Abstract: Pyridyl ethers of formula ##STR1## [where R is hydrogen, or 1 to 4 hydroxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, halogen, trifluoromethyl, phenyl, halophenyl, alkyphenyl, alkoxyphenyl, carboxy, carboxamide, nitro, thiol or alkylthio substituents and B is quinuclidyl or tyopanyl] are useful for the treatment of conditions which respond to antagonism of 5 - HT.sub.3 receptors e.g. the treatment of migraine, emesis, anxiety, gastro-intestinal disorders and psychotic disorders.

Abstract: The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R.sub.1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine, chlorine, bromine or trifluoromethyl, or a pyridyl group;R.sub.2 represents hydrogen or a straight-chained or branched alkyl group with 1-4 carbon atoms;R.sub.3 represents a straight-chained or branched alkyl group with 1-3 carbon atoms, a hydroxyalkyl group with 2-3 carbon atoms, a phenyl group which can be mono- or di-substituted by chlorine, bromine, methyl or methoxy, a cyclohexyl group or a dialkylamino alkyl group, where in each alkyl group can contain from 1-3 carbon atoms;R.sub.4 represents hydrogen or a straight-chained or branched alkyl group with 1-3 carbon atoms; orR.sub.3 and R.sub.

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: Compounds of formula: ##STR1## wherein: Ar is an aromatic group; R and R.sub.1 are H or CH.sub.3 ; A represents a nitrogenized heterocyclic radical; B is OH or forms with the adjacent CO group, either an amido group, or a carbonyloxy group; R.sub.2 and R.sub.3 are H or alkyl; m=0 or 1; and n=0, 1, 2 or 3.These compounds are useful as drugs having stimulating, protecting and/or correcting activities of the cerebral functions.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.

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: There are described compounds of formula I,ZCHRCON(--N.dbd.CR.sub.4 R.sub.5)CHR.sub.6 (CH.sub.2).sub.n COY Iwhere the substituents are defined in the disclosure.There are also described methods for making the compounds, formulations containing them and their use, e.g. as antihypertensives.

Abstract: There are disclosed pyridine-2-ethers and pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring corresponding to the formula ##STR1## the pyridine-N-oxides and/or amine oxides thereof and the pharmaceutically acceptable salts thereof. The compounds show analgesic activity.

Abstract: Compounds of formula (I): ##STR1## wherein: one of X and Y is CO and the other is NH;R.sub.1 is C.sub.1-6 alkoxy or C.sub.1-6 alkylthio;R.sub.2 is hydrogen, trifluoromethyl, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, halogen, nitro or amino, aminocarbonyl or aminosulphonyl 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 any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkoxy or nitro groups, or N-disubstituted by C.sub.2-5 polymethylene;R.sub.3 is amino, aminocarbonyl or aminosulphonyl N-substituted by one or two C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkoxy or nitro groups, or N-disubstituted by C.sub.

Abstract: Salicylic acid derivatives of the formula I ##STR1## wherein R.sup.1, W, X, Y and Z have the meanings indicated or a physiologically tolerated salt thereof, processes for their preparation, pharmaceutical formulations based on these compounds and their use as antidiabetic agents.

Abstract: There are disclosed nor-tropane derivatives substituted at the 3 position with aroylamino or heteroaroylamino and substituted at the 8 position with benzyl, substituted benzyl, 2-methyl thiophene, 3-methyl thiophene, 2-methyl furan or cyclohexylmethyl. The compounds are prepared by condensing the carboxylic acids corresponding to said aroyl or heteroaroyl group with the corresponding .beta.-3-amino-8-substituted nor-tropanes. The compounds possess neuroleptic properties.

