Abstract: This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--;Y is hydrogen, halogen and loweralkoxy;p is 1 or 2;n is 2, 3 or 4;R is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, amino, loweralkylamino, nitro, loweralkylthio, trifluoromethoxy, cyano, trifluoromethyl, ##STR2## R.sub.1 is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, carboxyl, loweralkylamino, nitro, loweralkylthio, cyano, and trifluoromethyl;m is 1 or 2; a pharmaceutically acceptable acid addition salt thereof and, where applicable the geometric and optical isomers and racemic mixtures thereof.The compounds and compositions of this invention are useful as antipsychotic agents, as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.
Abstract: 3.beta.-[4-iodophenyl]-tropan-2.beta.-carboxylic acid methyl ester tartrate is a high affinity binding ligand for neurotransmitters in mammalian brains. It and its congeners may be employed for imaging and other brain scanning techniques that allow the determination of the presence of cocaine receptors, such as neurotransmitters and the like.
Type:
Grant
Filed:
August 9, 1990
Date of Patent:
July 7, 1992
Assignee:
Research Triangle Institute
Inventors:
Frank I. Carroll, Anita H. Lewin, Philip Abraham, Michael J. Kuhar, John W. Boja
Abstract: The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1) ##STR1## wherein the symbols have the following meanings: .circle.A is phenyl, or a 5- or 6-membered aromatic group containing 1 or 2 of the following hetero atoms: oxygen and/or sulphur and/or nitrogen;R.sub.1 and R.sub.2 may be equal or different and are hydrogen or substituents;R.sub.3 is a hydrogen atom or, together with R.sub.4, may form a ring consisting of 6 or 7 carbon atoms;R.sub.4 is a hydrogen atom or alkyl group having 1-3 carbon atoms;R.sub.5 is a straight, branched or cyclic alkyl group having 1-4 carbon atoms;R.sub.6 is a straight or branched, saturated or unsaturated alkylene group having a chain length of 2-6 carbon atoms;Z is the group NR.sub.12, wherein R.sub.12 is a hydrogen atom or an alkyl group having 1-3 carbon atoms, or Z is an oxygen atom;n has the value 0 or 1;X is a carbonyl group, thiocarbonyl group or SO.sub.2 group;R.sub.7 and R.sub.
Type:
Grant
Filed:
January 9, 1989
Date of Patent:
December 26, 1989
Assignee:
Duphar International Research B.V.
Inventors:
Ineke Van Wijngaarden, Johannes M. A. Zwagemakers, Jan Van Dijk
Abstract: Non-peptidyl compounds characterized generally as .beta.-succinamidoacyl aminodios are useful as renin inhibitors for the treatment of hypertension.
Abstract: 3.alpha.-Benzoylamino-2.beta.-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding 2.beta.,3.beta.-epoxy-nortropane with benzylamine in the presence of phenol.
Abstract: Tropyl derivatives of the formula: ##STR1## in which R.sup.1 is (a) phenyl linked through a direct bond, --O--, ##STR2## (in which m=2 or 3); (b) diphenylmethyl; or (c) 10H-phenothiazin-10-yl; (each of which type may be substituted, or unsubstituted); R.sup.2 is --H, --OH, or --O Si (CH.sub.3).sub.3 ; and R.sup.3 is substituted or unsubstituted phenyl, e.g. 4-[3-(4-fluorobenzoyl)-8-azabicyclo [3.2.1]oct-8-yl]-1-(-4-fluorophenyl)-1-butanone, in free base form or pharmaceutically acceptable acid addition salts are useful as pharmaceuticals.
Abstract: Compounds of the formula (III) and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy or C.sub.1-6 alkylthio group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-7 acyl, C.sub.1-7 acylamino or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy or nitro or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy in which case R.sub.3 is any one of the groups given for R.sub.2 and R.sub.3 above;R.sub.4 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.6 where s is 0 to 2 and R.sub.6 is a C.sub.3-8 cycloalkyl group, or a group --(CH.sub.2).sub.t R.sub.7 where t is 1 or 2 and R.sub.7 is a phenyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.
Abstract: 3.alpha.-Benzylamino-2.beta.-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding 2.beta.,3.beta.-epoxy-nortropane with enzylamine in the presence of phenol.
Abstract: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substiutent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a tropane-3-carboxylate having a double bond in the 2,3-position with an aryl Grignard reagent. Transformations of the substituent on nitrogen are subsequently effected. Compounds where the 3-carboalkoxy group is in the exo configuration possess hypoglycemic activity, and those where the 3-carboalkoxy group is in the endo configuration possess narcotic antagonist activity.
Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein ##STR2## represents a tertiary aliphatic amine; wherein ##STR3## represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.