Abstract: Compounds having the formula R5O—A—NR4—R2  (V) where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent —SO— or —SO2— and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).

Abstract: Compounds having the formula R5O—A—NR4—R2  (V) where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent —SO— or —SO2— and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).

Abstract: Compounds having the formulaR.sup.5 O--A--NR.sup.4 --R.sup.2 (V)where R.sup.2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R.sup.4 and R.sup.5 are both hydrogen atoms or together represent --SO-- or --SO.sub.2 -- and A is C.sub.2 -C.sub.4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R.sup.4 and R.sup.5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).R.sup.2 O--A--NH.sub.

Abstract: Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formula A is C.sub.2-4 alkylene chain optionally substituted by lower alkyl, Z is oxygen or sulphur, R is hydrogen or lower alkyl, R.sup.1 is a mono or bicyclic aryl or heteroaryl radical, R.sup.2 is a mono or bicyclic heteroaryl radical and R.sup.3 is hydrogen or a specified radical such as lower alkyl, cycloalkyl, aryl, heteroaryl or optionally substituted amino.

Abstract: Selective 5-HT.sub.1A antagonists radiolabelled with .sup.3 H or .sup.11 C are radiolabelled ligands useful, for example, in pharmacological screening procedures and in positron emission tomography (PET) studies.

Abstract: This invention concerns peptides (I) having intracellular potassium channel modulating activity comprising the amino acid sequence shown in SEQ ID No: 2:(N terminal function) (I) Met Ile Ser Ser Val Cys Val Ser Ser 1 5} Tyr Arg Gly Arg Lys Ser Gly Asn Lys 10 15 Pro Pro Ser Lys Thr Cys Leu Lys Glu Glu 20 25 (C terminal function)in which the cysteines are optionally linked via a disulphide bridge and wherein ______________________________________ Met represents L-methionine Ile represents L-isoleucine Ser represents L-serine Val represents L-valine Cys represents L-cysteine Tyr represents L-tyrosine Arg represents L-arginine Gly represents glycine Lys represents L-lysine Asn represents L-asparagine Pro represents L-proline Thr represents L-threonine Leu represents L-leucine Glu represents L-glutamic acid ______________________________________or a variant thereof,with the proviso that excluded is the 13-Lys variant (where 13-Arg is replaced by 13-Lys) in which the cysteines are not linked via a disulphide bridge

Abstract: Piperazine derivatives of formula (I) are useful in the treatment of cognitive disorders. In formula (I), X is a group of (IIa): --(CH.sub.2).sub.n CR.sup.2 R.sup.3 CONR.sup.4 R.sup.5 or (IIIb): --A--NR.sup.6 COR.sup.7 where n, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have specified meanings.

Abstract: This invention concerns a compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds with the nitrogen ring optional bonds being between one adjacent pair on ring atoms,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; said aryl or heteroaryl radicals being optionally substituted by one or more substituents the same or different,R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, optionally substituted C.sub.6 -C.sub.10 aryl, optionally substituted heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl,R' represents one or more optional substituents the same or different, selected from one or more of the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.

Abstract: Compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula a and b each represents 0, 1, 2 or 3 such that the sum of a+b is 0, 1, 2 or 3, the dotted line represents an optional double bond which may be present in the ring, provided that a is at least 1, A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, R is a mono or bicyclic aryl or heteroaryl radical with the proviso that R is not an unsubstituted phenyl group, R.sup.1 is a mono or bicyclic heteroaryl radical, and R.sup.2 is cycloalkyl or cycloalkenyl.

Abstract: This invention concerns compounds of formula (I) ##STR1## where A is a C.sub.1 or C.sub.2 alkylene chain optionally substituted by lower alkyl; Z is a bicyclic oxygen-containing aryl radical (e.g. 2,3-dihydro-1,4-benzodioxin-5-yl); R is hydrogen or lower alkyl; R.sup.1 is aryl or aryl(lower)alkyl; R.sup.2 is hydrogen or lower alkyl; and R.sup.3 is hydrogen, an alkyl group of 1 to 10 carbon atoms, cycloalkyl of 3 to 12 carbon atoms; cycloalkyl(lower)alkyl, aryl or aryl(lower)alkyl or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom, and the pharmaceutically acceptable acid addition salts thereof. The compounds are 5-HT.sub.1A -antagonists which may be used, for example, in treating anxiety.

