Abstract: New 4-aminoquinoline derivatives having the formula ##STR1## wherein X is halogen or trifluoromethyl at the designated 7- or 8-position; Z is hydrogen, halogen, lower alkyl, lower alkoxy, nitro, di(lower alkyl)amino or trifluoromethyl, n is from 1 to 4, 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, and their pharmaceutically acceptable acid addition salts show anti-inflammatory activity.

Abstract: Compounds of formula ##STR1## in which X represents oxygen or sulphur;Y represents --CHOH-- or ##STR2## Z represents ##STR3## or a direct bond; R represents cycloalkyl group having 5 to 7 carbon atoms or an optionally substituted aryl or heteroaryl radical, or when --Z-- is a direct bond R also represents hydrogen;R.sup.1 represents hydrogen or lower alkyl.andR.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy;ora pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which reduce heart rate or have hyperglycaemic activity.

Abstract: The invention concerns benzoquinolizines of the general formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 and R.sup.2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen and R represents --CXNHR.sup.3 (where X is O, S or .dbd.NH and R.sup.3 is hydrogen or lower alkyl) or --(CH.sub.2).sub.n R.sup.4 (where n is 0 or 1 and R.sup.4 is aryl). These compounds lower blood pressure. Some are also anti-ulcer agents. The compounds in which R.sup.1, R.sup.2 and R are as defined above, with the proviso that when R is phenyl, R.sup.1 and R.sup.2 are not both lower alkoxy, are novel.

Abstract: Pyrrole derivatives of general formula (II) ##STR1## wherein R.sup.7 and R.sup.8 are the same or different and each represent hydrogen or lower alkyl, R.sup.13 and R.sup.14 are each hydrogen, lower alkyl or halogen with the proviso that at least one or R.sup.13 and R.sup.14 is halogen or (lower)alkyl, R.sup.15 and R.sup.16 are each hydrogen or lower alkyl and R.sup.17 is aryl or aryl(lower)alkyl are useful as hypotensive or antihypertensive agents.

Abstract: The invention provides a pharmaceutical composition in tablet form having an enteric coating and comprising 3-[2-(4-benzamido-1-piperidyl)ethyl]indole, embonate and a pharmaceutically acceptable carrier useful as a prolonged release antihypertensive formulation.

Abstract: The invention concerns a compound of formula II ##STR1## or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof wherein R.sup.5 represents hydrogen, hydroxy, lower alkoxy or lower alkyl, R.sup.6 represents hydrogen or lower alkyl, and R.sup.7 represents phenyl, lower alkoxy phenyl, halophenyl, or thenyl and X represents oxygen or sulphur. These indole derivatives exhibit psychotropic activity. The invention includes a method of alleviating depression in a warm blooded animal afflicted with depression which method comprises administering to said animal an effective amount of a compound of formula II or a pharmaceutically acceptable acid addition salt thereof.

Abstract: Compounds of formula ##STR1## in which hal represents halogen;R represents hydrogen or lower alkyl having 1 to 6 carbon atoms;R.sup.2 represents a subsituted or unsubstituted monocyclic heterocyclic group;and X represents oxygen or sulphur; or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which have hypotensive and/or antihypertensive activity.

Abstract: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine of formula I ##STR1## where n is 2,3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.1 is lower alkyl. The compounds may be aromatized and the aromatized compounds converted to 3,3-disubstituted-hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.

Abstract: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine derivatives of formula (I) and their aromatized derivatives of formula (II) ##STR1## where n is 2, 3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl, R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.3 is hydrogen, lower alkyl, aryl(lower)alkyl, lower alkenyl or lower alkynyl. The compounds are useful as intermediates for preparing 3,3-disubstituted -hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.

Abstract: The invention relates to copper complexes of 5,6,7,8-tetrahydroquinoline-8-thiocarboxamides. The copper complexes are of value in the treatment of ulcers and hypersecretion in mammals.

Abstract: (4,5-Diaryloxazol-2-yl)propionic and butyric acids having anti-inflammatory activity had previously been prepared by esterification of aroylarylcarbinols with a reactive derivative of butanedioic and pentanedioic acids, for instance, succinic or glutaric anhydride, isolation of the keto ester so formed and cyclization of the keto ester with a nitrogen-donating cyclizing agent, for instance, ammonium acetate in acetic acid. It has now been found that the omission of the isolation of the keto ester intermediate improves the purity of the oxazole product.

Abstract: The invention concerns novel benzoquinolizines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts. In formula (I) 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, lower alkyl, aryl or aryl(lower)alkyl or R.sup.3 and R.sup.4 together represent a tetra- or penta-methylene chain.The novel compounds of the invention lower blood pressure in warm-blooded animals.

