Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is NH; or O when Ar is of formula (a) and R.sub.2 is hydrogen or when Ar is a group of formula (b);R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;Ar is a group of formula (a): ##STR2## wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are optional substituents; or Ar is a group of formula (b): ##STR3## wherein Z is CH.sub.2, O, S or NR.sub.7 wherein R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 alkenyl-methyl, phenyl or phenyl C.sub.1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl; and Y is CH or N; or Z is CH or N and Y is NR.sub.a or CHR.sub.a where R.sub.a is as defined for R.sub.7 above;R.sub.b is present when the COX linkage is attached at the phenyl ring, and is selected from hydrogen, halogen, CF.sub.3, hydroxy, C.sub.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof:Ar--CO--X--Y--Z--OR.sub.1 (I)wherein: Ar is a group of formula (a): ##STR1## wherein either R.sub.2 is C.sub.1-6 alkoxy and one of R.sub.3, R.sub.4 and R.sub.5 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, CX.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-6 alkoxy, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.2 is hydrogen and R.sub.3, R.sub.4 and R.sub.5 are independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or halo; or any two on adjacent carbon atoms together are C.sub.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen; either R.sub.1 is C.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O) n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;X is N or CR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1-6 alkoxy;Y is N or CR.sub.4 wherein R.sub.4 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;R.sub.1 and R.sub.2 are independently selected from hydrogen, or halogen;Z is a group of formula (a), (b) or (c): ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; andR.sub.5 or R.sub.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 1, 2, or 3; and m and p are independently 1 or 2 such that m+n+p.gtoreq.4;X is NH; or O when Ar is of formula (a) and R.sub.4 is hydrogen or when Ar is a heteroaromatic group which may be substituted;R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;Ar is a group: ##STR2## wherein either R.sub.4 is C.sub.1-6 alkoxy and one of R.sub.5, R.sub.6, and R.sub.7 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkyl or phenyl C.sub.

Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;X is a moiety capable of hydrogen bonding to the NH group depicted in formula (I);R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, carboxy, C.sub.1-6 alkoxycarbonyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.4-5 polymethylene; andZ is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; and R.sub.3 or R.sub.4 is C.sub.1-7 alkyl, C.sub.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkyl;R.sub.2 is amino or C.sub.1-7 acylamino;R.sub.3 is halo or C.sub.1-6 alkythio;R.sub.4 and R.sub.5 are independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-4 alkyl any of which phenyl moieties may be substituted by one or two of halo, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl, --(CH.sub.2).sub.s R.sub.7, s being 0 to 2 andR.sub.7 being C.sub.3-8 cycloalky, --(CH.sub.2).sub.t R.sub.8, t being 1 or 2 andR.sub.8 being thienyl or phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.

Abstract: Certain endo-9-lower-alkyl 9-azabicyclo[3.3.1]nonane-3-amines are valuable intermediates for the preparation of 2-methoxy-4-amino-5-halo-N-[9-lower-alkyl]-azabicyclo[3.3.1]nonanylbenzami des wherein said final products possess useful pharmacological activity, such as ability to regulate gastro-intestinal function, anti-emetic activity and CNS activity.

Abstract: A compound of formula (XXII): ##STR1## or a compound of formula (XXIII): ##STR2## wherein in formula (XXIII), j.sup.1 -1 is 1 to 4; and Q.sub.6 and Q.sub.7 are on the same carbon atom; and wherein, in formulae (XXII) and (XXIII), Q.sub.6 is NH.sub.2 and Q.sub.7 is H, and either p is 0 to 2 and q is 1; or p is 1 and q is 0 to 3; and one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl --C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen; and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, or N-oxide thereof, or a solvate of any of the foregoing: ##STR1## wherein p is 0 to 2; q is 0 to 3; j is 0 to 4;one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen;and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl; andA is of formula (II): ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 are each independently selected from hydrogen, halogen, CF.sub.3 C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 carboxylic acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.

Abstract: This invention relates to novel substituted benzamides having useful pharmacological properties, to pharmaceutical compositions containing them, to a process for their preparation and to intermediates therefor.N-(2-Diethylaminoethyl)-2-methoxy-4-amino-5-chlorobenzamide, 1-ethyl-2(2-methoxy-5-sulphamoylbenzamidomethyl)pyrrolidine and N-[4'-(1"-benzyl)-piperidyl]-2-methoxy-4-amino-5-chlorobenzamide are well known compounds having useful pharmacological activity such as the ability to regulate the gastro-intestinal function anti-emetic activity and CNS activity.It has now been found that certain intermediates for a structurally distinct class of substituted benzamides also has useful pharmacological activity, in particular dopamine antagonist activity.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, N-oxide or solvent adduct thereof: ##STR1## wherein: R.sub.1 is C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or, together with R.sub.5 is C.sub.1-2 alkylene, and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two together are C.sub.1-2 alkylenedioxy, or the other two are the same or different and are selected from the class of hydrogen, halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl hydroxy, nitro or amino, aminocarbonyl or aminosulphonyl optionally N-substituted by one or two C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, phenyl or phen C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.4-5 polymethylene, or R.sub.1 and R.sub.2 together are C.sub.1-2 alkylenedioxy, and R.sub.3 and R.sub.4 together are C.sub.1-2 alkylenedioxy or R.sub.3 and R.sub.

