Pfizer Corporation

John Edward Kemp

Peter E Cross

John C Danilewicz

James Robert Wright

Roger P Dickinson

Michael Snarey

David Alker

David A Cox

Allan L Ham

Certain 1-azabicyclo[2.2.1]heptanes useful as muscarinic receptor

Antiarrhythmic agents of the formula: ##STR1## and their pharmaceutically acceptable salts, wherein R and R.sup.1, which are the same or different, are C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, --CH.sub.2 CH.sub.3, --CH.sub.2 Cl, --CF.sub.3 or --NH.sub.2 ;

4-Substituted-1-(4-alkylsulphonamidophenyl)piperazines as antiarrhythmic

6-Alpha and 6-beta-substituted penicillanic acid derivatives of the formula: ##STR1## wherein R is H or a conventional penicillin carboxy protecting group or an ester forming residue readily hydrolyzable in vivo and R.sup.1 is a perhaloalkyl group of from 1 to 4 carbon atoms wherein the halogen atoms are fluoro or chloro, undergo SN.sub.2 nucleophilic displacement with halide or azide ions with inversion of configuration at C-6 to yield the corresponding 6-beta or 6-alpha-halo- or azido-substituted product.

6-Perhaloalkylsulfonyloxy-penicillanic acids and derivatives thereof

A series of novel 2-amino and 4-aminoquinazoline derivatives have been prepared, including their acid addition salts. These derivatives all possess a single nitrogen-containing benzo-fused heterocyclic ring moiety at either the 4- or 2-positions of the molecule, respectively, with the ring moiety being attached through the nitrogen atom to the aforesaid quinazoline nucleus. Such compounds are useful in therapy as highly potent antihypertensive agents. Methods for their preparation are described in detail, including various synthetic routes leading to the required novel intermediates.

Aminoquinazoline therapeutic agents

Novel-3-alkyl-9-aminoalkyl-1,2,3,4-tetrahydrocarbazoles having gastric anti-secretory activity are prepared. A typical embodiment is 3-tertiary-butyl-9-(2-pyrrolidino-ethyl)-1,2,3,4-tetrahydrocarbazole.

Tetrahydro-carbazole derivatives as gastric anti-secretory agents

A series of novel 2-amino and 4-aminoquinazoline derivatives have been prepared, including their acid addition salts. These derivatives all possess a single nitrogen-containing benzo-fused heterocyclic ring moiety at either the 4- or 2- positions of the molecule, respectively, with the ring moiety being attached through the nitrogen atom to the aforesaid quinazoline nucleus. Such compounds are useful in therapy as highly potent antihypertensive agents. Methods for their preparation are described in detail, including various synthetic routes leading to the required novel intermediates.

2 (OR 4) Amino 4 (or 2) N-hetero quinazolines

A series of novel substituted phenoxypropylamine derivatives have been prepared by reacting the appropriate 1-phenoxy-2,3-epoxypropane compound with a suitable organic amine reagent. The resulting 1-phenoxy-3-alkylaminopropan-2-ols are useful in the field of chemotherapy as anti-angina agents. Preferred members include compounds having an acetamido group substituted on the phenyl ring of the phenoxy moiety. Alternate methods of preparation are also provided.

Phenoxypropanolamine therapeutic agents

A series of novel substituted phenoxypropyl piperazine derivatives have been prepared by reacting the appropriate 1-phenoxy-2,3-epoxypropane compound with 1-phenoxy-3-(4-phenylpiperazine-1-yl)propan-2-ols suitable N-phenylpiperazine reagent. The resulting 1-phenoxy13-(4-phenylpiperazine-1-yl)propan-2-ols are useful in the field of chemotherapy as antihypertensive agents. Preferred members include compounds having an acetamidomethyl, carboxymethyl or carbamoylmethyl group substituted on the phenyl ring of the phenoxy moiety. Alternate methods of preparation are also provided.

Phenoxypropanolpiperazines

Novel 3-alkyl-9-aminoalkyl-1,2,3,4-tetrahydrocarbazoles having gastric anti-secretory activity are prepared. A typical embodiment is 3-tertiary-butyl-9-(2-pyrrolidino-ethyl)-1,2,3,4-tetrahydrocarbazole.

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Canterbury, United Kingdom

John Edward Kemp