Abstract: The invention relates to pharmaceutical compositions for use in treating ulcers or hypersecretion in mammals comprising a compound of formula Ia ##STR1## where Hal is a halogen atom, R.sup.1 is hydrogen or alkyl of 1-6 carbon atoms, R is hydrogen, alkyl of 1-5 carbon atoms (which may be substituted by two or more chlorine or bromine atoms), alkenyl of 2 to 5 carbon atoms, perfluoroalkyl of 1-5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms, R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or COR.sup.4 where R.sup.4 is as defined for R and R and R.sup.4 may be the same or different, and a pharmaceutically acceptable carrier.Methods of treatment of affected mammals and some novel compounds are also described.

Abstract: Novel 4-pyridinamine derivatives having the formula ##STR1## [where R.sup.1 and R.sup.2 are aryl or heteroaryl (optionally linked together by a lower alkylene bridge) or one of R.sup.1 and R.sup.2 is aryl or heteroaryl and the other of R.sup.1 and R.sup.2 is lower alkyl or ar(lower)alkyl, R.sup.3 and R.sup.4 are each hydrogen or lower alkyl and n is 0 or 1] and their non-toxic acid addition salts are described. They show CNS activity and may be used as antidepressant drugs. Some also show stimulant activity.Novel intermediates having the formula ##STR2## are also described.

Abstract: The invention provides compounds of general formula I ##STR1## and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein R represents hydrogen or lower alkyl, R.sup.1 represents hydrogen or lower alkyl, R.sup.2 represents hydrogen or lower alkyl, R.sup.3 represents hydrogen, halogen, lower alkoxy, hydroxy, or lower alkyl, R.sup.4 represents hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, thienyl, furyl, phenyl; phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy or trifluoromethyl; or benzoyl, halobenzoyl, lower alkanoyl, cycloalkanoyl of 6 to 8 carbon atoms, or thienoyl, A represents an alkylene, mono- or diketo- or hydroxy-alkylene radical having from 1 to 5 carbon atoms and X is oxygen or sulphur.The compounds exhibit action on the cardiovascular system particularly hypotensive and/or anti-hypertensive activity.

Abstract: The invention provides a new process for preparing indoles in which a 4-acylamido-1-[3-indolyl-alylene] pyridinium compound or a corresponding tetrahydropyridine compound is reduced with alkali metal borohydride in special solvents to give a corresponding piperidine compound.

Abstract: The invention relates to new tetrahydroquinoline derivatives which are intermediates useful in the preparation of anti-ulcer agents. The new derivatives have formula (I) ##STR1## wherein M is sodium, potassium or lithium, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or a lower alkyl, or a phenyl radical, and any of R.sup.4, R.sup.5 and R.sup.6 may be a gem-di-lower alkyl radical.

Abstract: The invention relates to pharmaceutical compositions for use in treating ulcers or hypersecretion in mammals comprising a compound of formula Ia ##STR1## WHERE Hal is a halogen atom, R.sup.1 is hydrogen or alkyl of 1-6 carbon atoms, R is hydrogen, alkyl of 1-5 carbon atoms (which may be substituted by two or more chlorine or bromine atoms), alkenyl of 2 to 5 carbon atoms, perfluoroalkyl of 1-5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms, R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or COR.sup.4 where R.sup.4 is as defined for R and R and R.sup.4 may be the same or different, and a pharmaceutically acceptable carrier.Methods of treatment of affected mammals and some novel compounds are also described.

Abstract: 4-Aryl-4-hydroxythiazolines can be obtained by treatment of aroylmethyl bromides with thiourea or a N-(lower alkyl)thiourea. The hydroxythiazolines are believed to have the formula ##STR1## where Ar is aryl and R is hydrogen or lower alkyl. The compounds are also capable of existing in open chain tautomeric form. The compounds show anti-ulcer activity in mammals.

Abstract: The invention concerns novel guanidine derivatives of the general formula (I) ##STR1## or pharmaceutically acceptable acid addition salts thereof, where.circle.Nrepresents ##STR2## wherein R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl, trifluoromethyl or halogen and R.sup.11 and R.sup.12 each represent hydrogen, lower alkyl, trifluoromethyl or halogen with the proviso that when one or both R.sup.11 or R.sup.12 groups represent halogen then R.sup.1 and R.sup.2 each represent lower alkyl, trifluoromethyl or halogen, R.sup.9 and R.sup.10 each represent hydrogen, lower alkyl or trifluoromethyl and R.sup.13 and R.sup.14 each represent hydrogen, lower alkyl, trifuoromethyl or halogen with the proviso that when one or both R.sup.13 and R.sup.14 groups represent halogen then R.sup.9 and R.sup.10 each represent lower alkyl or trifluoromethyl and R.sup.7 and R.sup.8 each represent hydrogen or lower alkyl and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each represent hydrogen or lower alkyl or R.sup.4 and R.sup.