or a pyridyl; and Z is hydroxy or an acyloxy; with proviso that when R.sub.1 and/or R.sub.2 are hydroxy, Z is hydroxy, and their pharmaceutically acceptable salts, which have excellent analgesic and anti-tussive activities, and a process for the preparation thereof.
摘要:
1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##SPC1##Wherein X is hydroxy, methoxy, methyl or trifluoromethyl; and R is an unsubstituted monocycloalkyl group having 6 to 8 carbon atoms or 2-methoxyphenyl; provided that when X is hydroxy, R is cyclohexyl, and when X is trifluoromethyl, R is 2-methoxyphenyl,And their pharmaceutically acceptable salts, which have excellent analgesic, anti-tussive and anti-inflammatory activities, without undesirable side effect such as narcotic activity, and a process for the preparation thereof.
摘要:
1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.
摘要:
The present invention relates to compounds represented by the general formula (I): ##STR1## wherein R.sub.1 is H or methoxy, R.sub.2 is H, methoxy, OH or F, R.sub.3 is H or F, R.sub.4 is H or F at 7-, 8- or 9-position, and .circle.Ar is a benzene, thiophene or pyridine ring, provided that (i) at least two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, (ii) R.sub.2 or R.sub.3 is F when R.sub.4 is F, (iii) R.sub.1, R.sub.3 and R.sub.4 are H when R.sub.2 is methoxy or OH, (iv) R.sub.2 and R.sub.3 are not simultaneously F, and (v) R.sub.2 and R.sub.3 are H or F, and both R.sub.1 and R.sub.4 are H when .circle.Ar is a thiophene or pyridine ring, or a physiologically acceptable acid addition salt thereof. The compounds of the present invention have an excellent protective effect against cerebral anoxia and some of them have also an inhibitory effect on lipid peroxidation of mitochondrial membrane of brain and an anti-convulsant activity and are useful as an agent for prevention or treatment of cerebral diseases caused by hypoxia in mammals including human.
摘要:
Methane-sulfonamide derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 and R.sub.3 are the same or different and are each hydrogen or a straight or branched alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group: --CH.sub.2 SO.sub.2 NR.sub.2 R.sub.3 is bonded to the carbon atom of either of X and Y,and an alkali metal salt thereof, and a process for the preparation of said methane-sulfonamide derivatives. Said compounds have an excellent anticonvulsant activity and are useful as anticonvulsants for controlling convulsions and seizures in patients with epilepsy.
摘要翻译:下式的甲磺酰胺衍生物:其中R 1是氢或卤素原子,R 2和R 3相同或不同,各自为氢或具有1至3个碳原子的直链或支链烷基, 的X和Y是碳原子,另一个是氮原子,条件是:-CH 2 SO 2 NR 2 R 3基团与X和Y中的任一个的碳原子键合,及其碱金属盐,以及制备所述 甲磺酰胺衍生物。 所述化合物具有优异的抗惊厥活性,可用作控制癫痫患者惊厥和癫痫发作的抗惊厥药。
摘要:
1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.
摘要:
Novel acetic acid derivatives of the formula: ##STR1## wherein X is oxygen or sulfur; R.sub.1 is hydrogen or a lower alkyl; R.sub.2 is hydroxy, an alkoxy, an alkenyloxy, a cycloalkyloxy, an aryloxy, a substituted aryloxy, an aryl-lower alkoxy, a substituted aryl-lower alkoxy, an aryl-lower alkenyloxy, a substituted aryl-lower alkenyloxy, an .omega.-disubstituted amino-lower alkoxy, a lower alkoxycrbonyl-lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group ##STR2## wherein R.sub.3 is hydrogen, hydroxy, a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy-lower alkyl, R.sub.4 is hydrogen, a lower alkyl or a hydroxy-lower alkyl, or the R.sub.3 and R.sub.4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group --CH(R.sub.1)COR.sub.2 is joined to the carbon atom at 2- or 3-position, and pharmaceutically acceptable salts thereof, processes for their preparation, and pharmaceutical compositions containing these compounds. They have excellent anti-inflammatory, analgesic and antipyretic activities with weak ulcerogenicity in the gastrointestinal tract and toxicity.
摘要:
Hexahydro-.gamma.-carboline derivatives of the formula: ##SPC1##Wherein R.sub.1 is methyl or ethyl, and R.sub.2 is hydrogen, methyl or ethyl, with proviso that when R.sub.1 is ethyl, R.sub.2 is hydrogen, and their pharmaceutically acceptable acid addition salts, which exhibit excellent psychotropic effect, and a process for the preparation thereof.
摘要:
Compounds of the formula: ##STR1## wherein A means an alkylene; Y--Z means ##STR2## --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or ##STR3## R.sub.1 and R.sub.2 are each a substituent; R.sub.3 is hydrogen atom, alkyl, or alkoxy; R.sub.4 is phenyl, phenylalkyl, phenylalkenyl, diphenylmethyl, naphthyl, thiazolyl, optionally substituted pyridyl, optionally substituted pyrimidinyl, quinolyl, benzoylalkyl, benzoyl, furoyl, thenoyl, phenyloxycarbonyl, phenyloxysulfonyl, or phenylsulfonyl; a is 2 or 3, b and c are each 1 or 2, and d is an integer of 0 to 2, provided that the phenyl, phenyl moiety and naphthyl may optionally be substituted, and a pharmaceutically acceptable salt thereof, process for the preparation thereof, and pharmaceutical composition containing the same. The compounds and salt thereof show potent calcium antagonistic activity and are useful for prophylaxis and treatment of hypertension and/or ischemic heart disease.