摘要:
Acylhydrazone compounds having excellent pyschotropic activity which are represented by the formula: ##STR1## wherein Z is selected from the groups having the formulas: ##STR2## wherein n is an integer of from 0 to 2 and R.sup.1 -R.sup.12 are as defined hereinbelow.
摘要:
A process for producing butyrophenone derivatives of the formula: ##EQU1## which comprises reacting a compound of the formula: ##SPC1##With an amine of the formulaH-W(wherein Ar represents a group of either one of the formulas: ##SPC2##Z is a secondary amino group and W is the residue of an amine excluding a hydrogen atom therefrom). The said butyrophenone derivatives and their salts exhibit a variety of beneficial pharmacological activities including a central and autonomic nervous system depressing activity.
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:
Novel olefinic aryl ketone compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy, R.sup.2 is hydrogen or halogen, and X is a group of the formula: ##STR2## and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reaction of an acetylenic alcohol of the formula: ##STR3##wherein R.sup.1 and R.sup.2 are each as defined above with formaldehyde and an piperidine compound of the formula: , or its non-toxic salt; reduction of the resultant acetylenic aryl alcohol; and oxidation of the resultant olefinic aryl alcohol.
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:
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:
Butyrophenone compounds having excellent psychotropic activities represented by the formula: ##STR1## wherein R.sup.1 is a halogen atom, R.sup.2 is a lower alkyl group, and Z is a group of either one of the formulae: ##STR2## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.3 is a hydrogen atom or a hydroxyl group but only when said additional single bond linkage is not present and R.sup.4 is a hydrogen atom or a phenyl or benzyl group optionally substituted with one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy and trifluoromethyl on the benzene ring (except monohalophenyl)), ##STR3## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.5 is a hydrogen atom or a lower alkyl group and R.sup.6 and R.sup.7 are each a hydrogen atom, a halogen atom or a lower alkyl group), ##STR4## (wherein R.sup.8 is a hydrogen atom or a lower alkyl group and R.sup.9 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group), ##STR5## (wherein R.sup.10 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group), or ##STR6##
摘要:
Butyrophenone compounds having excellent psychotropic activities represented by the formula: ##STR1## wherein R.sup.1 is a halogen atom, R.sup.2 is a lower alkyl group, and Z is a group of either one of the formulae: ##STR2## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.3 is a hydrogen atom or a hydroxyl group but only when said additional single bond linkage is not present and R.sup.4 is a hydrogen atom or a phenyl or benzyl group optionally substituted with one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkyoxy and trifluoromethyl on the benzene ring (except monohalophenyl)), ##STR3## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.5 is a hydrogen atom or a lower alkyl group and R.sup.6 and R.sup.7 are each a hydrogen atom, a halogen atom or a lower alkyl group), ##STR4## (wherein R.sup.8 is a hydrogen atom or a lower alkyl group and R.sup.9 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group), ##STR5## (wherein R.sup.10 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group), or ##STR6##
摘要:
Spiro amine derivatives having excellent antihypertensive activity and central nervous system depressant activity, and represented by the formula: ##STR1## and their preparation and use.