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 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: 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 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: Bicyclic carboxamides of formula I ##STR1## and the 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 formulaX represents --CR.sup.2 .dbd.CR.sup.2 -- or --(CR.sup.2)q--;m represents 0,1 or 2; n represents 0,1 or 2; p represents 0,1,2 or 3 and q represents 0,1,2 or 3;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,R.sup.1 is an aryl or aryl(lower)alkyl radicaland each R.sup.2 is independently hydrogen or lower alkyl.

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.

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 R is hydrogen or one or two lower alkyl groups, R.sup.1 is a mono of bicyclic aryl or heteroaryl radical, R.sup.2 is aryl and A is a C.sub.2-5 alkylene chain optionally substituted by lower alkyl.

Abstract: Azetidine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula R is hydrogen or one or more specified substituents. The compounds have hypotensive activity. Some are also 5-HT.sub.1A agonists.

Abstract: The invention concerns a compound formula II ##STR1## or an acid addition salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are the same or different and represent hydrogen, or loweralkyl, cycloalkyl or lower aralkyl, any of which radicals may be substituted by lower alkyl, lower alkoxy or CF.sub.3 or phenyl radicals which may be substituted by lower alkyl or CF.sub.3 or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered saturated ring R.sup.4 and R.sup.5 may also represent lower alkoxy, or cycloalkoxy, n is 1, 2, or 3 and, if more than one R.sup.4 radical is present the R.sup.4 radicals may be the same or different with the provisos that (1) when R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are all hydrogen, R.sup.6 R.sup.7 are not both hydrogen, (2) when R.sup.1 and R.sup.3 are both phenyl and when R.sup.1 is methyl and R.sup.4 is methyl then R.sup.6 and R.sup.7 are not both methyl, and (3) when R.sup.1 is hydrogen or methyl, R.sup.

Abstract: The invention concerns a process for preparing a thiazolo[3,2-a]benzimidazole of formula I ##STR1## in which formula n is 1 or 2, and R.sub.1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, or a salt thereof which comprises dehydrating a compound of formula II, ##STR2## or a salt thereof wherein n and R, are as defined above, and COOR is an acid or ester function in the presence of an acid selected from sulphuric, sulphonic and phosphoric acid or mixtures thereof and if desired or required an inert solvent provided that if water is present then the amount of water is less than about 15% by volume of the acid, the reaction being carried out with heating if necessary.

Abstract: Pyrimidoindoles of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl a mono- or bicyclic aryl radical or a group of mormula R.sup.3 O--B--[where R.sup.3 O is (lower)alkoxy,aryl(lower)alkoxy or hydroxy and B is a lower alkylene chain optionally containing one double or triple bond], R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower) alkylamino and A, together with the carbon atom to which it is attached, represents 5, 6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as hypoglyceamics.

Abstract: Compounds of formula ##STR1## wherein A represents a lower alkylene chain optionally containing one double or triple bond, RO represents (lower)alkoxy, aryl(lower)alkoxy, hydroxy or protected hydroxy, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino and R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl and their pharmaceutically acceptable acid addition salts are useful as hypoglycaemics or as intermediates for hypoglycaemics.