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: 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: 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 invention concerns compounds having the Z-configuration of formula: ##STR1## or salts thereof, wherein R represents an optionally substituted aryl or heteroaryl radical, R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, carboxy, hydroxy (C.sub.1 -C.sub.6)alkyl, halogen, halo(C.sub.1 -C.sub.6)alkyl, carboxy(C.sub.1 -C.sub.6)alkyl, optionally substituted aryl or heteroaryl or optionally substituted aralkyl or heteroarylalkyl; n represents 0, 1 or 2; R.sup.4 and R.sup.5 each independently represent hydrogen or a substituent selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl or R.sup.4 and R.sup.5 are geminal C.sub.1 -C.sub.6 alkyl substituents and R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl which possess antiinflammatory activity.

Abstract: Amide derivatives of formula (I) and their pharmaceutically acceptable salts (where a and b each represent 0, 1, 2 or 3 such that a+b=0, 1, 2 or 3, the dotted line represents an optional double bond, A is an optionally substituted C.sub.1-2 -alkylene chain, R is mono or bicyclic aryl or heteroaryl radical, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an aryl, aralkyl, heteroaryl or heteroarylalkyl and --CONR.sup.3 R.sup.4 represents a specified amide group) are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.

Abstract: Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.

Abstract: This invention concerns compounds of formula (I) wherein E represents hydrogen, C.sub.1 -C.sub.6 alkyl or a group Ar.sup.1 -A.sup.1 ; Ar and Ar.sup.1 when present each represent an aryl group of 6 to 10 carbon atoms or a heteroaryl group of 5 to 10 ring atoms wherein the heteroatoms are selected from oxygen, nitrogen and sulphur, which may be optionally substituted by one or more substituents selected from alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halogen, haloalkyl of 1 to 6 carbon atoms, haloalkoxy of 1 to 6 carbon atoms, cyano, amino, mono- or di-(C.sub.1 -C.sub.6) alkylamino, hydroxy and nitro; A and A.sup.1 when present are the same or different alkylene groups having one or two carbons linking Ar or Ar.sup.

Abstract: The invention concerns a method for treating depression or senile dementia using a compound which acts selectively as an agonist of gamma aminobutyric acid (GABA) at GABA autoreceptors with the proviso that the compound is not fengabine and progabide.

Abstract: (Endo)-N-[[[8-azabicyclo[3.2.1]octan-3-yl]amino]carbonyl]-2-(cyclopropylmet hyloxy)benzamide and pharmaceutically acceptable salts thereof possess 5-HT.sub.3 antagonistic activity and are useful in the treatment of neuro-psychiatric disorders (e.g. anxiety), gastro-intestinal disorders and migraine.

Abstract: The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar.sup.1 --A.sup.1 --; Ar and Ar.sup.1 are the same or different aryl groups (including heteroaryl) which are optionally substituted, eg by one or more substituents commonly used in pharmaceutical chemistry; A and A.sup.1 are the same or different alkylene groups having one or two carbon atoms linking Ar or Ar.sup.1 to N and optionally substituted by lower alkyl and/or optionally substituted aryl, B is an alkylene group of 3 or 4 carbon atoms, which may be substituted by lower alkyl; D.sup.1 represents halogen, CH.sub.3, CR.sup.1 R.sup.2 NH.sub.2, SO.sub.3 H or SO.sub.2 NR.sup.6 R.sup.7 where R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl and R.sup.6 and R.sup.7 are each hydrogen, lower alkyl or aralkyl of 7 to 12 carbon atoms or R.sup.6 and R.sup.

Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl and X is a functionalized group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, into alia, for the treatment of CNS disorders, such as anxiety.

Abstract: Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.

Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl and X is a functionalised group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, into alia, for the treatment of CNS disorders, such as anxiety.

Abstract: Disclosed herein are piperazine derivatives of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein W is (CH.sub.2).sub.m, CHOH or O,m is one of the integers 1 or 2,A is an alkylene chain of 1 to 3 carbon atoms optionally substituted by one or more (lower)alkyl groups,R is hydrogen or lower alkyl,R.sup.1 and R.sup.2 are each, independently, aryl or heteroaryl radicals with the proviso that R.sup.1 is not an optionally substituted indolyl radical,R.sup.3 is hydrogen or lower alkyl andR.sup.4 is an aryl or heteroaryl radical.The compounds are 5HT.sub.1A binding agents which may be used, for example, in the treatment of CNS disorders such as anxiety.

Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl, and X is a functionalised group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, inter alia, for the treatment of CNS disorders, such as anxiety.