Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: This invention presents a series of novel tropane-based derivatives complexed with either technetium or rhenium that are specific for central nervous system receptors, in particular, dopamine or serotonin receptors. The compounds of the invention have utility, inter alia, as imaging agents for CNS receptors.

Abstract: The invention provides novel compounds of formula (I) and formula (II) ##STR1## wherein R.sup.1 represents a group of formula (A) ##STR2## where each of W, X, Y and Z and represents either a group CR or the nitrogen atom, provided that not more than two of W, X, Y and Z represent the nitrogen atom and where each R present is independently selected from hydrogen and halogen atoms and cyano, amino, hydrazino, acylamino, hydroxy, alkyl, hydroxyalkyl, alkoxy, haloalkyl, haloalkoxy, alkenyl, alkenyloxy, alkoxyalkenyl, alkynyl, carboxylic acyl, alkoxycarbonyl, aryl and heterocyclyl groups, said groups comprising up to 6 carbon atoms, and wherein R.sup.2 represents a group XR.sup.3 where X represents oxygen or a group NR.sup.4 where R.sup.3 and R.sup.

Abstract: A process for preparing a compound of formula (I), wherein n is 2 or 3; which process comprises reducing a compound of formula (II), wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl and n is 2 or 3; by catalytic hydrogenation in the presence of a rhodium catalyst.

Abstract: Cocaine analogs are disclosed. The analogs, certain 6-alkyl substituted tropane derivatives, bind to the cocaine binding site on dopamine transporter, without interfering with the dopamine receptor. The craving for cocaine is thereby blocked. The analogs may readily be synthesized stereoselectively, and are relatively resistant to metabolic degradation.

Abstract: Disclosed are bridge-substituted analogs of tropanes and benztropines as well as methods for: imaging of cocaine receptors; treatment of cocaine abuse; and imaging and treatment of Parkinson's disease.

Abstract: Selective blockade of DA and 5-HT uptake sites with 3-aryltropane derivatives.

Abstract: Selective blockade of DA and 5-HT uptake sites with 3-aryltropane derivatives.

Abstract: The invention provides a reagent for the presumptive identification of cocaine, cocaine salts and phencyclidene comprising cobalt thiocyanate, at least one poly-hydroxy alcohol and a third component selected from the group consisting of a polyether, a silicon derivative of a polyether and mixtures thereof, with the proviso that the poly-hydroxy alcohol is not glycerol.

Abstract: An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: ##STR1## wherein R= ##STR2## wherein n=2-8; R'=C.sub.w H.sub.2w+1 wherein w=0-6 and C includes an isotope of carbon; andX=an isotope of Cl, an isotope of Br, an isotope of F, an isotope of I, or Sn(R".sub.1 R".sub.2 R".sub.3), whereinR".sub.1 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group;R".sub.2 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group; andR".sub.3 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group.Additionally, a precursor of a radiolabeled neuroprobe and a kit for preparing the iodinated neuroprobe are provided.

Abstract: The present invention discloses compounds of the formula, ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R.sup.3, and R.sup.4 each have the meanings set forth in the specification.The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e dopamine, serotonin, noradrenalin, reuptake inhibitors.

Abstract: A compound of formula (I) or a salt thereof, or a solvate thereof: ##STR1## wherein B represents a C.sub.1-4 n-alkylene group wherein each carbon is optionally substituted by a C.sub.1-6 alkyl group; Z represents a bond, CH.sub.2, (CH.sub.2).sub.2 or X--CH.sub.2 --CH.sub.2 wherein X represents O or S; D represents CO, SO.sub.2, NH--CO or NH--SO.sub.2 ; T represents a bond and U represents CH.sub.2 or T represents CH.sub.

Abstract: Neuroprobes that include rhenium, manganese, and technetium for use in mapping monoamine reuptake sites are disclosed. Non-radioactive tricarbonylrheniumcyclopentadienyl (TRCp) or non-radioactive tricarbonylmanganesecyclopentadienyl (TMCp) phenyltropane analogs are synthesized for use as testing surrogates for radioactive technetium congeners. Ferrocenyl analogs of phenyltropane are disclosed as useful precursors for the preparation of novel tricarbonyltechnetiumcyclopentadienyl (TTCp) phenyltropane analogs in radioactive form.