Abstract: 1-Substituted imidazoles having the formula ##STR1## wherein A is a chemical bond or a straight or branched, saturated or unsaturated, aliphatic residue having from 1 to 6 carbon atoms wherein 1, 2 or 3 of such carbon atoms may be replaced by a corresponding number of heteroatoms selected from oxygen, sulphur and nitrogen; R is a fused, saturated or unsaturated, non-aromatic carbocyclic, polycyclic ring system; a saturated or unsaturated carbocyclic spirocyclic ring system, optionally containing one or more ring heteroatoms selected from oxygen, sulphur and nitrogen; ora saturated or unsaturated, carbocyclic bridged-polycyclic ring system, optionally containing one or more ring heteroatoms selected from oxygen, sulphur and nitrogen and having one or more bridges;or AR together represent a straight or branched, saturated or unsaturated, aliphatic residue having 3 to 6 carbon atoms, wherein 1, 2 or 3 such carbon atoms may be replaced by a corresponding number of heteroatoms selected from oxygen, sulphur and nit

Abstract: Pharmaceutical compositions comprising compounds of formula (I) or pharmaceutically acceptable salts and/or N-oxides and/or solvates thereof: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy or C.sub.1-6 alkylthio group; andone of R.sub.2, R.sub.3 and R.sub.4 is hydrogen, the second is C.sub.1-6 alkylthio and the third is selected from the class of substituents consisting of 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 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl or aminosulphonyl optionally N-substituted by one or two C.sub.1-6 alkyl groups; orR.sub.1 is joined to R.sub.2 to form C.sub.1-2 alkylenedioxy; andone of R.sub.3 and R.sub.4 is C.sub.1-6 alkylthio and the other is selected from the class of substituents defined above;R.sub.5 is hydrogen or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.7 where s is 0 to 2 and R.sub.7 is a C.sub.

Abstract: There are disclosed nor-tropane derivatives substituted at the 3 position with aroylamino or heteroaroylamino and substituted at the 8 position with benzyl, substituted benzyl, 2-methyl thiophene, 3-methyl thiophene, 2-methyl furan or cyclohexylmethyl. The compounds are prepared by condensing the carboxylic acids corresponding to said aroyl or heteroaroyl group with the corresponding .beta.-3-amino-8-substituted nor-tropanes. The compounds possess neuroleptic properties.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: n, p and q independently are 0 to 2;R.sub.5 is hydrogen or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.7 where s is 0 to 2 and R.sub.7 is a C.sub.3-8 cycloalkyl group, or a group --(CH.sub.2).sub.t R.sub.8 where t is 1 or 2 and R.sub.8 is C.sub.2-5 alkenyl or a phenyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and halogen, or a thienyl group;R.sub.12 is C.sub.1-6 alkylsulphonyl;and eitherR.sub.1 is C.sub.1-6 alkoxy or C.sub.1-6 alkylthio; and one of R.sub.2 and R.sub.11 is hydrogen and the other is C.sub.1-6 alkoxy, C.sub.1-6 alkyl or hydroxy; or R.sub.1 and R.sub.2 together are C.sub.1-3 alkylenedioxy; and R.sub.11 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkoxy,hydroxy, nitro, C.sub.1-7 acyl, amino, C.sub.1-7 acylamino, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl, C.sub.

Abstract: Novel 3 .beta.-aroylamino and 3 .beta.-heteroaroylamino nor-tropanes and granatanes are provided having the general formula: ##STR1## Wherein n=1 or 2, R represents a benzyl or a substituted benzyl group and A-CO represents one of a specific range of aroyl groups. The compounds of the invention are useful in the treatment of psychism or digestive troubles.

Abstract: Histamine H.sub.2 -receptor antagonists having the formula ##STR1## wherein R.sub.1 represents C.sub.1 -C.sub.4 alkyl or benzyl, R.sub.2 represents hydrogen or C.sub.1 -C.sub.4 alkyl, and Het represents an imidazole, pyrazole, pyrimidine, pyrazine, pyridazine, thiazole, isothiazole, oxazole, isoxazole, triazole, thiadiazole, benzimidazole, or furan ring either unsubstituted or substituted with a C.sub.1 -C.sub.4 alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino, or dimethylaminomethyl group are disclosed along with a synthetic method of producing such compounds and their use as gastric-acid-production inhibitors.

Abstract: There are disclosed nor-tropane derivatives substituted at the 3 position with aroylamino or heteroaroylamino and substituted at the 8 position with benzyl, substituted benzyl, 2-methyl thiophene, 3-methyl thiophene, 2-methyl furan or cyclohexylmethyl. The compounds are prepared by condensing the carboxylic acids corresponding to said aroyl or heteroaroyl group with the corresponding .beta.-3-amino-8-substituted nor-tropanes. The compounds possess neuroleptic properties.