Abstract: Disclosed are compounds of the formulaR.sub.1 --Ar--(CH.sub.2).sub.a --X--(CH.sub.2).sub.b --NH--Hetwherein R.sub.1 is guanidino or substituted guanidino, Ar is furandiyl, thiophendiyl, phenylene, pyridinediyl, pyrimidinediyl, thiazolediyl, thiadiazolediyl or imidazolediyl; a is 0, 1 or 2; b is 2, 3, 4 or 5; and Het is a bicyclic heteroary group, and pharmaceutically acceptable salts, quaternized derivatives, N-oxides and solvates thereof. The compounds are useful for the treatment or prophylaxis of disorders relating to excess gastric acid secretion in mammals.

Abstract: A compound of the formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.2-7 acyl, C.sub.2-7 acylamino, or amino, aminocarbonyl or aminosulphone optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-6 alkylsulphone or nitro;R.sub.5 is hyrogen or C.sub.1-6 alkyl;R.sub.6 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.7 where s is 0 to 2 and R.sub.7 is a C.sub.3-8 cycloalkyl group, or a group --(CH.sub.2).sub.t R.sub.8 where t is 1 or 2 and R.sub.8 is C.sub.2-5 alkenyl or a phenyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and halogen; andn, p and q are independently 0 to 2; have useful pharmacological activity.

Abstract: Compounds of formula (I), pharmaceutically acceptable salts, quaternary derivatives and N-oxides thereof, and pharmaceutically acceptable solvates of any of the foregoing: ##STR1## wherein p is 1 to 3;B is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sub.11 where t is 1 or 2 and R.sub.11 is thienyl or furyl optionally substituted or is phenyl optionally substituted; and(i) A is a group of formula (II): ##STR2## in which either (a) one of X and Y is CO and the other is NH; or X is CO and Y is NR.sub.6 ; and or(b) one of X and Y is CO and the other is NH; or(ii) A is a group of formula (III): ##STR3## in which one of X and Y is CO and the other is NH, having useful pharmacological properties, pharmaceutical compositions containing them, a process and intermediates for their preparation, and the use of the compounds.

Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts and N-oxides thereof, wherein: R.sub.1 is a C.sub.1-6 alkoxy group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkyl-S(O).sub.n wherein n is 0, 1 or 2, nitro, C.sub.1-6 alkoxy, hydroxy, or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C.sub.1-6 alkyl groups;or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy in which case R.sub.3 is any one of the groups given for R.sub.1 and R.sub.2 above;R.sub.4 is hydrogen, C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl;R.sub.5 is hydrogen or C.sub.1-4 alkyl;X is an oxygen or sulphur atom; or a sulphoxide group >S.about.O;p is 1 or 2; andr is 1 or 2; are useful in the treatment of disorders related to imparied gastrointestinal motility.

Abstract: Substituted benzamides having useful pharmacological properties, pharmaceutical compositions containing the same, pharmaceutically acceptable salts thereof, and procedure for administering said compositions. The active compounds have dopamine antagonist activity which is an effective amount of a compound of formula (I) and the compositions are particularly useful for the treatment of humans suffering from emesis impaired gastro-intestinal motility and disorders of the central nervous system. The administration of the compositions overcomes these disorders of the central nervous system and ordinary additions. The active compounds are characterized by having the formula (I), wherein R.sub.2 and/or R.sub.3 are sulphone groups, preferably either R.sub.2 or R.sub.3 being an aminosulphone or alkylsulphone group, which groups may optionally be substituted by 1 or 2 C.sub.1-6 alkyl groups.

Abstract: This invention relates to novel substituted benzamides having useful pharmacological properties, to pharmaceutical compositions containing them, and to a process for their preparation.N-(2-Diethylaminoethyl)-2-methoxy-4-amino-5-chlorobenzamide, 1-ethyl-2(2-methoxy-5-sulphamoylbenzamidomethyl)pyrrolidine and N-[4'-(1"-benzyl)-piperidyl]-2-methoxy-4-amino-5-chlorobenzamide are well known compounds having useful pharmacological activity such as the ability to regulate the gastro-intestinal function anti-emetic activity and CNS activity.It has now been found that a certain structurally distinct class of substituted benzamides also has useful pharmacological activity, in particular dopamine antagonist activity.