Pfizer Corporation

Gillian M Samuels

Martin James Wythes

John C Danilewicz

Ian T Barnish

Nicholas Kenneth Terrett

Keith James

Michael T Williams

Susan Frances Robson

Kathryn Louise Monkhouse

Alan Brian Wilson

Shirley Jones

Gillian Christine Land

Martin J Wythes

Paul Gupta

Juan Lahuerta

Method of treatment

A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6- membered carbocyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3,4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.

Glutaramide diuretic agents

A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.

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Barham, United Kingdom

Gillian M Samuels