Abstract: The invention relates to compounds of formula II ##STR1## and their pharmaceutically acceptable salts wherein R.sup.5 represents hydrogen, acyl, lower alkyl or cycloalkyl; R.sup.6 represents hydrogen, halogen, trifluormethyl, or lower alkyl; R.sup.7 represents hydrogen, lower alkyl, hydroxy, lower alkoxy, arylloweralkoxy; R.sup.8 represents hydrogen or lower alkyl; and R.sup.9 represents hydrogen or lower alkyl.The compounds have dopamine blockade activity and may be used in the treatment of psychoses including schizophrenia.

Abstract: Indoloquinolizines of the formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts [wherein R.sup.1 represents hydrogen, lower alkyl or lower aralkyl, R.sup.2 and R.sup.3 each represent hydrogen, halogen, lower alkoxy or lower alkyl, R.sup.4 represents hydrogen, halogen or lower alkyl and R.sup.5 represents lower alkyl or aryl] possess antihypertensive activity.

Abstract: The disclosure describes new 4-aminoquinoline derivatives of general formula ##STR1## and their pharmaceutically acceptable acid addition salts, where X is trifluoromethyl or halogen, Z is hydrogen or a defined substituent and R is a group having one of the formulae ##STR2## where R.sup.1 is hydrogen or lower alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl and A is lower alkylene. The new 4-aminoquinoline derivatives show analgesic activity and, in some cases, anti-inflammatory activity.

Abstract: The invention concerns compounds of formula ##STR1## or salts thereof, wherein R represents an acyl group which possess anti-inflammatory activity and have low toxicity. Methods for preparing the compounds and pharmaceutical compositions are also disclosed.

Abstract: Novel compounds of formula I ##STR1## are described wherein R is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms, R.sup.1 is hydrogen, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, lower alkoxy, halogen, formyl, phenyl, phenylalkyl or acetal [CH(OR.sup.2).sub.2 where R.sup.2 is lower alkyl, or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, Z is an anion, A is an alkylene radical having from 1 to 3 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and X is a benzothiazole, benzimidazole, benzoxazole, or phenyl radical which may be substituted and acid addition or quaternary ammonium salts of compounds wherein X is a benzimidazole radical. The compounds are used for the treatment of ulcers or hypersecretion. Treatment methods are claimed as well as pharmaceutical compositions.

Abstract: The invention relates to the preparation of 1-bromo-2-D-alkylpropanoyl-L-proline derivatives and analogous compounds which are useful as chemical intermediates to angiotensin converting enzyme (ACE) inhibitors and to the stereospecific synthesis of such ACE inhibitors having the formula: ##STR1## wherein R.sup.1 is lower alkyl and R.sup.4 and R.sup.5 are both hydrogen or together with the carbons to which they are attached represent a benzene ring optionally substituted by defined substituents. Intermediates of formula ##STR2## are also disclosed wherein R.sup.1, R.sup.4, R.sup.5 are as defined above and B.sup.+ is a cation.

Abstract: The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinium radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, eg where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.

Abstract: Compounds having the formula ##STR1## wherein Y represents --CHOH-- or ##STR2## Z and Z.sup.1 independently represent ##STR3## --SO.sub.2 --, --COCH.sub.2 --, or --CO(CH.sub.2).sub.2 --; Z may also represent --CH.sub.2 --, --(CH.sub.2).sub.2, --CHMe--, or --CMe.sub.2 --; R.sup.1 and R.sup.2 independently represent hydrogen or substituents selected from halogen, lower-alkoxy, nitro, amino, lower alkylamino, trifluoromethyl, hydroxy, aryl lower alkoxy and lower alkyl; or R.sup.1 and R.sup.2 when adjacent together with the carbon atoms to which they are attached form a six membered carbocyclic ring; R.sup.3 represents hydrogen, halogen, lower alkyl or lower alkoxy, R.sup.4 represents lower alkyl or hydrogen; .alpha. and .beta. each represent hydrogen or a direct bond between the carbon atoms to which they are attached, and acid addition quaternary ammonium salts thereof, are disclosed which possess antihypertensive activity.

Abstract: The invention relates to a pharmaceutical composition comprising an anti-ulcer effective amount of a compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, phenyl, halophenyl, loweralkylphenyl, loweralkoxyphenyl, or aralkyl of 7 to 12 carbon atoms, R.sup.1 represents hydrogen or lower alkoxy, R.sup.2 represents hydrogen, chlorine or trifluoromethyl and n is 1 or 2, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable carrier.A method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula I is also disclosed. Some compounds of formula I are novel and within the scope of the invention.

Abstract: Novel cyanoguanidine derivatives having the formula ##STR1## wherein Ar is a phenyl or pyrrol-1-yl group substituted by one or more substituents selected from halogen, trifluoromethyl, lower alkyl, lower alkoxy and nitro and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen or lower alkyl or R.sub.1 and R.sub.2 taken together form dimethylene or trimethylene, lower blood pressure and, in some cases are also anti-ulcer agents.

Abstract: The invention concerns compounds of formula ##STR1## wherein the sulphur is bonded to the pyridinium ring at position 2 or 4, Y is --S-- or --CH.sub.2 --, R represents hydrogen, or a lower alkyl group, or other carboxylic protecting group; R.sup.1 represents hydrogen or lower alkyl; R.sup.2 represents lower alkyl, aryl of 6 to 10 carbon atoms or aralkyl of 7 to 11 carbon atoms; R.sup.3 represents hydrogen or a substituent selected from lower alkyl, halogen and lower alkoxy; q and r are each 1 or 2; and X.sup..crclbar. represents a halide ion or an organosulphonate ion, which are antihypertensive agents and are useful as intermediates to captopril and analogous compounds.

