2,6-methano-2H-1-benzoxocincarboxylic acids, esters and amides
AssigneeRhone-Poulenc Rorer Pharmaceuticals Inc.
InventorsJohn E. Airey, Matthew R. Powers, Walter Rodriguez, Raymond D. Youssefyeh
Life of this patent
Estimating the term…
Abstract
Novel compounds which are 2,6-methano-2H-1-benzoxocincarboxamides having 5-HT.sub.3 -antagonist properties including unique CNS, antiemetic and gastric prokinetic activities and which are void of any significant D.sub.2 receptor binding affinity, therapeutic compositions and methods of treatment of disorders which result from 5-HT.sub.3 activity using said compounds. Processes for their preparation and the preparation of their intermediates are also disclosed.
Claims16
A product prepared by the treatment of a compound of the formula ##STR26## and its steroisomers, enantiomers, diasteroisomers and racemic mixtures with an amine of the formula H.sub.2 N-Z;
- where:
- R.sub.1 is hydrogen, an amino or alkylamino optionally substituted with a protecting group halo or haloalkyl;
- R.sub.2 is hydrogen, halo, sulfamyl, mono- and di-alkylsulfamyl or haloalkyl;
- R' and R" are hydrogen or alkyl;
- and
- Z is:
- ##STR27## and its racemic mixtures and stereospecific isomers.
A compound of the formula:
- ##STR29## where:
- R is NH-Z;
- R.sub.1 is hydrogen, an amino or alkylamino optionally substituted with a protecting group, halo or haloalkyl;
- R.sub.2 is hydrogen, halo, sulfamyl, mono- and di-alkylsulfamyl optionally substituted with a protecting group or haloalkyl;
- R' and R" are hydrogen or alkyl;
- vicinal R' and/or R" groups may form a C.dbd.C double bond;
- and
- Z is ##STR30## and its stereoisomers, enantiomers, diastereoisomers and racemic mixtures;
- or pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.