Abstract: An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: ##STR1## wherein: R=aryl, substituted aryl, heterocyclic, CO(CH.sub.2).sub.n Y, (CH.sub.2).sub.n CHF.sub.2, and (CF.sub.2).sub.n Y, wherein:Y=Cl, Br, I, (CH.sub.2).sub.m, aryl, substituted aryl, heterocyclic CO.sub.2 H, CO.sub.2 R.sup.3, CO.sub.2 NR.sup.3 R.sup.4, OH, OR.sup.3, CH(OR.sup.3).sub.2, CR.sup.3 (OR.sup.4).sub.2, OC0R.sup.3, OSO.sub.2 R.sup.3, OCONR.sup.3 R.sup.4, OCOOR.sup.3, CONR.sup.3 R.sup.4, NR.sup.3 R.sup.4, NR.sup.3 COR.sup.4, NR.sup.3 CO.sub.2 R.sup.4, NR.sup.3 CONR.sup.4 R.sup.5, NCS, NCO;R.sup.3, R.sup.4 and R.sup.5 =alkyl, substituted alkyl, alkenyl, substituted alkenyl, aryl, substituted aryl, or heterocyclic;m=3-8; andn=1-6;R'=C.sub.w H.sub.2w+1 wherein w=0-6 and C includes an isotope of carbon; andX=an isotope of Cl, an isotope of Br, an isotope of F, an isotope of I, or Sn(R".sub.1 R".sub.2 R".sub.3), whereinR".sub.1 =a C.sub.p H.sub.

Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or >CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.

Abstract: A stereoselective process for forming compounds related to 4-endotropanamine through the reactive amination of a corresponding ketone with a triacyloxy borohydride.

Abstract: This invention is directed to novel benzyl quaternary ammonium compounds and their synthesis. The compounds have valuable utility as organic directing agents in the crystallization of a silicate structure which, in turn, is useful as a catalyst component, sorbent, and/or ion-exchanger. More particularly, this invention is concerned with benzyl quaternary ammonium compounds synthesized by selective alkylation of the bridgehead nitrogen of tropane or quinuclidine with a benzyl salt.

Abstract: An aminobenzoic acid derivative represented by the following general formulas (I), (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints: ##STR1## wherein R.sup.1 represents a group such as an alkynyl or cyanoalkyl group; R.sup.2 represents a group such as an amino or acylamino group; R.sup.3 represents a halogen atom; X represents --O-- or --NH--; and A represents an oxygen or sulfur atom.

Abstract: A process of enantioselective synthesis of seven-membered carbocycles in the presence of di-rhodium(II) tetracarboxylate catalysts.

Abstract: Compounds of general formula: ##STR1## where: Ar=phenyl or beta-naphtyl, or aromatic heterocyclic 6-membered ring containing one or two nitrogen atoms;R.sub.1 =one or more substituents of the Ar nucleus, preferably in para position, and selected out of the group consisting of H, CH.sub.3, CH.sub.2 --CH--(CH.sub.3).sub.2, O--CH.sub.3, Cl, F, Br, CF.sub.3, NH.sub.2, S--CH.sub.3, CN, NO.sub.2 R.sub.2 =H, CH.sub.3, C.sub.2 H.sub.5, CH(CH.sub.3).sub.2 ;R.sub.3 = ##STR2## Where R.sub.4 =H, CH.sub.3, C.sub.2 H.sub.5 R.sub.5 =H, CH.sub.3X=none O, S, NH, NCH.sub.3, --CH=CH--, --C.ident.C--Y=O, NH,both in the racemic Form and in the isomeric enantiomeric forms,which produce a nootropic effect, i.e. memory enhancement and learning facilitation, as well as an analgesic effect.

Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: This invention relates to novel dopamine D-1 and D-2 imaginging agents which are both fluorinated and iodinated and can appropriately labelled for use in both PET and SPECT imaging. Compounds include S-(-)-2-fluoroethoxy-3-methyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodoben zamide and R(+)-2,3-dimethoxy-N-[(1-(4'-fluorobenzyl)-2-pyrrolidinyl)methyl]-5-iodobe nzamide.

Abstract: The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R.sub.3, and R.sup.4 each have the meanings set forth in the specification.The compounds possess valuable pharmaceutical properties as dopamine reuptake inhibitors.

Abstract: (Endo)-N-[[[8-azabicyclo[3.2.1]octan-3-yl]amino]carbonyl]-2-(cyclopropylmet hyloxy)benzamide and pharmaceutically acceptable salts thereof possess 5-HT.sub.3 antagonistic activity and are useful in the treatment of neuro-psychiatric disorders (e.g. anxiety), gastro-intestinal disorders and migraine.

Abstract: A benzamide derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkanoyl group; R.sup.2 represents a hydrogen atom or a halogen atom; R.sup.3 represents a lower alkoxy group; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a lower alkyl group, or a lower alkoxy group; A represents C.sub.1 -C.sub.7 alkylene group which may optionally be substituted with a lower alkyl group; X represents a methylene group, an oxygen atom, or a sulfur atom; m represents an integer of from 0 to 3; n represents an integer of from 0 to 3; and p represents an integer of from 0 to 2 and a pharmacologically acceptable salt thereof is provided. These compounds are useful since they have gastrointestinal stimulating activity, and a pharmaceutical composition comprising said compound is useful for the treatment of gastrointestinal diseases.

