摘要:
2-(Phenylmethylene)cycloalkylamines of the formula wherein the cycloalkyl ring is cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl and R is hydrogen, C 1-3 alkyl of 4-alkylenedioxy when n is 2; R a and R b are each hydrogen or hydrocarbyl or NR 2 is optionally substituted azetidino. These compounds, and their acid addition salts, can have analgesic and anti-depressant activity.
摘要:
Compounds of formula I and pharmaceutically acceptable salts thereof; in which R, and R 2 , which are the same or different, are H or an optionally substituted hydrocarbon group or R, and R 2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;
R 3 is an optionally substituted aromatic hydrocarbon group; and R 4 is a hydrocarbon group containing at least one substituent selected from the group consisting of hydroxy and acylated derivatives thereof, optionally substituted alkoxy groups, optionally substituted cycloalkyloxy groups, optionally substituted alkylenedioxy groups, oxo and groups of formula S(O) p R 5 in which p is 0, 1 or 2 and R 5 is an alkyl group, said hydrocarbon group being optionally substituted by additional substituents, are useful in the treatment of depression.
in which n = 0 or 1; in which, when n = 0, R 1 is H, an alkyl, a cycloalkyl, a cycloalkylmethyl, an alkenyl or, an alkynyl group a heterocyclic ring or an optionally substituted phenyl ring or when n = 1, R 1 is H or an alkyl group; in which R 2 and R 3 are H or an alkyl group; in which A is a group of formula III
in which W is an oxygen atom or a group of formula -S(O) m -, a group of formula -CR 12 R 13 -, a cycloalkylidene group or a cycloalkylene group; x is 0 or an integer from 1 to 5; y is 0 or an integer from 1 to 5. in which R 4 is a carbocyclic ring, a heterocyclic ring, a cyano group, a carbamoyl group, an alkoxycarbonyl group, an amido group, an acyloxy group, a hydroxy group, a thiol group, or a group of formula -OR 20 , -SR 20 , -SOR 20 or SO 2 R 20 . in which R 5 , R 6 and R 7 are H, halo, trifluoromethyl, hydroxy, an alkyl group, an alkoxy or alkylthio group, phenyl or R 5 and R 6 , together with the carbon atoms to which they are attached, form an optionally substituted second benzene ring; in which R 8 and R 9 are H or an alkyl group containing 1 to 3 carbon atoms; and pharmaceutically acceptable salts thereof have utility in the treatment of depression. Processes for their preparation and compositions containing them are disclosed.
摘要:
Naphthalene derivatives of the formula: wherein R 1 is hydrogen atom or a lower alkoxycarbonyl and R 2 is a lower alkoxycarbonyl, or R' and R 2 are combined together to form a group of the formula: each of R 3 and R 4 is a lower alkoxy, or one of R 3 and R 4 is hydrogen atom and the other is a lower alkoxy, and Ring A is a substituted or unsubstituted benzene ring, and a pharmaceutically acceptable salt thereof are disclosed. Said naphthalene derivative (I) and its salt have excellent hypolipidemic activity and are useful for treatment or prophylaxis of hyperlipidemia and/or arteriosclerosis. Disclosed are also a process for the production of compounds of formula (I), the use of said compounds and the production of medicaments and pharmaceutical compositions containing compounds of formula (1) as active ingredient.
摘要:
57 Acetylene compounds of the formula (I): wherein Y, R 1 , R,, R 3 , and R 4 are as described herein, m is 0-3, n is 0-2 and Ar is pehnyl or an aromatic heterocycle are disclosed. The compounds possess antihypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.
摘要:
57 Acetylene compounds of the formula (I): wherein Y, R 1 , R,, R 3 , and R 4 are as described herein, m is 0-3, n is 0-2 and Ar is pehnyl or an aromatic heterocycle are disclosed. The compounds possess antihypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.