Abstract: Compounds of the formula ##STR1## wherein Ar is ##STR2## R.sub.1 is hydrogen, fluorine, bromine, methyl or methoxy; X is .dbd.CO, .dbd.CH--CN, .dbd.CH--OH, --O--, --S--, --NH--, ##STR3## and R is hydrogen, 4-fluoro, 4-chloro, 4-trifluoromethyl, 3-trifluoromethyl, 3-trifluoromethyl-4-chloro, 4-methyl or 4-methoxy;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as neuroleptics.

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: There are disclosed nor-tropane derivatives substituted at the 3 position with aroylamino or heteroaroylamino and substituted at the 8 position with benzyl, substituted benzyl, 2-methyl thiophene, 3-methyl thiophene, 2-methyl furan or cyclohexylmethyl. The compounds are prepared by condensing the carboxylic acids corresponding to said aroyl or heteroaroyl group with the corresponding .beta.-3-amino-8-substituted nor-tropanes. The compounds possess neuroleptic properties.

Abstract: Imidazoles of formula (I) ##STR1## wherein A is a chemical bond or a straight or branched, saturated or unsaturated, aliphatic residue having from 1 to 6 carbon atoms wherein 1, 2 or 3 of such carbon atoms may be replaced by a corresponding number of heteroatoms selected from oxygen, sulphur and nitrogen providing (in the case of 2 or 3 heteroatoms) that any such heteroatom is not located adjacent to a further such heteroatoms or heteroatomsR is a fused, saturated or unsaturated, non-aromatic carbocyclic, polycyclic ring system; a saturated or unsaturated, carbocyclic spirocyclic ring system, optionally containing one or more ring heteroatoms selected from oxygen, sulphur and nitrogen; or a saturated or unsaturated, carbocyclic bridged-polycyclic ring system, optionally containing one or more ring heteroatoms selected from oxygen, sulphur and nitrogen and having one or more bridges;or AR together represent a straight or branched, saturated or unsaturated, aliphatic residue having 3 to 6 carbon atoms, wherein

Abstract: There are disclosed nor-tropane derivatives substituted at the 3 position with aroylamino or heteroaroylamino and substituted at the 8 position with benzyl, substituted benzyl, 2-methyl thiophene, 3-methyl thiophene, 2-methyl furan or cyclohexylmethyl. The compounds are prepared by condensing the carboxylic acids corresponding to said aroyl or heteroaroyl group with the corresponding .beta.-3-amino-8-substituted nor-tropanes. The compounds possess neuroleptic properties.

Abstract: N-(diphenylmethoxy-mono- or bicyclic-alkyleneiminoalkyl)-dicarboximides, e.g. those of the formula ##STR1## A=aliphatic or cycloaliphatic radical R,R'=H, alkyl, halogen or CF.sub.3R"=H or both are ethyleneq=2-4and salts thereof are antiallergics and antiasthmatics.

Abstract: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substitutent 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: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substitutent 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: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substituent 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: 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: The invention relates to novel nortropine-carbazate derivatives of the general formula (I), ##STR1## wherein R.sub.1 is C.sub.1-4 alkyl, phenyl or halophenyl group,R.sub.2 is hydrogen or a C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl, C.sub.1-4 acyl, phenoxycarbonyl or C.sub.1-4 alkoxycarbonyl group, andR.sub.3 is hydrogen of a C.sub.1-4 alkyl or C.sub.1-4 acyl group, orR.sub.2 and R.sub.3 may form together a C.sub.1-10 alkylene group attachedTo the nitrogen atom with a double bond, as well as to pharmaceutically acceptable acid addition salts of said compounds.The above compounds are new and can be applied as narcosis potentiating agents.The compounds of the general formula (I) can be prepared by reacting a compound of the general formula (II), ##STR2## wherein R.sub.1 is as defined above and Q is halogen, C.sub.1-4 alkoxy or phenoxy, with a hydrazine compound of the general formula (III), ##STR3## wherein R.sub.2 and R.sub.3 are as defined above.