Abstract: Bioactive cocaine analogs of the general formulae: ##STR1## are provided wherein X' is H or (C.sub.1 -C.sub.5)alkyl, X is H, halo, alkyl, alkoxy, perfluoroalkyl, nitro, alkoxycarbonyl, dialkoxyphosphonyl, acyl, perfluoroacyl, azido (substituted)silyl or (substituted)thio, and Y is H, halo, nitro, amino or (substituted)amino, alkoxycarbonyl, carboxy, alkyl or alkoxy; and the pharmaceutically acceptable salts thereof.

Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: An aminobenzoic acid derivative represented by the following general formulas (I), (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints: ##STR1## wherein R.sup.1 represents a group such as an alkynyl or cyanoalkyl group; R.sup.2 represents a group such as an amino or acylamino group;R.sup.3 represents a halogen atom;X represents --O-- or --NH--; andA represents an oxygen or sulfur atom.

Abstract: Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have the formula ##STR1## Wherein Y=CH.sub.2 R.sub.3, CO.sub.2 R.sub.2 or ##STR2## R.sub.1 =hydrogen, C.sub.1-5 alkyl, R.sub.2 =hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen or amine,R.sub.3 =OH, hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, Cl Br, I, CN, NH.sub.2, NHC.sub.1-6 alkyl, NC.sub.1-6 alkyl, OCOC.sub.1-6 alkyl, OCOC.sub.1-3 alkylaryl,A=S, 0 or NHX=H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen, amino, acylamido, andZ=H, I, Br, Cl, F, CN, CF.sub.3 NO.sub.2, N.sub.3, OR.sub.1, CO.sub.2 NH.sub.2, CO.sub.2 R.sub.1, C.sub.1-6 alkyl , NR.sub.4 R.sub.5, NHCOR.sub.5, NHCO.sub.2 R.sub.6,wherein R.sub.4 -R.sub.6 are each C.sub.1-6 alkyl.

Abstract: The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R.sup.3, and R.sup.4 each have the meanings set forth in the specification.The compounds possess valuable pharmaceutical properties as dopamine reuptake inhibitors.

Abstract: 3-Piperidino-1-chromanol derivatives and analogs having the formula ##STR1## wherein A and B are taken together and are --CH.sub.2 CH.sub.2 -- or A and B are taken separately and are each H;X is CH.sub.2 or O;X.sup.1 is H or OH;Z is H, F, Cl, Br or OH;Z.sup.1 is H, F, Cl, Br or (C.sub.1 -C.sub.3)alkyl;n is 0 or 1; andm is 0 or an integer from 1 to 6;pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: Preparation of biologically active tropane derivatives of novel configurations. The compounds are prepared by decomposing vinyldiazomethanes in the presence of pyrroles to provide a bicyclic ring containing the basic tropane ring system which is then reacted with an aryl Grignard reagent in the presence of a copper (I) or (II) salt to provide 3-aryl-tropane derivatives.

Abstract: This invention relates to compounds of the formula ##STR1## where X is --0--, --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, trifiuoromethoxy, cyano, trifluoromethyl, ##STR2## where aryl is ##STR3## 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 agent, as 5-HT.sub.3 receptor antagonists and as inhibitors of the reuptake of serotonin.

Abstract: New substituted urea compounds of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 is a group of formula II, III or IV ##STR2## where n is 2 or 3, p is 1 or 2, q is 1 to 3, r is 1-3 and R.sup.4 and R.sup.5 are H, C.sub.1-7 alkyl or C.sub.3-6 cycloalkyl; and wherein R.sup.2 is an oxadiazole, substituted with C.sub.1[ alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.3-7 cycloalkyl, benzyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, amino or alkylamino; orwherein R.sup.2 --C--R.sup.6 .dbd.--N--O--R.sup.7 wherein R.sup.6 is hydrogen or methyl and R.sup.7 is C.sub.1-6 alkyl which may be substituted with C.sub.3-7 cycloalkyl;and wherein R.sup.3 is hydrogen, halogen, nitro, substituted amine, trifluoromethyl, C.sub.1-6 alkyl or C.sub.1-6 alkoxy.The compounds are useful in pharmaceutical preparations for treating psychotic disorders, nausea and vomiting.

