Abstract: Guanidines of formula ##STR1## and their pharmaceutically acceptable acid addition salts, (wherein R.sup.1 and R.sup.2 each represents lower alkyl or trifluoromethyl and R.sup.3 and R.sup.4 each represents hydrogen or lower alkyl or R.sup.3 and R.sup.4 together represent dimethylene or trimethylene) are useful in treating or preventing diarrhoea in mammals or poultry. The compound, if desired, may be administered with one or more antimicrobial, adsorbent, anti-emetic, parasympatholytic or antihistaminic agents.
Abstract: The invention concerns compounds of formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Ar represents an optionally substituted indolyl group; A represents a straight or branched chain alkylene or oxoalkylene group, each having 2-4 carbon atoms and R represents an optionally substituted aryl (including heteroaryl) group, which possess anti-hypertensive and psychotropic activity, and are useful in the treatment of high blood pressure or as anti-depressants.
Abstract: The invention provides a compound of the formula I ##STR1## wherein Y is a heterocyclic radical of formula ##STR2## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, hydroxy, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, loweralkoxy, halogen, formyl, phenyl, phenylalkyl, halophenyl, or acetal [CH(OR.sup.4).sub.2 where R.sup.4 is lower alkyl or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, the dotted lines in formula V represent an optional double bond in one of the indicated positions, A is a saturated or unsaturated alkylene radical having from 1 to 6 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and R.sup.3 is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms and Z.sup.- is an anion, and acid addition salts thereof, with the provisos that (1) when more than one R.sup.1 radical is present in the molecule then the R.sup.
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 pyridinum radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, e.g. where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.
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: 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, e.g. where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.
Abstract: Morpholine derivatives of the formula ##STR1## and their acid addition salts, wherein n represents 1, 2 or 3, R.sup.3 is alkyl of 1 to 10 carbon atoms, R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cyclo (lower)alkylmethyl and OR.sup.5 is hydroxy, acyloxy or a protected hydroxy group possess analgesic and/or opiate antagonistic activity or are useful as intermediates for other compounds of formula I possessing such activity.
Abstract: Xanthine derivatives are provided which exhibit psychotropic activity in that they inhibit 5-hydroxytryptamine reuptake in vitro and are indicated for antidepressive use.
Type:
Grant
Filed:
January 12, 1982
Date of Patent:
September 27, 1983
Assignee:
John Wyeth and Brother Limited
Inventors:
Terence J. Ward, Martyn D. Wood, Michael G. Wyllie
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: 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: 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.30 is a cation.
Abstract: Dihydropyridines of formula ##STR1## where R.sup.6 is lower alkyl and R.sup.5 is lower alkyl or aryl (lower)alkyl are prepared by a novel process from sodium or potassium salts of 1-substituted-1,6-dihydro-5-hydroxy-3[2H]-pyridones. The dihydropyridines are useful as intermediates for pharmacologically active 1-optionally substituted-3-phenyl or substituted phenylpiperidin-5-ols and esters. Some of the piperidinols and esters are novel; those where the 1-substituent is aryl(lower)alkyl are intermediates, those where the 1-substituent is cycloalkyl(lower)alkyl are analgesics or antidepressants and those in which the 1-position is unsubstituted are anti-secretory agents.
Abstract: Morpholine derivatives of the formula ##STR1## and their acid addition salts, wherein n represents 1, 2 or 3, R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cyclo(lower)alkylmethyl, R.sup.2 and R.sup.3 are each hydrogen or alkyl of 1 to 10 carbon atoms and OR.sup.5 is hydroxy, acyloxy or a protected hydroxy group possess analgesic and/or opiate antagonistic activity or are useful as intermediates for other compounds of formula I possessing such activity.
Abstract: The invention concerns compounds of formula ##STR1## or salts thereof, wherein R represents hydrogen which possess anti-inflammatory activity and have low toxicity. Methods for preparing the compounds and pharmaceutical compositions are also disclosed.
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 claimed.
Abstract: The invention relates to shaped articles carrying chemicals, particular to pharmaceutical dosage forms carrying pharmaceuticals, which disintegrate rapidly in water. The shaped articles comprise an open matrix network of carrier material carrying the chemical. The articles may be prepared by subliming solvent from a composition comprising the chemical and a solution of the carrier material in a solvent, the composition being in the solid state in a mould.
Type:
Grant
Filed:
July 17, 1981
Date of Patent:
February 1, 1983
Assignee:
John Wyeth & Brother Limited
Inventors:
George K. E. Gregory, James M. Peach, James D. Du Mayne
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, 5 is sulphur and Y is an optionally substituted pyridine, pyridinium, tetrahydropyridine or tetrahydropyridinium radical. Certain novel compounds and pharmaceutical compositions are also claimed.
Abstract: Morpholine derivatives of the formula ##STR1## and their pharmaceutically acceptable acid addition salts[wherein R.sup.1 represents lower alkyl. R.sup.2 represents hydrogen, lower alkyl, benzyl, lower alkoxymethyl or an acyl group; R.sup.3 represents hydrogen, lower alkyl or phenyl; R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, tetrahydrofurylmethyl or cycloalkylmethyl] possess analgesic and/or opiate antagonistic activity.