摘要:
2-Propanol derivatives of the formula: ##SPC1##And their pharmaceutically acceptable acid addition salts, which are useful as medicaments and can be produced by reacting a compound of the formula: A-CH.sub.2 -Z with a compound of the formula: A'-H [wherein R is hydrogen or lower alkanoyl; R.sub.1 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; W is oxygen, sulfur, sulfinyl or sulfonyl; Y is a group of either one of the formulae: ##SPC2##(wherein R.sub.2 is hydrogen, halogen, lower alkyl or lower alkoxy and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl); A and A' are each a group of either one of the formulae: ##SPC3##(wherein R.sub.1, W and Y are each as defined above), provided that A and A' are different each other; and Z is a group of either one of the formulae: ##EQU1## (wherein X is halogen, alkylsulfonyloxy or arylsulfonyloxy and R is as defined above)].
摘要:
A 3-benzazocine compound of the formula: ##SPC1##Wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.8 are each hydrogen or lower alkyl, R.sub.2 is hydrogen, lower alkyl or phenyl and R.sub.6 and R.sub.7 are each lower alkyl, and its pharmaceutically acceptable acid addition salts, which are useful as analgesics and can be produced by reacting a tetrahydropyridine compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each as defined above or its salt with a Lewis acid.
摘要:
Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or halogen and R.sup.3 is hydrogen or methyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are each as defined above or their non-toxic salts, or by condensation of the corresponding compounds of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each defined above, and X is a conventional interchangeable group such as halogen or sulfonyloxy with methylamine or dimethylamine.
摘要:
Novel compounds of the formula: ##STR1## wherein R is a hydrogen or fluorine atom, W is an oxygen atom or an ethylenedioxy or ethylenedithio group and Z is a certain secondary amino group, which are useful as central nervous system depressants, can be prepared by the reaction of a compound of the formula: ##STR2## wherein X is a halogen atom and R and W are each as defined above with a secondary amine of the formula: H--Z wherein Z is as defined above, in case of W being ethylenedioxy or ethylenedithio, optionally followed by hydrolysis and can be reduced to give a compound of the formula: ##STR3## wherein R and Z are each as defined above, which are useful as antipsychotic and/or analgesic agents.
摘要:
Indolylacetic acid derivatives, which have excellent anti-inflammatory, antipyretic and analgesic activities, represented by the formula, ##STR1## wherein X.sub.1 and X.sub.2 are each methylene; A is an unsubstituted ethylenically unsaturated hydrocarbon chain having up to 5 carbon atoms; m is 0 or 1; n is 1 or 2; R.sub.3 is alkyl having up to 4 carbon atoms; cycloalkyl having 3 to 7 carbon atoms, unsubstituted or C.sub.1 -C.sub.4 alkyl-, nitro-, trifluoromethyl-, methylenedioxy-, ethylenedioxy- or halogen-substituted phenyl, or halogen-, C.sub.1 -C.sub.4 alkyl- or phenyl-substituted or benzene ring-condensed C.sub.3 -C.sub.7 cycloalkyl, or unsubstituted or halogen-, C.sub.1 -C.sub.4 alkyl- or phenyl-substituted or benzene ring-condensed C.sub.5 -C.sub.6 cycloalkenyl; and B is ##STR2## .
摘要:
Novel butyrophenone derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydroxyl group or ##STR2## (wherein R.sub.6 and R.sub.7 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.2 represents an optionally substituted phenyl group or ##STR3## (wherein R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.4 represents a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group, R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group, R.sub.10 represents a hydrogen atom or an acyl group represented by R.sub.3 CO- (wherein R.sub.3 is a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group) and Z represents two hydrogen atoms or an oxygen atom, provided that when Z is an oxygen atom and R.sub.1 is ##STR4## R.sub.10 can not be a hydrogen atom, and their acid addition salts, which are useful as central and autonomic nervous system depressants.
摘要:
A 3-phenoxypropylamine derivative of the formula: ##SPC1##Wherein Y is ##SPC2##(wherein R.sub.1 is a halogen atom or a trifluoromethyl group) or ##SPC3##(wherein R.sub.2 is a lower alkyl group) and its pharmaceutically acceptable salts which are useful as central nervous system depressing agents.
摘要:
Ortho-acylated anilide derivatives represented by the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each C.sub.1 - .sub.3 alkyl, and n is 1 or 2, and salts thereof.
摘要:
Novel olefinic aryl ketone compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1.sub.-4 alkyl, or C.sub.1.sub.-4 alkoxy, R.sup.2 is hydrogen or halogen, and R.sup.3 and R.sup.4 are each hydrogen, halogen, C.sub.1.sub.-4 alkyl or trifluoromethyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reaction of an acetylenic alcohol of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, with formaldehyde and an amine of the formula: ##STR3## wherein R.sup.3 and R.sup.4 are each as defined above; reduction of the resultant acetylenic aryl alcohol; and oxidation of the resultant olefinic aryl alcohol.
摘要:
Phenoxypropylamine derivatives of the formula: ##STR1## (in which R.sub.2 is a halogen atom or a trifluoromethyl group) and R.sub.1 is a halogen atom or a C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkenyl group, and their pharmaceutically acceptable salts, which are useful as neuroleptic agents and can be prepared by reacting a compound of the formula: ##STR2## wherein X is a halogen atom and R.sub.1 is as defined above with a compound of the formula:H-Ywherein Y is as defined above.