Abstract: The present invention provides intermediates for the preparation of compounds of the formula wherein R, R1, W, X, Y, Ar and ZA are defined herein.

Abstract: Compounds of the formula (I): where X1, A, Ar1, X and R are as defined in the specification, and pharmaceutically-acceptable salts thereof, are new, and are useful as tachykinin inhibitors which act at the NK1, NK2 and NK3 receptors or a combination of two or more thereof.

Abstract: The present invention provides a compound of formula (I) wherein R is phenyl, C3-C7 cycloalkyl or heteroaryl, each of which being optionally benzo- or C3-C7 cycloalkyl-fused and optionally substituted, including in the benzo- or C3-C7 cycloalkyl-fused portion, by from 1 to 3 substituents each independently selected from C1-C4 alkyl, fluoro(C1-C4)alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, phenoxy, C2-C4 alkanoyl, halo, C1-C4 alkoxycarbonyl, C3-C7 cycloalkyl, —S(O)m(C1-C4 alkyl), cyano, —NR2R3, —S(O)mNR2R3, —NR4(C1-C4 alkanoyl) and —CONR2R3, or R is 2,3-dihydrobenzo[b]furanyl or chromanyl; R1 is H or C1-C6 alkyl; W is a direct link, methylene or ethylene; X is unbranched C2-C4 alkylene; Y is phenyl, naphthyl, benzyl, pyridyl, thienyl or C3-C7 cycloalkyl, each of which being optionally substituted by from 1 to 3 substituents each independently selected from C1-C4 alkyl, fluoro(C1-C4)alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, halo and cyano; Ar is phenyl, naphthyl, benzyl, th

Abstract: The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R.sup.1, m, n p are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.

Abstract: Selective muscarinic receptor antagonists of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are both optionally substituted phenyl, the broken line is an optional bond, X is >COH--, >SiOH-- or CH-- when the double bond is absent or is >C.dbd. when the double bond is present, X being attached to a carbon atom of A, A is selected from certain piperidine and pyrrolidine groups, n is 1 to 3 and R.sup.3 is optionally substituted phenyl or thienyl, pyridyl or pyrazinyl.

Abstract: A compound of the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup..sup.4, Y, m and n are defined herein are useful as muscarinic receptor antagonists.

Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.

Abstract: MUSCARINIC RECEPTOR ANTAGONISTS OF THE FOLLOWING FORMULAE: ##STR1## Muscarinic receptor antagonists, useful especially in the treatment of irritable bowel syndrome, of formula (IA) or (IB) or a pharmaceutically acceptable salt thereof, where R.sup.2 and R.sup.3 are each independently H, halo or C.sub.1 -C.sub.4 alkyl; m is 0, 1 or 2; n is 1, 2 or 3; Y is a direct link, O or S; with the proviso that when n is 1, Y is a direct link; Het is a group of formula (A) or (B), where p is 0, 1 or 2, q is 1, 2 or 3, and r is 0, 1, 2 or 3, with the proviso that the sum of p, q and r is at least 3, the N atom of "Het" being attached to the group (CH.sub.2).sub.n in formula (IA) and to the H atom in formula (IB); and R.sup.1 is a group of formula (a), (b) or Het.sup.1, where R.sup.4 and R.sup.5 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.t OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.t NR.sup.6 R.sup.7, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.

Abstract: Compounds of formula (1), wherein X is CH or N; Z is CH.dbd.CH or S; A is CH.sub.2 CH.sub.2, CH.dbd.CH, CH(OH)CH.sub.2, or COCH.sub.2 ; B is a direct link or --CH.sub.2 --, --CH(CH.sub.3)-- or --C(CH.sub.3).sub.2 --; or when Z is CH.dbd.CH, B may form a cyclopentane ring fused to the attached benzene ring; Y completes a fused benzo or thienyl ring which is optionally substituted by halo or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2; and m is 0 or 1; are antagonists of both PAF and histamine H.sub.1 having utility in the treatment of allergic inflammatory conditions such as allergic rhinitis.

Abstract: According to the invention there is provided a compound of formula (I): R.sup.1 --O(CH.sub.2).sub.m A(CH.sub.2).sub.n XR or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is a group of formula (a or b) where Z is --(CH.sub.2).sub.2-, --CH.dbd.CH--, --CH.sub.2 --S-- or --CH.sub.2 --O--; R is a group of formula (c, d or Het) and A is a group of formula (e, f or g) in which the N atom is attached to the group (CH.sub.2)n; m is 1 or 2; n is an integer of from 1 to 4; p is 1, 2 or 3; R.sup.2 and R.sup.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy-(C.sub.1 -C.sub.4 alkyl), hydroxy, C.sub.1 -C.sub.4 alkoxy, halo, trifluoromethyl, nitro, cyano, sulphamoyl, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), carboxy, --CO.sub.2 (C.sub.1 -C.sub.4 alkyl), --CH.sub.2).sub.q CONR.sup.4 R.sup.5, -- (CH.sub.2).sub.q OCONR.sup.4 R.sup.5, --CH.sub.2).sub.q NR.sup.6 R.sup.7 or --NHSO.sub.2 NH.sub.2 in which R.sup.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.

Abstract: A series of novel 1-(phenethyl) and 1-(2-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone.

Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.

Abstract: A series of novel 1-(phenethyl) and 1-(1-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone. The most preferred compound is (3R)-diphenylmethoxy-1-(3,4-methylenedioxyphenethyl)piperidine. Methods for preparing these compounds from known starting materials are provided.

Abstract: The invention provides compounds of the formula: ##STR1## wherein k is 1, 2 or 3;m is 1, 2 or 3;n is 1, 2 or 3;p is 0, 1 or 2;X is O, S or a direct link, with the proviso that when X is O or S, n is 2 or 3;R.sup.1 is H or C.sub.1-C.sub.4 alkyl; andR.sup.2 is an optionally substituted phenyl or heteroaryl group; andpharmaceutically acceptable salts thereof.These compounds are useful for the treatment of motility disorders, particularly those of the gut such as irritable bowel syndrome.

Abstract: Dihydropyridines having unsaturated side chains are disclosed. The compounds are useful anti-ischemic and antihypertensive agents.

Abstract: 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.

Abstract: 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.

Abstract: Compounds of the formula: ##STR1## where R is an optionally substituted aryl or heteroaryl group;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; and Y is --(CH.sub.2).sub.n -- where n is 2, 3 or 4, --CH.sub.2 CH(CH.sub.3)-- or --Ch.sub.2 C(CH.sub.3).sub.2 --; and their pharmaceutically acceptable salts.The compounds have utility as anti-ischaemic and antihypertensive agents and as synthetic intermediates to other dihydropyridine calcium antagonists.

Abstract: Dihydropyridine derivatives of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts; wherein R is a substituted aryl group;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.3 alkyl;Y is --(CH.sub.2).sub.n -- where n is 2, or --CH.sub.2 CH(CH.sub.3)--; and Het is a 6-membered aromatic heterocyclic group attached to the adjacent oxygen atom by a carbon atom.The compounds have utility as anti-ischaemic and anti-hypertensive agents.