Abstract: This invention concerns compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted line represents an optional bond,one of R.sup.1 and R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.16 aralkyl, --(CHR.sup.6).sub.n CHR.sup.7 CN, --(CHR.sup.6).sub.n CHR.sup.7 CONH.sub.2, --(CHR.sup.6).sub.n CHR.sup.7 COOR.sup.8, --(CHR.sup.6).sub.n CHR.sup.7 CH.sub.2 OH wherein n is 0 or 1, R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1 -C.sub.6 alkyl- or C.sub.7 -C.sub.16 aralkyl-, and R.sup.7 also represents hydroxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.2 -C.sub.7)alkanoyloxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6 alkoxy)carbonyl- and R.sup.8 is hydrogen or C.sub.1 -C.sub.6 alkyl;the other of R.sup.1 and R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl; R.sup.3 is C.sub.6 -C.sub.10 aryl or heteroaryl group optionally substituted by one or more substituents the same or differnet,R.sup.2 and R.sup.

Abstract: Piperazine derivatives of formula (I) and their salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, R, R.sup.2 and R.sup.4 are hydrogen or lower alkyl, R.sup.1 is mono- or bicyclic aryl or heteroaryl, R.sup.3 is lower alkyl or cycloalkyl, A is an alkylene chain and X is --CO--. --CR.sup.5 OH-- (where R.sup.5 is hydrogen, lower alkyl or cycloalkyl), --S--, --SO-- or --SO.sub.2 -- or X can also be --(CH.sub.2).sub.n -- (where n is 0, 1 or 2) when R.sup.3 is cycloalkyl.

Abstract: This invention concerns a compound of generic formula ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group;R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl C.sub.6 -C.sub.10 aryl, heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl;R' represents one or more optional substituents the same or different, selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6)alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, C.sub.6 -C.sub.10 or heteroaryl or an (C.sub.6 -C.sub.

Abstract: A novel asymmetric synthesis is provided for preparing optically active amides of formula (A) and their salts. ##STR1## In the formula, X represent --N-- or --CH--, R represents a mono or bicyclic aryl or heteroaryl group, R.sup.1 is an aryl or heteroaryl radical, and R.sup.2 and R.sup.3 have specified meanings. The products are useful as 5-HT.sub.1A antagonists.Novel diesters of formula D useful as intermediates in the process are also disclosed.

Abstract: This appliciation discloses a process for preparing a lactone of general formula (I), where R is an optionally substituted phenyl group or an optionally substituted mono- or bicyclic heteroaryl radical which process comprises reacting an anion of a malonate of formula (II) with an ethylene compound of formula (III) Y--CH.sub.2 --CH.sub.2 OZ, to give a compound of formula (IV) and hydrolysing the compound of formula (IV) to give a lactone of formula (I). The lactones are of use as intermediates for preparing 5-HT.sub.1A binding agents.

Abstract: Amide Derivatives of formula (I) wherein R.sup.1 is a mono or bicyclic heteroaryl radical, R.sup.2 is cycloalkyl, R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl, and R.sup.5 is a group of formula (A) or (B) or (C): R.sup.8 --CH.sub.2 --CH.sub.2 -- or (D) or (E): R.sup.9 OCH.sub.2 CHOHCH.sub.2 -- or (F): R.sup.9 OCH.sub.2 CH.sub.2 -- and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.

Abstract: Piperazine derivatives of formula (I) and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, A is an optionally substituted alkylene chain, Z is a specified bicyclic nitrogen containing heteroaromatic radical, R is hydrogen or lower alkyl, R.sup.1 is aryl or aryl(lower)alkyl and R.sup.2 and R.sup.3 are hydrogen or specified organic radicals or --NR.sup.2 R.sup.3 represents a heterocyclic ring.

Abstract: Piperazine derivatives of formula (I) and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, R and R.sup.3 are hydrogen or lower alkyl or R.sup.3 is spirocycloalkyl, R.sup.1 and R.sup.2 are aryl or heteroaryl radicals and n is 1 or 2 and m is 1 to 3 and the total of n+m is 2-4.

Abstract: Amide Derivatives of formula (I): R.sup.5 NR.sup.4 (CR.sub.2).sub.2 CHR.sup.3 CONR.sup.1 R.sup.2 and their pharmaceutically acceptable salts are 5-HT1A binding agents and may be used, for example, as anxiolytics. The radicals, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have specified meanings.