Abstract: Heterocyclic thromboxane synthetase inhibitors of the formula ##STR1## wherein R.sup.1, which is attached to the 2-, 3- or 4-position, is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, hydroxy or C.sub.1 -C.sub.4 alkoxy;Y, which is attached to the 2- or 3-position, is --COOH, --COO(C.sub.1 -C.sub.4 alkyl) or --CONH.sub.2 ;X is O, S, NH, N(C.sub.1 -C.sub.4 alkyl) or N(benzyl); andR, which is attached to the 5-, 6- or 7-position, is a group of the formula ##STR2## or (3- or 4-pyridyl)--Z.sup.2 -- wherein Z.sup.1 is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 O-- and Z.sup.2 is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O-- or --OCH.sub.2 --;and their pharmaceutically acceptable salts; processes for their preparation, and pharmaceutical compositions containing them which are useful, for example, in the treatment of thrombosis.

Abstract: Dihydropyridine anti-ischaemic and anti-hypertensive agents of the formula: ##STR1## and their pharmaceutically acceptable salts; wherein R is aryl or heteroaryl; R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 or 2-methoxyethyl; n is 1 or 2; m is 1, 2 or 3; X is a 5 or 6 membered aromatic heterocyclic group which is linked to the adjacent alkoxymethyl group by a ring carbon atoms thereof; and Z is a group--NR.sup.3 R.sup.4 or a 5 to 6 membered nitrogen containing heterocyclic group; where R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; R.sup.4 is H, C.sub.1 -C.sub.4 alkyl, CO(C.sub.1 -C.sub.4 alkyl), COCF.sub.3, CONR.sup.5 R.sup.6, SO.sub.2 (C.sub.1 -C.sub.4 alkyl) or a heterocyclic or SO.sub.2 -heterocyclic group, wherein the heterocyclic group is optionally substituted; R.sup.5 and R.sup.6 and each independently H or C.sub.1 -C.sub.4 alkyl or taken together with the nitrogen atom to which they are attached, they form a pyrrolidinyl, piperidyl, morpholino, piperazinyl or N-(C.sub.1 -C.sub.

Abstract: 1,4-Dihydropyridine derivatives of the formula ##STR1## and their pharmaceutically acceptable acid addition salts; where:R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or2-methoxyethyl;Y is --(CH.sub.2).sub.2 --, --CH.sub.2).sub.3 --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --;R.sup.3 is ##STR2## , and pharmaceutical compositions containing such compounds, have utility as anti-ischaemic and antihypertensive agents.

Abstract: 1,4-Dihydropyridine derivatives of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts; where R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or2-methoxyethyl;Y is --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --;R.sup.3 is hydrogen or an organic substituentare useful in treating or preventing heart conditions or hypertension.

Abstract: 1,4-Dihydropyridine derivatives of the formula: ##STR1## wherein R is aryl or heteroaryl; R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; Y is --(CH.sub.2).sub.n --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 13 ; n is 1 to 3; and X is a 5 or 6 membered nitrogen containing aromatic heterocyclic ring which may optionally be substituted by one or more C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, CN, --N(R.sup.3).sub.2, (CH.sub.2).sub.m CO.sub.2 H, (CH.sub.2).sub.m CO.sub.2 (C.sub.1 -C.sub.4 alkyl) or (CH.sub.2).sub.m CON(R.sup.3).sub.2 group wherein each R.sup.3 is independently H or C.sub.1 -C.sub.4 alkyl and m is 0 or 1; and their pharmaceutically acceptable acid addition salts, and pharmaceutical preparation containing such compounds, have utility as anti-ischaemic and antihypertensive agents.

Abstract: A novel series of carboxy-substituted naphthalenes and carboxy-substituted benzo-fused heterocycles, such as carboxy-substituted derivatives of indole, benzofuran and benzothiophene, has been prepared, including their pharmaceutically acceptable salts. These particular compounds are useful in therapy for the treatment of thrombosis, ischaemic heart disease, stroke, transient ischaemic attack, migraine, peripheral vascular disease, the vascular complications of diabetes and endotoxic shock. Preferred member compounds include 2-(1-imidazolylmethyl)-3-methylbenzo[b]thiophene-5-carboxylic acid and 3-methyl-2-(3-pyridylmethyl)benzo[b]thiophene-5-carboxylic acid, respectively. Methods for preparing these compounds from known starting materials are provided.

