摘要:
Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##
摘要:
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## Y is a bond or lower alkylene; R.sub.2 and R.sub.3 are independently hydrogen, lower-alkyl or halogen;R.sub.4 is ##STR3## R.sub.5 is hydrogen, lower-alkyl or halogen; R.sub.6 is hydrogen, lower-alkyl or halogen;R.sub.7 is hydrogen or lower-alkyl;R.sub.8 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.9 is lower-alkyl;R.sub.10 is lower-alkyl, trifluoromethyl or difluoromethyl;or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents.
摘要:
1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.
摘要:
The invention relates to intermediates in the production of dialkylenepiperidino compounds and their enantiomers and their use for the treatment of substance p- and neurokinin-dependent pathology.
摘要:
The invention relates to compounds of formula: ##STR1## in which Y represents--either a group Cy--N in whichCy represents a phenyl, optionally substituted; a C.sub.3 -C.sub.7 cycloalkyl group; a pyrimidinyl group or a pyridyl group; or a group ##STR2## in which Ar represents a phenyl, optionally substituted, a pyridyl group; a thienyl group;x is zero or one;X represents a hydroxyl, a C.sub.1 -C.sub.4 alkoxy; a hydroxyalkyl; a C.sub.1 -C.sub.4 acyloxy; a phenacyloxy; a carboxyl; a C.sub.1 -C.sub.4 carbalkoxy; a cyano; an aminoalkylene; a group --N--(X.sub.1).sub.2 in which the groups X.sub.1 independently represent hydrogen, a C.sub.1 -C.sub.4 alkyl; a group ##STR3## in which Alk represents a C.sub.1 -C.sub.6 alkyl; a group ##STR4## in which the Alk.sub.1 is a C.sub.1 -C.sub.3 alkylene and Alk'.sub.1 is a C.sub.1 -C.sub.3 alkyl; a C.sub.1 -C.sub.4 acyl; a group --S--X.sub.2 in which X.sub.2 represents hydrogen or a C.sub.1 -C.sub.4 alkyl group; or alternatively X forms a double bond with the carbon atom to which it is linked and with the adjacent carbon atom in the heterocycle;m is 2 or 3;Ar' represents a phenyl, optionally substituted; a thienyl; a benzothienyl; a naphthyl; an indolyl; an indolyl N-substituted with a C.sub.1 -C.sub.3 alkyl;R represents hydrogen, a C.sub.1 -C.sub.4 alkyl;T represents a group selected from --C(O)-- and --C(W)--NH--W being an oxygen or sulphur atom, andZ represents either hydrogen, or M or OM when T represents a --C(O)-- group, or M when T represents a group--C(W)--NH; M represents a C.sub.1 -C.sub.6 alkyl; a phenylalkyl, a pyridyl alkyl; a naphthylalkyl; a pyridylthioalkyl; a styryl; or one of its salts with inorganic or organic acids.
摘要:
Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents C.sub.1-6 alkyl;R.sub.2 represents H or C.sub.1-6 alkyl;R.sub.3 represents H or C.sub.1-3 alkyl; and pharmaceutically acceptable salts and solvates (for example hydrates) thereof.The compounds are indicated as useful for the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.
摘要:
This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases, and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.
摘要:
This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases, and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.
摘要:
6-Substituted-1,2-benzisothiazolin-3-ones carrying an aminoalkyl group in the 2-position and being optionally substituted in the 4- and/or 5-position are antithrombotic agents. The compounds, of which 2-(2-diethylaminoethyl)-4,5-dimethyl-1,2-benzisothiazolin-3-one is a representative embodiment, can be prepared by cyclization of an appropriately substituted bis-[2-(aminoalkylcarbamyl)phenyl]disulfide, or by other disclosed methods.