Pfizer Corporation

Keith James

Ian T Barnish

John C Danilewicz

Nicholas Kenneth Terrett

Michael T Williams

Gillian M Samuels

Martin James Wythes

Martin J Wythes

N-(1-(2-carboxyethyl35cloalkylcarbonyl)-beta-alanine derivatives for

The invention provides the substantially optically pure 2(S)-stereoisomeric form of compounds of the formulae: ##STR1## and the salts thereof, together with processes for their preparation. The compounds are intermediates for the preparation of antihypertensive agents.

Glutaric acid derivatives and preparation thereof

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

The invention provides the substantially optically pure 2(S)-steroisomeric form of compounds of the formulae: ##STR1## and the salts thereof, together with processes for their preparation. The compounds are intermediates for the preparation of antihypertensive agents.

2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependent, neutral endopiptidase.

Cycloalkyl-substituted 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.

2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.

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Deal, United Kingdom

Keith James