Abstract: A series of novel 3-(1-imidazolylmethyl)indolylacrylic acid and 3-(3-pyridylmethyl)indolylacrylic acid derivatives has been prepared, including their pharmaceutically acceptable acid addition and base salts. These particular compounds are useful in therapy for the treatment of thrombosis, ischaemic heart disease, stroke, transient ischaemic attack, migraine, and the vascular complications of diabetes. Preferred member compounds include E-3-{1-[2-methyl-3-(1-imidazolylmethyl)]indolyl}-acrylic acid and E-3-{1-[2-methyl-3-(3-pyridylmethyl)]-indolyl} acrylic acid, respectively. Methods for preparing these compounds from known starting materials are provided.

Abstract: The N-(substituted benzyl) imidazoles are selective enzyme inhibitors and thus are useful in the treatment of heart disease, circulatory and vascular problems.

Abstract: Dihydropyridine anti-ischaemic and antihypertensive agents of the formula: ##STR1## where Y is --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 --;R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl;andR.sup.3 and R.sup.4 are each independently C.sub.1 -C.sub.4 alkyl or aryl-(C.sub.1 -C.sub.4 alkyl); or R.sup.3 and R.sup.4 taken together with the nitrogen atom to which they are attached represent a group of the formula: ##STR2## where R.sup.5 is C.sub.1 -C.sub.4 alkyl, aryl, aryl-(C.sub.1 -C.sub.4 alkyl), benzhydryl; 2-methoxyethyl, 2-(N,N-di[C.sub.1 -C.sub.4 alkyl]amino) ethyl, or cyclopropylmethyl;their pharmaceutically acceptable acid addition salts, processes for the preparation of the compounds, and pharmaceutical compositions containing them.

Abstract: Heterocyclic thromboxane synthetase inhibitors of the formula ##STR1## wherein R.sup.1, which is attached to the 2-, 3- or 4-position, is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, hydroxy or C.sub.1 -C.sub.4 alkoxy;Y, which is attached to the 2- or 3-position, is --COOH, --COO(C.sub.1 -C.sub.4 alkyl) or --CONH.sub.2 ;X is O, S, NH, N(C.sub.1 -C.sub.4 alkyl) or N(benzyl); andR, which is attached to the 5-, 6- or 7-position, is a group of the formula ##STR2## or (3- or 4-pyridyl)-Z.sup.2 - wherein Z.sup.1 is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 O-- andZ.sup.2 is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O-- or --OCH.sub.2 --;and their pharmaceutically acceptable salts; processes for their preparation, and pharmaceutical compositions containing them.

Abstract: A series of novel 3-(pyrid-3- or -4-ylalkyl)-indoles useful as inhibitors of the action of the thromboxane synthetase enzyme without significantly inhibiting the action of the prostacyclin synthetase or cyclo- oxygenase enzymes is disclosed.

Abstract: Compounds of the general formula: ##STR1## wherein X is a group of the formula: ##STR2## m is 2 or 3; n is an integer of from 1 to 4; and R is a 5-membered heterocyclic group containing as heteroatoms a nitrogen atom and an additional oxygen or sulphur atom or up to three further nitrogen atoms; or a 6-membered heterocyclic group containing one or two nitrogen atoms;and the pharmaceutically acceptable acid addition salts thereof, are able to selectively inhibit the action of the thromboxane synthetase enzyme without significantly inhibiting the action of the prostacycline synthetase or cyclo-oxygenase enzymes and are thus useful in the treatment of ischaemic heart disease, stroke, transient ischaemic attack, thrombosis, migraine and the vascular complications of diabetes.