Abstract: Compounds of the Formula (5) and processes for their preparation and use, particularly in the manufacture of unsymmetrical triphenodioxazine dyes: ##STR1## wherein: Y is H, alkyl, substituted alkyl, alkoxy, Cl or Br;R is a group of Formula (3) ##STR2## R.sup.1 and R.sup.2 are each independently alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form an optionally substituted 4, 5 or 6 membered alicyclic or heterocyclic ring;R.sup.3 is H;Z is Cl, Br or A--NH; andA is H or the residue of a primary amine.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6 or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; andR.sub.3 is chloro, fluoro, bromo, cyclopropyl, C.sub.1-3 alkyl substituted by one, two or three halogen atoms, or R.sub.3 is a group (CH.sub.2).sub.n R.sub.9 where R.sub.9 is --CN, --OH, --OCH.sub.3, --SH, --SCH.sub.3, --C.tbd.CH or --CH.dbd.CH.sub.2 and n is O or 1, with the proviso that when n is 0, R.sub.9 is not --OH or --SH.

Abstract: Azacyclic compounds selected from the group consisting of ##STR1## wherein R.sup.1 is H or C.sub.1-6 -alkylR.sup.3 is ##STR2## wherein R' is C.sub.3-8 -alkyl, cyclopropyl, C.sub.4-8 -cycloalkyl, benzyl which may be substituted, or C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl, andR" is H or C.sub.1-8 -alkyl or C.sub.1-6 -alkoxy or C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or aryl, andR'" is H or C.sub.1-6 -alkyl or C.sub.4-8 -cycloalkyl; andR.sup.4 is H, C.sub.1-8 -alkyl or Cl; and ##STR3## provided that R.sup.3 is not ##STR4## wherein R' is C.sub.3-8 -alkyl, cyclopropyl or C.sub.1-3 -alkoxymethyl, and provided that R.sup.3 is not --CH.dbd.N--OR'", wherein R'" is H or C.sub.1-6 -alkyl, when the compounds of formula I is ##STR5## and a salt thereof with a pharmaceutically-acceptable acid. The new compounds are useful in improving the cognitive functions of the forebrain and hippocampus of mammals, and are useful in the treatment of Alzheimer's disease.

Abstract: Preparation of biologically active tropane derivatives of novel configurations. The compounds are prepared by decomposing vinyldiazomethanes in the presence of pyrroles to provide a bicyclic ring containing the basic tropane ring system which is then reacted with an aryl Grignard reagent in the presence of a copper (I) or (II) salt to provide 3-aryltropane derivatives.

Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH=CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: Aryl ureas and carbamic acid derivatives of formulaA--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including 3,5-dichlorophenylW is O or SY is NH or O andB is a specified saturated azacyclic ring, e.g. tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.

Abstract: N-benzyl tropane amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compounds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.

Abstract: Aroyl ureas and carbamic acid derivatives of formulaA--CO--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including optionally substituted phenylW is O or SY is NH or S andB is a specified saturated azacyclic ring, eg tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.

Abstract: Certain specific substituted benzobicyclic carboxamides and their valuable use as 5-HT3 antagonists having CNS and gastric prokenetic activity void of any significant D.sub.2 receptor binding activity are disclosed.

Abstract: Compounds of the general formula: ##STR1## wherein the various substituents are defined hereinbelow have pharmacological properties rendering them useful as antiemetic agents with reduced undesirable side-effects. Various methods are described for their preparation involving formation of the amide link, etherification of the 2-hydroxy derivative, introducing the R.sup.5 CH.sub.2 group on the N-unsubstituted azabicyclooctane or nonane or, for 4-amino compounds by hydrolysing a 4-acylamino derivative.

Abstract: Carbocyclic and heterocyclic carbonylmethylene- and carbonylmethylpiperidines and -pyrrolidines are serotonin antagonists.

Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.

Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;X is a moiety capable of hydrogen bonding to the NH group depicted in formula (I);R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, carboxy, C.sub.1-6 alkoxycarbonyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.4-5 polymethylene; andZ is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; and R.sub.3 or R.sub.4 is C.sub.1-7 alkyl, C.sub.

Abstract: A new class of anti-spasmodic thioester compounds having a heterocyclic ring containing the nitrogen atom of a secondary or tertiary amine or a bicycloheterocyclic ring system containing the nitrogen atom of a secondary or tertiary amine. These compounds have the general formula I ##STR1## wherein: =n is an integer from 0 to 2;R.sub.1 is aryl or cycloalkyl;=R.sub.2 is hydrogen or hydroxyl; andR.sub.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6 or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; andR.sub.3 is chloro, fluoro, bromo, cyclopropyl, C.sub.1-3 alkyl substituted by one, two or three halogen atoms, or R.sub.3 is a group (CH.sub.2).sub.n R.sub.9 where R.sub.9 is --CN, --OH, --OCH.sub.3, --SH, --SCH.sub.3, --C.tbd.CH or --CH.dbd.CH.sub.2 and n is O or 1, with the proviso that when n is 0, R.sub.9 is not --OH or --SH.