John Wyeth Brother, Limited

John F White

Michael C Minchin

Terence J Ward

Christine Ennis

Alan C White

Michael C Warren

Amine derivatives containing a phosphonic acid moiety

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.

Method of treating depression and tri-substituted amines therefor

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.7 together with the nitrogen atom to which they are attached represent a 5 or 6 membered ring, which compounds are useful, for treating depression or cerebral insufficiency or dementias in animals.

Composition for treating depression with (N-heteroaryl)alkylamines

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

Method and amines used therein

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, e.g. 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.7 together with the nitrogen atom to which they are attached represent a 5 or 6 membered ring, which compounds are useful, for treating depression or cerebral insufficiency or dementias in animals.

Composition for treating depression with (S- or O-heteroaryl)alkyl amines

The invention concerns a method for treating pain and/or CNS disorders characterized in that the method uses a compound which acts selectively as an antagonist of gamma aminobutyric acid (GABA) at GABA autoreceptors relative to GABA.sub.A receptors.

Method of treatment and heterocyclic compounds used therein

Pharmaceutical tetrahydroisoquinolines

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, e.g. 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.7 together with the nitrogen atom to which they are attached represent a 5 or 6 membered ring, which compounds are useful, for treating depression or cerebral insufficiency or dementias in animals.

Composition for treating depression with aralkyl amines

The invention concerns benzoquinolizines of general formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents hydrogen or lower alkyl and R.sup.4 represents a heterocyclic radical attached to the SO.sub.2 group through a carbon atom of the heterocyclic ring. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.

Benzoquinolizines as .alpha..sub.2 -adrenoceptor antagonists

The invention concerns benzoquinolizines of formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents methyl or ethyl, A represents a direct bond between the S and N atoms or a lower alkylene group having 1 to 3 carbon atoms in the chain between the S and N atoms, R.sup.4 and R.sup.5 each independently represent hydrogen, lower alkyl, aryl or aryl(lower)alkyl or together with the nitrogen atom to which they are attached represent a five or six membered heterocyclic ring. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity and can be incorporated into pharmaceutical compositions.

.alpha..sub.2 -Adrenoceptor antagonistic benzoquinolizines

The invention concerns benzoquinolizines of the general formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein the ##STR2## linkage represents a single bond linkage of formula ##STR3## or a double bond linkage of formula ##STR4## R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 and R.sup.4 which may be the same or different each represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, di(lower)alkylamino or trifluoromethyl and X is O, S or NH. The compounds possess anti-secretory activity.

Benzoquinolizines, anti-secretory compositions containing them, and

The invention concerns benzoquinolizines of the general formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 and R.sup.2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen and R represents --CXNHR.sup.3 (where X is O, S or .dbd.NH and R.sup.3 is hydrogen or lower alkyl) or --(CH.sub.2).sub.n R.sup.4 (where n is 0 or 1 and R.sup.4 is aryl). These compounds lower blood pressure. Some are also anti-ulcer agents. The compounds in which R.sup.1, R.sup.2 and R are as defined above, with the proviso that when R is phenyl, R.sup.1 and R.sup.2 are not both lower alkoxy, are novel.

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Wokingham, United Kingdom

John F White