Abstract: Heterobicyclic glyoxylic acids, L- and DL-heterobicyclic glycines and their derivatives of the formulae ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein R is OR.sup.2 or NHR.sup.3 ;R.sup.2 is hydrogen or alkyl having from one to four carbon atoms;R.sup.3 is hydrogen, alkyl having from one to four carbon atoms, alkoxyalkyl having from one to four carbon atoms in each of the alkyl groups or R.sup.4 R.sup.5 C.sub.6 H.sub.3 CH.sub.2 -- where R.sup.4 and R.sup.5 are H, OH, F, Cl, Br, I, or alkyl or alkoxy having from one to four carbon atomsR.sup.1 is hydrogen, alkyl having from one to four carbon atoms or R.sup.4 R.sup.5 C.sub.6 H.sub.3 --; X is oxygen or sulfur; n is 0 or 1 and the broken line represents an optionally present double bond; useful in treatment of diseases and conditions which are characterized by reduced blood flow, reduced oxygen availability or reduced carbohydrate metabolism in the cardiovascular system.

Abstract: Certain 2-(1-imidazolylmethyl)pyridine compounds, having a further substituent O--Y--Z at the 3- or 5-position of the pyridine ring. Y is --(CH.sub.2).sub.n --, --CH.sub.2 C.sub.6 H.sub.4 --, or --CH.sub.2 (Het)--, where n is an integer from 1 to 4 and Het is a heterocyclic group; Z is a carboxy (COOH) or carboxycarbonyl (COCOOH) group, or an ester or amide derivative thereof. The compounds of the invention selectively inhibit the thromboxane synthetase enzyme, without significantly inhibiting the action of the prostacyclic or cyclo-oxygenase enzymes in animals, including man. The compounds are useful, therefore, in the treatment of thrombosis, ischaemic heart disease, stroke, transient ischaemic attack, migraine and the vascular complications of diabetes.

Abstract: Derivates of L- and DL-hydroxyphenylglycines of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl, R.sup.1 is hydrogen, amino or alkoxy having from one to six carbon atoms and R.sup.2 is the residue of certain .alpha.-amino acids are useful in treating diseases and conditions which are characterized by reduced blood flow, oxygen availability or carbohydrate metabolism in the cardiovascular system. Derivatives of D-hydroxyphenylglycine of formula (II) are substantially inactive in treating such diseases and conditions.

Abstract: Novel 3-(1-Imidazolylalkyl)indoles and the pharmaceutically acceptable acid addition salts thereof are disclosed. The novel compounds are useful in selectively inhibiting the action of the thromboxane synthetase enzyme without significantly inhibiting the action of the prostacycline synthetase or cyclooxygenase enzymes and are thus of value as therapeutic agents for the treatment of ischaemic heart disease, stroke, transient ischaemic attack, thrombosis, migraine and the vascular complications of diabetes.

Abstract: Novel 2-(Imidazol-1-ylmethyl)pyrroles and pharmaceutically acceptable acid addition salts thereof are disclosed. The novel compounds are useful in selectively inhibiting the action of the thromboxane synthetase enzyme.

Abstract: 5-Substituted 2-pyrroleglyoxylic acids, L- and DI-5-substituted 2-pyrrolylglycines and their derivatives of the formulae ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein R is hydrogen or alkyl having from one to four carbon atoms;R.sup.1 is alkyl or alkylthio having one to ten carbon atoms, alkenyl having from three to six carbon atoms, cycloalkylthio having from five to seven carbon atoms or AR.sup.3 where A is a member bonded to the pyrrole ring and is alkylene or alkylenethio having from one to four carbon atoms or alkenylene having from two to four carbon atoms and R.sup.3 is cycloalkyl having from three to seven carbon atoms, cycloalkenyl having from five to seven carbon atoms or C.sub.6 H.sub.4 R.sup.4 where R.sup.4 is H, F, Cl, Br, I, alkyl or alkoxy, the latter two groups each having from one to four carbon atoms;R.sup.

Abstract: The use of phenylglyoxylic acids and derivatives thereof in the treatment of ischemic heart disease and the hyperglycemia of diabetes.

Abstract: A series of 2-(imidazol-1-ylmethyl)pyridines and 2-(imidazol-1-ylmethyl)quinolines has been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy for the treatment of ischaemic heart disease, migraine, transient ischaemic attack and stroke. Preferred member compounds include 2-(imidazol-1-ylmethyl)-3-methoxypyridine, 2-(imidazol-1-ylmethyl)-3-methoxy-6-methylpyridine and 2-(imidazol-1-ylmethyl)-3-benzyloxypyridine, respectively. Alternate methods of preparation are provided and the principal synthetic routes leading to the preferred compounds are described in some detail.