Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 - represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.

Abstract: Pyridine derivatives having the formula I ##STR1## and their pharmaceutically acceptable salts (where n is 0 or 1; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is an aromatic group) exhibit anti-secretory activity and may be used as anti-secretory agents and/or as anti-ulcer agents.

Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.

Abstract: The invention provides novel imidazoquinolines, processes for their preparation and pharmaceutical compositions containing them. The compounds have Formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,R.sup.1 and R.sup.2 are the same or different and are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyalkyl, C.sub.1-6 hydroxyalkyl, hydroxy, halogen, nitro, carboxy, carboxylic lower alkyl ester, carbamoyl, carbamoyloxy, cyano, loweralkanoyl, lower alkanoylamino or trifluoromethyl, Het is a heterocyclic group chosen from imidazolyl, imidazolinyl, benzimidazolyl, thiazolyl, thiazolinyl, quinolyl, piperidyl, pryidyl, benzothiazoly and pyrimidyl, any of which heterocyclic groups may be substituted, and x is 0 or 1, and pharmaceutically acceptable salts thereof.The compounds are anti-ulcer/anti-secretory agents.

Abstract: Compounds having the formula I ##STR1## and their pharamaceutically acceptable acid addition salts, wherein R.sub.1 is hydrogen or lower alkyl, A is a direct bond or lower alkylene and R.sub.2 is pyridinyl or pyridinyl monosubstituted by lower alkyl, are useful as anti-ulcer agents and, in the case where A is a direct bond, as anti-secretory agents.

Abstract: This invention relates to compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 independently represent hydrogen or a substituent selected from lower alkyl, lower alkoxy, halogen, alkanoyl of 2 to 7 carbon atoms, lower alkoxycarbonyl, halolower alkyl, hydroxy, cyano, amino, mono- or diloweralkyl amino, C.sub.2 -C.sub.7 alkanoylamino, carboxy, carboxylower alkyl, hydroxyloweralkyl, carbamoyl, carbamoyloxy, lower alkyl- or aryl-carbonyl, (lower alkoxy)-lower alkoxy, phenyl or a phenyl group itself optionally substituted by a substituent as hereinbefore defined excepting phenyl, or an adjacent pair of R.sup.1-4 together with the carbon atoms to which they are attached complete a six membered unsaturated carbocyclic or nitrogen containing heterocyclic ring, optionally substituted by one or more of the substituents listed above for R.sup.1 ; m represents 0 or 1; and R.sup.5, R.sup.6, R.sup.7 and R.sup.

Abstract: The invention provides a compound of formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,Ar is a phenyl or naphthyl group which may be substituted or unsubstituted,R.sup.1 and R.sup.2 are the same or different and are hydrogen, alkyl, alkoxy, alkoxyalkyl, hydroxyalkyl, hydroxy, halogen, nitro, carboxy, a carboxylic alkyl ester, carbamoyl, carbamoyloxy, cyano, acyl, acylamino or trifluoromethyl, or an acid addition salt thereof.The compounds are useful for the treatment of ulcers or hypersecretion in mammals. Pharmaceutical compositions containing the novel compounds and processes for their preparation are described.

Abstract: The invention concerns novel compounds of formula IIIAR.sub.x.sup.a Si(NCS).sub.4-x IIIAwherein R.sup.a is selected from electron donating substituents consisting of alkoxy of 1-10 carbon atoms, cycloalkoxy of 4-8 carbon atoms, aralkoxy of 7-12 carbon atoms, phenoxy which may be substituted by alkyl of 1-10 carbon atoms, alkoxy of 1-10 carbon atoms or trifluoromethyl, the group R.sup.b R.sup.c N-wherein R.sup.b and R.sup.c are selected from alkyl of 1-6 carbon atoms, cycloalkyl of 4-6 carbon atoms, phenyl which may be substituted by alkyl of 1-10 carbon atoms, alkoxy of 1-10 carbon atoms or trifluoromethyl, and aralkyl of 7-12 carbon atoms or R.sup.b and R.sup.

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 provides new silyl derivatives of 5,6,7,8-tetrahydroquinolines and related compounds. The tetrahydroquinolines are substiuted at the 8-position by the group SiR.sub.3 where R may be one of various hydrocarbon groups or an electron donating substituent. The 8-position may also carry a lithium, sodium or potassium atom. The new silyl derivatives may be prepared by treating a corresponding 8-lithio, sodio or potassio tetrahydroquinoline with a silyl halide R.sub.3 SiHal followed by a metal compound R*M where M is sodium, potassium or lithium and R* is alkyl, cycloalkyl, aralkyl or aryl or an amine residue. The new silyl derivatives are useful intermediates for the preparation of known 5,6,7,8-tetrahydroquinline-8-nitriles, amides and thioamides employing an alkyl silyl isothiocyanate or cyanate. The nitriles and thioamides are anti-ulcer agents. The related compounds may be made by analogous methods.

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: This invention concerns compounds of formula ##STR1## and acid addition salts thereof, wherein R represents lower alkoxy, alkanoyloxy of 2 to 7 carbon atoms or hydroxy;R.sup.1 and R.sup.2 independently represent hydrogen, lower alkoxy, alkanoyloxy of 2 to 7 carbon atoms, hydroxy or lower alkyl;R.sup.3, R.sup.4 and R.sup.5 each represent hydrogen or lower alkyl with the proviso that at least one of R.sup.3, R.sup.4 and R.sup.5 is lower alkyl;and R.sup.6 and R.sup.7 each represent hydrogen or lower alkyl which possess anti-ulcer activity.

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: An improved process for preparing fused carbocyclic ring derivatives of pyridine especially 5,6,7,8-tetrahydroquinoline 8-nitriles, amides and thioamides is described. The nitriles and thioamides are anti-ulcer and/or anti-secretory agents. Typically a compound of formula A ##STR1## wherein M is sodium, potassium, lithium or MgHal where Hal is chlorine, bromine or iodine, is reacted with a silyl compound R.sub.x.sup.a Si(NCY).sub.4-x III, wherein R.sup.a is selected from electron donating substituents, e.g. alkoxy or dialkylamino, and hydrocarbon substituents e.g. alkyl, at least one R.sup.a being an electron donating substituent, Y is oxygen or sulphur, x has a value from 1 to 3, then subjecting the product to hydrolysis or alcoholysis to obtain the corresponding nitrile, amide or thioamide, provided that when a nitrile is desired the molar ratio of compound III to compound A is at least 2:1 and x is 3 and Y is S. The products may be isolated as acid addition salts.

Abstract: The invention relates to the preparation of 1-bromo-2-D-alkylphopanoyl-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 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: 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.