Burroughs Wellcome Co.

Other

Peter B Thorogood

Jeremy G Vinter

Compounds of the formula: ##STR1## wherein R is (Hal).sub.m wherein Hal represents a halogen atom and m is 1 or 2, or R is-(B.sup.1).sub.n1 W.sup.1 wherein B.sup.1, n.sup.1 and W.sup.1 are as defined below;

Imidazole derivatives, compositions and use

Pharmaceutical formulations comprising an imidazole (or pharmaceutically acceptable salt thereof) of formula: ##STR1## wherein (i) A is an aliphatic hydrocarbon residue of from 1 to 4 carbon atoms and R is a naphthyl, tetrahydronaphthyl, heterocyclyl, arylthio, arylalkylthio, aryloxy, arylalkyloxy, arylhydroxymethylene, arylcarbonyl, arylalkylcarbonyl, alkyloxy, alkylthio or a substituted cycloalkyl or cycloalkenyl group or

Imidazole derivatives and salts thereof, their synthesis and

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; or

Prevention of thrombolic disorder with imidazole derivatives and salts

A method for (i) the treatment or prophylaxis of a thrombo-embolic disorder of a mammal or a mammalian tissue (ii) the prevention, treatment or prophylaxis of angina pectoris, or (iii) the prevention or delay of the onset of shock, which comprises the administration to the mammal or mammalian tissue of a non-toxic, effective amount of an imidazole of the formula: ##STR1## in which A is a straight or branched, saturated or unsaturated acyclic hydrocarbon radical of from 1 to 3 carbon atoms, n is 0 or 1, and R is ##STR2## wherein m is 0 or an integer which is at least 1 and the or each Q substituent, which, when m is greater than 1 may be the same or different is selected from a saturated or unsaturated hydrocarbon group of from 1 to 4 carbon atoms; alkoxy of from 1 to 4 carbon atoms; nitro; phenyl; acyloxy; halo; trihalomethyl; hydroxy; carboxyl; a salt of such a carboxyl group; carboalkyloxy; carboaryloxy; carboarylalkyloxy; --NR.sup.6 R.sup.7 and --CONR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 may be the same or different and are each hydrogen or alkyl of from 1 to 4 carbon atoms; the imidazole being the free base or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations of some inidazoles within the class suitable for use in the method of treatment are also novel. Methods of preparing the imidazoles are provided.

1-[3-(2,4-Dichlorophenyl)propyl]imidazole and salts thereof

1-Substituted-imidazoles of the formula: ##STR1## in which A is selected from the group consisting of straight or branched, saturated or unsaturated, acyclic hydrocarbon radicals of from 1 to 3 carbon atoms and R is ##STR2## wherein n is an integer which is at least 1, and the or each Q substituent, which when n is greater than 1 may be the same or different, is selected from a saturated alkyl group of from 1 to 4 carbon atoms or an unsaturated alkyl group of from 2 to 4 carbon atoms, with the proviso that when A is unsaturated Q may also be selected from alkoxy of from 1 to 4 carbon atoms; halo; trihalomethyl; hydroxy; carboxyl; a salt of such a carboxyl group; carboalkyloxy; carboaryloxy; carboarylalkyloxy; --NR.sup.6 R.sup.7 or --CONR.sup.6 R.sup.7 ; in which R.sup.6 and R.sup.7 may be the same or different and are hydrogen or alkyl of from 1 to 4 carbon atoms; the 1-substituted-imidazole being the free base or an acid addition salt thereof. Methods of preparing the 1-substituted-imidazoles are also provided. The imidazoles have pharmacological properties that make them of use in the treatment of thromboembolic disorders, shock and angina pectoris.

Imidazole derivatives and salts thereof, their synthesis, and

Imidazole derivatives for treating myocardial infarction

Imidazole derivatives and salts thereof

Imidazole derivatives and angina pectoris

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 heteroatoms

Imidazole derivatives and salts thereof and pharmaceutical formulations

The invention relates to a class of imidazoles substituted by cycloalkyl or cycloalkenyl which have pharmacological properties making them useful in medicine, in particular in the prophylaxis and treatment of thrombo-embolic disorders, and also of shock and angina pectoris.

Treatment of shock

The invention relates to a class of imidazoles substituted by cycloalkyl or cycloalkenyl which have pharmacological properties making them useful in medicine, in particular in the prophylaxis and treatment of thrombo-embolic disorders.

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London, United Kingdom

Peter B Thorogood