Pfizer Corporation

Stephen Challenger

Donald Stuart Middleton

Alan Stobie

David Cameron Pryde

Adam Gillmore

Andrew Simon Cook

Roger P Dickinson

David James Rawson

Kevin Neil Dack

Kim James

David Ellis

Andrew Michael Derrick

Yousef Hajikarimian

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein Ris optionally substituted Calkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, Calkoxy, &#x2014;NRRor &#x2014;NRSOR; X is the linkage &#x2014;(CH)&#x2014; or &#x2014;(CH)&#x2014;O&#x2014; (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by Calkoxy; hydroxy; hydroxy(Calkyl); Ccycloalkyl; carbocyclyl; heterocyclyl; or by Calkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two Rgroups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R is optionally substituted C alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C alkoxy, &mdash;NR R or &mdash;NR SO R ; X is the linkage &mdash;(CH ) &mdash; or &mdash;(CH ) &mdash;O&mdash; (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C alkoxy; hydroxy; hydroxy(C alkyl); C cycloalkyl; carbocyclyl; heterocyclyl; or by C alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

The invention provides S-(&plus;)-3-&lcub;1-(1,3-benzodioxol-5-yl)-2-&lsqb;(2-methoxy-4-methylphenyl)sulfonylamino&rsqb;-2-oxoethyl&rcub;-1-methyl-1H-indole-6-carboxylic acid, which is substantially free from its (R)-(&minus;)-enantiomer, and pharmaceutically acceptable derivatives thereof. The compounds are useful in the treatment of inter alia acute renal failure, restenosis and pulmonary hypertension.

Indole derivatives useful in therapy

Hydrogenation

The invention provides a process for preparing a compound of the formula: ##STR1## or a base salt thereof, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by up to 3 substituents each independently selected from the group consisting of C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6 alkoxy)-; and R.sup.3 is C.sub.1 -C.sub.6 alkyl or benzyl, said benzyl group being optionally ring-substituted by up to 2 nitro or C.sub.1 -C.sub.4 alkoxy substituents comprising reacting a compound of the formula: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or benzyl or C.sub.1 -C.sub.4 alkoxy; and R.sup.2 and R.sup.3 are as previously defined for a compound of the formula (I), with hydrogen peroxide or a source of peroxide ions: said process being optionally followed by conversion of the compound of the formula (I) to a base salt thereof. The present invention also relates to novel compounds of the formula (II).

Preparation of glutaric acid derivatives

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Sandwich, United Kingdom

Stephen Challenger