Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: A class of 1,4-disubstituted piperazine derivatives, further substituted on one of the carbon atoms of the piperazine ring, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: A class of 1,2,3,6-tetrahydropyridine derivatives, substituted in the 4-position by a fused bicyclic heteroaromatic moiety and in the 1-position by an optionally substituted benzyl moiety, are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.

Abstract: A class of substituted 3-fluoro-4-aminopiperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.sbsb..alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.sbsb..alpha. receptor subtype relative to the 5-HT.sub.1D.sbsb..beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: The present invention provides compounds of formula (I), wherein R.sup.1 is a 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms selected from nitrogen, oxygen and sulphur, which group is optionally substituted; R.sup.2 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3, OCF.sub.3, NO.sub.2, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.1-4 alkyl substitued by C.sub.1-4 alkoxy, where R.sup.a and R.sup.a R.sup.b each independently represent hydrogen or C.sub.1-4 alkyl; R.sup.3 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 -alkoxy substituted by C.sub.1-4 alkoxy or CF.sub.3 ; R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, A, X and Y are as defined in the specification; and m is zero or , and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and pos therpetic neuralgia.

Abstract: Tachykinin receptor antagonists are useful for the treatment of cystic fibrosis.

Abstract: The present invention relates to compounds of formula (I) ##STR1## wherein X is --NR.sup.6 R.sup.7 or C-- or N-linked imidazolyl; Y is hydrogen or C.sub.1-4 alkyl optionally substituted by hydroxy; R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are selected from a variety of suitable aromatic substituents; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2-4 alkyl substituted by C.sub.1-4 alkoxy or hydroxy; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, or C.sub.2-4 alkyl substituted by one or two of C.sub.1-4 alkoxy, hydroxy or a 4, 5 or 6 membered heteroaliphatic ring containing one or two heteroatoms selected from N, O and S; or NR.sup.6 R.sup.7 is a saturated or partially saturated heterocyclic ring of 4 to 7 ring atoms, optionally containing one of O, S, NR.sup.8, S(O) or S(O).sub.2 and optionally substituted by one or two of hydroxy.sub.1-4 alkyl, C.sub.1-4 alkoxy C.sub.

Abstract: Compound of formula (I), or a pharmaceutically acceptable salt thereof or a prodrug thereof wherein E represents --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --; R represents hydrogen or C.sub.1-6 alkyl; Q represents a moiety of formula Qa, Qb, Qc or Qd which are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D.sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.

Abstract: The present invention relates to compounds of formula (I), wherein n is zero, 1, 2 or 3; R represents C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halogen, cyano, trifluoromethyl SO.sub.2 C.sub.1-6 alkyl, NR.sup.a R.sup.b, NR.sup.a COR.sup.b or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are each H, C.sub.1-4 alkyl, phenyl or trifluoromethyl; R.sup.1 represents phenyl optionally substituted by 1, 2 or 3 of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, --O(CH.sub.2).sub.p O-- (where p is 1 or 2), halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR.sup.a, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, NR.sup.a R.sup.b, NR.sup.a COR.sup.b, NR.sup.a CO.sub.2 R.sup.b, COR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; naphthyl; benzhydryl; or benyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or trifluoromethyl; R.sup.

Abstract: The present invention relates to compounds of the formula (I) ##STR1## wherein X, Z, R, R.sup.1, R.sup.2, Ar, n and m are as defined herein which are of use in the treatment or prevention of neuropathy, asthma, osteoarthritis, rheumatoid arthritis or migraine.

Abstract: Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1 to 6 carbon atoms, optionally substituted in any position by a hydroxy group; T represents nitrogen or CH; U represents nitrogen or C--R.sup.2 ; V represents oxygen, sulphur or N--R.sup.3 ; --F--G-- represents --CH2--N--, --CH2--CH-- or --CH.dbd.C--; R.sup.1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, any of which groups may be optionally substituted; and R.sup.2 and R.sup.3 independently represent hydrogen or C.sub.

Abstract: A class of benzimidazole derivatives, substituted at the 2-position by a substituted piperazinylmethyl or piperazinylethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D.sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.

Abstract: The present invention relates to a method for the synthesis of 1,3-disubstituted quinazolinedione derivatives which comprises:(a) reacting a haloformate functionalized polystyrene resin with a substituted anthranilic acid derivative under conditions effective to form a urethane-linkage;(b) reacting the product of step (a) with a primary amine under conditions effective to form an anthranilamide derivative;(c) heating the anthranilamide to effect intramolecular cyclization thereby liberating the 1,3-disubstituted quinazolinedione derivative from the resin into solution; and(d) isolating the 1,3-disubstituted quinazolinedione by filtration and solvent removal.

Abstract: Disclosed is a class of 1H-indazole derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, which are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D4 receptor subtype over other dopamine receptor subtypes, and are accordingly, of benefit in the treatment and/or prevention of psychotic disorders, such as schizophrenia, while manifesting fewer side-effects than those associated with classical neuroleptic drugs.

Abstract: A class of substituted pyrimidine derivatives are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular schizophrenia ##STR1##

Abstract: The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, A.sup.1, A.sup.2, X, m and n are defined herein. The compounds of this invention are tachykinin receptor antagonists and are of particular use in the treatment of pain, inflammation, migraine and emesis.

Abstract: The present invention relates to compounds of formula (I): wherein X is N or CH; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of p articular use in the treatment of pain, inflammation, migraine and emesis.

Abstract: Aralkylamino substituted azacyclic compounds of formula (I) and their salts and prodrugs. The variables are defined herein. The compounds are useful as tachykinin antagonists and are of particular use in the treatment of pain, inflammation, migraine, and emesis.

Abstract: The present invention relates to spiroketal derivatives of formula (I) and pharmaceutically acceptable salts thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, m and n are as defined in the specification, and to processes for their preparation, to intermediates used in their synthesis, to pharmaceutical compositions containing them, and to their use in therapy. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

Abstract: The present invention relates to compounds of formula (I) wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are selected from a variety of suitable aromatic substituents; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2 -alkyl substituted by C.sub.1-4 alkoxy or hydroxy; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, C.sub.2-4 alkyl substituted by C.sub.1-4 alkoxy or hydroxy, or the group C(.dbd.NR.sup.c)NR.sup.a R.sup.b ; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, form an optionally substituted saturated heterocyclic ring of 4 to 7 ring atoms which may optionally contain in the ring one oxygen or sulphur atom or a group selected from NR.sup.8, S(O) or S(O).sub.2 ; or R.sup.6 and R.sup.