Abstract: 3-Aryl-3-aryloxyalkylamines of the general formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are hydrogen or lower alkyl, R.sup.3 is hydrogen, lower alkyl or benzyl, Ar is phenyl optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups, and Ar.sup.1 is methylsulphinyl, methylsulphonyl- or cyano-substituted phenyl, 2- or 4-pyridyl, 2-pyrazinyl, 2-quinolinyl, 2-thienyl or 2-thiazolyl exhibit activity on the central nervous system, e.g. as antidepressants.

Abstract: The invention concerns benzoquinolizines of the general formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein the ##STR2## linkage represents a single bond linkage of formula ##STR3## or a double bond linkage of formula ##STR4## R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 and R.sup.4 which may be the same or different each represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, di(lower)alkylamino or trifluoromethyl and X is O, S or NH. The compounds possess anti-secretory activity.

Abstract: The invention provides a compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, phenyl, halophenyl, loweralkylphenyl, loweralkoxyphenyl or aralkyl of 7 to 12 carbon atoms, R.sup.1 represents hydrogen or fluorine, R.sup.2 represents hydrogen, fluorine, chlorine or trifluoromethyl, n is 1 or 2 or pharmaceutically acceptable acid addition salt thereof.Pharmaceutical compositions containing the compounds are also covered as are methods of treating ulcers or hypersecretion using the compounds. Corresponding thiocompounds, useful as intermediates, are also disclosed.

Abstract: 4-Aryl-4-aryloxypiperidines of the general formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl, R.sup.3 is hydrogen, lower alkyl or benzyl, Ar is phenyl optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups and Ar.sup.1 is a phenyl radical optionally substituted by one or more cyano, methylsulphinyl, methylsulphonyl, lower alkoxy, trifluoromethyl, lower alkyl, lower alkenyl, halogen, nitro, amino or acylamino groups or an aromatic heterocyclic mono- or di-cyclic radical, exhibit activity on the central nervous system, e.g. as antidepressants.

Abstract: Novel benzoxazocines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 represents hydrogen, or one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro, amino acylamino, mono- or di- (lower)alkyl-amino or cyano substituents, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together represent --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, R.sup.5 represents hydrogen, lower alkyl, phenyl (lower)alkyl or cycloalkyl (lower)alkyl, and Ar is a phenyl radical optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups exhibit activity on the central nervous system, particularly as antidepressants. The compounds can be prepared from novel alcohols of formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Ar are as defined above and X is fluorine, chlorine or bromine.

Abstract: The invention relates to packages containing shaped articles carrying chemicals, particularly to pharmaceutical dosage forms carrying pharmaceuticals. The shaped articles, which disintegrate rapidly in water are contained in depressions in sheets of filmic material and are enclosed by a covering sheet adhering to the filmic material. The shaped articles may be formed in the depressions by a sublimation process.

Abstract: The invention concerns the treatment of ulcers and hypersecretion in a mammal using compounds of the formula IAr--A--S--Y Iwhere Ar is phenyl, which may be substituted or cycloalkyl of 5 to 7 carbon atoms, A is saturated or unsaturated lower alkylene which may be substituted by lower alkyl, oxo or hydroxy, S is sulphur and Y is an optionally substituted pyridine, pyridinium, tetrahydropyridine or tetrahydropyridinium radical. Certain novel compounds and pharmaceutical compositions are also disclosed.

Abstract: 2-Oxo-hexahydroazepine, -piperidine or pyrrolidines of formula ##STR1## wherein n is 2,3 or 4, R is hydrogen, lower alkyl, aryl(lower)alkyl, loweralkenylmethyl or cycloalkylmethyl, R.sup.1 is hydrogen or lower alkyl and R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl are prepared by a novel process involving reaction of an anion of a lactam of formula ##STR2## where R.sup.3 is lower alkyl, aryl(lower)alkyl, trialkyl-, triaryl- or triarylalkyl-silyl with a benzyne of formula ##STR3## where R.sup.4 is lower alkyl, aryl(lower)alkyl or trialkyl-, triaryl- or triarylalkyl-silyl. The products are useful as intermediates for preparing pharmacologically active 2-unsubstituted -hexahydroazepine, -piperidine and pyrrolidine derivatives.

Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable acid addition or quaternary ammonium salts thereof wherein the piperidine ring is substituted in the 3 or 4 position; X represents .dbd.CH-- or .dbd.N--; Y represents --NR.sup.5 --, --O-- or --S-- wherein R.sup.5 is hydrogen or lower alkyl; A is lower alkylene or hydroxy lower alkylene, Z and Z.sup.1 independently represent ##STR2## Z may also represent --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CHMe-- or --CMe.sub.2 --; R.sup.1, R.sup.2, R.sup.3 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, trifluoromethyl, lower-alkanoylamino, hydroxy or aryl lower alkoxy; or R.sup.1 and R.sup.2 when adjacent together with the carbons to which they are attached form a six membered carbocyclic ring; and R.sup.4 represents hydrogen or lower alkyl, are disclosed which possess psychotropic activity and are useful as anti-depressants.