Abstract: Compounds are described of the formulae (1a) and (1b) ##STR1## in which: --COR.sup.1 is an ester group,n is 1 or 2,W is C.sub.1-7 alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,Y is a saturated heterocyclic amino group,R.sup.2 is substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or cinnamyl, andR.sup.3 is --H or C.sub.1-5 alkanoyl, including their salts.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic or antiasthmatic agents.

Abstract: Compounds of the formula (I) ##STR1## in which R.sub.1 and R.sub.2 each may represent hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, or alkyl, substituted by hydroxy, C.sub.1-3 alkoxy, amino, C.sub.1-3 alkylamino or di-C.sub.1-3 alkylamino or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an alicyclic heterocyclic ring which may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom are described.Alk is a straight lower alkylene chain,Q is a furan or thiophen ring, the furan ring optionally bearing a further substituent R.sub.5 adjacent to the group R.sub.1 R.sub.2 NAlk-- or Q represents a benzene ring.R.sub.5 represents halogen or C.sub.1-3 alkyl which may be substituted by a hydroxy or C.sub.1-3 alkoxy group;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4;Y represents .dbd.O or .dbd.S;R.sub.3 represents hydrogen in which case R.sub.

Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.

Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the substituents are defined later.The compounds show pharmacological activity as selective histamine H.sub.2 -antagonists.

Abstract: The invention relates to a process for the preparation of ranitidine of formula (I) ##STR1## which comprises reacting a thiol of formula (II) ##STR2## with an alkylating agent of formula (III) ##STR3## The ethyleneimino derivative of formula (III) is a novel compound.

Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered alicyclic heterocyclic ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5-positions, the furan ring optionally bearing a further substituent R.sub.

Abstract: The invention relates to a process for the preparation of ranitidine of formula (I) ##STR1## which comprises reacting a thiol of formula (II) ##STR2## with an alkylating agent of formula (III) ##STR3## The ethyleneimino derivative of formula (III) is a novel compound.

Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans --CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturated heterocyclic amino group; andR.sup.4 is aralkyl (in which the aryl portion is substituted by alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoylamino, aroylamino, phenalkyl, aminosulphonyl, alkanoylaminosulphonyl, phenylsulphonyl, nitro, tetrazolyl, substituted phenyl or thienyl).These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.

Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, aralkyl, trifluoroalkyl, heteroaralkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkyamino or cycloalkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups, or a hydroxy group and/or may contain another heteroatom selected from oxygen and sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms and is attached to the cyclohexadiene ring at either the 4- or 5- position;X represents --CH.sub.2 or --O--;m represents 2, 3, 4 or 5 and when X is --O-- the chain (CH.sub.2).sub.

Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienylalkyl, naphthylalkyl or cinnamyl,and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstruction and may be formulated for use as antithrombotic and antiasthmatic agents.

Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which R.sub.4 represents hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, and R.sub.5 represents hydrogen or a C.sub.1-4 alkyl group or R.sub.4 and R.sub.5 may, together with the nitrogen atom to which they are attached, form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.

Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached from a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.

Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is C.sub.2-4 alkanoyl, C.sub.3-6 alkenyl (optionally substituted), C.sub.1-12 alkyl, or substituted or unsubstituted phenylalkyl, biphenylalkyl or naphthylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.

Abstract: The present invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and bioprecursors thereof in which ##STR2## represents either ##STR3## R.sup.1 represents hydrogen, halogen, C.sub.1-4 alkoxy, hydroxy, alkyl, R.sup.4 CH(OH)--, cyano or R.sup.5 CONH--, R.sup.2 and R.sup.3, which may be the same or different, each represents a straight or branched chain alkyl group or alkenyl group or R.sup.2 and R.sup.3 may, together with the nitrogen atom to which they are attached, form a saturated heterocyclic ring containing from 5 to 7 members which may optionally contain an oxygen atom; R.sup.4 represents hydrogen or alkyl; and R.sup.5 represents hydrogen, alkyl or C.sub.1-4 alkoxy. The compounds have been shown to exhibit H.sub.1 -antagonist activity in standard pharmacological tests.

Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same of different, each represent hydrogen, C.sub.1 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino alkylamino dialkylamino or cycloalkyl or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom which is oxygen or sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms,Q represents a furan or thiophene ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5- positions, the furan ring optionally bearing a further substituent R.sub.

Abstract: The invention relates to compounds of the formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2 represent hydrogen, an aliphatic or cycloaliphatic group, or R.sub.1 and R.sub.2 together with the nitrogen atom form a 5 to 10 membered heterocyclic ring:Alk represents a straight or branched alkylene chain;Q represents furan, thiophen or benzene ring which is incorporated into the rest of the molecule;X represents --CH.sub.2 --, ##STR2## --O-- or --S-- whereR.sub.6 represents hydrogen or methyl;n represents zero, 1 or 2;m represents 2, 3 or 4;R.sub.3 represents hydrogen, a substituted or unsubstituted aliphatic or aryl group and;R.sub.4 and R.sub.5, which may be the same or different, each represent hydrogen, a substituted or unsubstituted aliphatic, aryl, or together with the nitrogen atom form a heterocyclic group.

Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.

Abstract: Thiophene carboxamides are described of general formula I ##STR1## in which the amide function is in the 2- or 3-position on the thiophene ring, R.sub.1 to R.sub.5 inclusive are hydrogen atoms or lower alkyl groups, X is --CH.sub.2 --, --O-- or --NR.sub.6 -- where R.sub.6 is hydrogen or a lower alkyl group, n is a number from 0 to 3 and Ar is an optionally substituted phenyl groupand their physiologically acceptable salts.The compounds have been found to lower blood pressure in animals and to exhibit a blocking action at .beta.-adrenoreceptors and their use is indicated for the treatment of cardiovascular disorders such as hypertension and angina. Some of the compounds also exhibit a blocking action on .alpha.-adrenoreceptors and their use is indicated for the treatment of hypertention.

Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof,in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl;R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.

Abstract: The invention relates to compounds of the general formula ##STR1## and physiologically acceptable salts and N-oxides, hydrates and bioprecursors thereof, in which R.sub.1 and R.sub.2 which may be the same or different each represent hydrogen, C.sub.1-8 alkyl, C.sub.4-8 cycloalkyl, C.sub.3-6 alkenyl, aralkyl with 1 to 4 carbon atoms in the alkyl residue or C.sub.1-8 alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.5 represents hydrogen or C.sub.1-8 alkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached, form a saturated monocyclic 5 to 7 membered heterocyclic ring which may additionally contain the heterofunction O or ##STR3## R.sub.3 represents straight or branched chain C.sub.1-8 alkyl, alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue, C.sub.1-8 hydroxyalkyl, C.sub.1-8 alkoxycarbonyl, alkyl thioalkyl with 1 to 8 carbon atoms in each alkyl residue, halogen or aryl;R.sub.4 represents hydrogen, C.sub.1-8 alkyl, C.sub.