Abstract: The present invention relates to compounds of formula (I) ##STR1## wherein X is a 5- or 6-membered C-linked heteroaromatic ring containing 1 to 4 nitrogen atoms and optionally containing in the ring one oxygen or sulphur atom; Y is a group of the formula --(CH.sub.2).sub.n NR.sup.6 R.sup.7 or a methylene- or ethylene-linked imidazolyl group; Z is hydrogen or C.sub.1-4 alkyl optionally substituted by a hydroxy group; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.9a and R.sup.9b are a variety of substituents; R.sup.6 is hydrogen, C.sub.1-6 akyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, or C.sub.2-4 akyl 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, or C.sub.2-4 alkyl substituted by one or two substituents selected from 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 R.sup.6 and R.sup.

Abstract: The subject N-(2-benzyloxy-1-phenethyl)-N-(2'-methoxyethyl)amino-methane compounds of the formula: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and Het are defined herein) are tachykinin receptor antagonists which are useful in the treatment of pain, inflammation, migraine and emesis.

Abstract: The present invention provides methods for the treatment or prevention of mania or hypomania which comprises administration of a NK-1 receptor antagonist, optionally with an antipsychotic agent, and pharmaceutical compositions containing a NK-1 receptor antagonist.

Abstract: The present invention provides methods for the treatment or prevention of bipolar disorder without concomitant therapy with other antidepressant or anti-anxiety agents which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.

Abstract: A class of heteroaromatic compounds incorporating a substituted five-membered heteroaromatic nucleus which contains at least two nitrogen atoms are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia and depression.

Abstract: The present invention provides a method for the treatment or prevention of sexual dysfunctions which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such an NK-1 receptor antagonist.

Abstract: A class of 1-?3-(1H-indol-3-yl)propyl!-4-benzylpiperazine derivatives of formula I, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by a range of substituted alkyl groups, 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: The present invention provides a method for the treatment or prevention of movement disorders using an orally active, long acting, CNS-penetrant NK-1 antagonist and pharmaceutical compositions comprising such an antagonist.

Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.

Abstract: The present invention provides a method for the treatment or prevention of substance use disorders using an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.

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 1-4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1-6 carbon atoms; T represents nitrogen or CH; R.sup.1 represents aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, either of which groups may be optionally substituted; and R.sup.2 represents hydrogen or C.sub.1-6 alkyl 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.

Abstract: The present invention relates to a traceless solid phase process for the preparation of an indole derivative, which comprises the following steps:(1) reaction of an optionally substituted 2-iodoaniline derivative via the nitrogen atom of the NH.sub.2 moiety thereof with a dihydropyran-functionalized polymeric resin under conditions effective to form an aminal linkage;(2) reaction of the tetrahydropyran aminal derivative thereby obtained with an acetylene derivative in the presence of a transition metal catalyst under conditions effective to promote indole formation;(3) treatment of the product thereby obtained with acid, whereby the aminal linkage is cleaved and the desired indole derivative is liberated from the resin; and(4) isolation of the desired indole derivative thereby obtained.

Abstract: Triazole derivatives represented by formula (IIA), and salts and prodrug thereof, wherein R.sup.1 represents C.sub.1-6 alkoxy(C.sub.1-6)alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl(C.sub.1-6)alkyl, aryl, aryl(C.sub.1-6)alkyl, aryloxy(C.sub.1-6)alkyl, aryl(C.sub.2-6)alkenyl, aryl(C.sub.2-6)alkynyl, C.sub.3-7 heterocycloalkyl(C.sub.1-6)alkyl, heteroaryl, heteroaryl(C.sub.1-6)alkyl, heteroaryl(C2-6)alkenyl or heteroaryl(C.sub.2-6)alkynyl, any of which groups may be optionally substituted; are selective agonist of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

Abstract: A class of 1-?3-(1H-indol-3-yl)propyl!-4-(2-phenylethyl) piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, and on the phenyl ring of the phenethyl moiety by fluoro, chloro, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D .alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D .alpha. receptor subtype relative to the 5-HT.sub.1D .alpha. subtype; they are therefore usefull 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 relates to compounds of formula (I): ##STR1## wherein m is zero, 1 or 2; and n is zero or 1, with the proviso that the sum total of m+n is 1 or 2;R.sup.1 represents phenyl; naphthyl; benzhydryl; or benzyl, where the naphthyl group or any phenyl moiety may be substituted;R.sup.2 represents hydrogen; phenyl; heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; naphthyl; benzhydryl; or benzyl; wherein each heteroaryl, the naphthyl group and any phenyl moiety may be substituted;R.sup.3 and R.sup.4 each independently represents hydrogen or C.sub.1-6 alkyl or R.sup.3 and R.sup.4 together are linked so as to form a C.sub.1-3 alkylene chain;Q represents CR.sup.5 R.sup.6 or NR.sup.5 ;X and Y each independently represents hydrogen, or together form a group .dbd.O; andZ represents a bond, O, S, SO, SO.sub.2, NR.sup.c or --(CR.sup.c R.sup.d)--, where R.sup.c and R.sup.d each independently represent hydrogen or C.sub.

Abstract: The present invention relates to the use of a non-ionic surface-active agent or an emulsion for the reduction of the hemolytic effects of an amphiphilic compound. There is also provided a method for reducing the hemolytic effects of an amphiphilic compound which comprises formulating said compound with a non-ionic surface-active agent or in the form of an emulsion.

Abstract: This invention relates to methods and compositions for treating pain and nociception in a patient by administering a combination of a piperidine tachykinin antagonist and an opioid analgesic.

Abstract: The present invention relates to compounds of formula (I), wherein R.sup.1 and R.sup.4 represent hydrogen, halogen, 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, C.sub.1-6 alkoxy, C.sub.1-4 alkyl substituted by a hydroxy or C.sub.1-4 alkoxy group, OCF.sub.3, hydroxy, trifluoromethyl, trimethylsilyl, nitro, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, COR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b, where R.sup.a and R.sup.b are each independently hydrogen or C.sub.1-4 alkyl; R.sup.2, R.sup.3 and R.sup.5 represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy substituted by a C.sub.1-4 alkoxy group, or trifluoromethyl; R.sup.6 represents C.sub.1-6 alkyl, optionally substituted by oxo, substituted by a 5-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, oxadiazole and thiadiazole, wherein each heteroaromatic ring is substituted at the available carbon atom by a group of the formula: ZNR.sup.7 R.sup.8.

Abstract: A class of substituted 1,2,3,6-tetrahydropyridine derivatives are disclosed that are ligands for dopamine receptor subtypes within the body. These compounds are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.

Abstract: A class of N-substituted piperazine, piperadine and tetrahyrdopyridine derivatives of formula (I), further substituted at the 4-position by an optionally substituted aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 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. In formula (I) Z represents --SO.sub.2 NR.sup.5 R.sup.6, or a group of formula (b).