Pfizer Corporation

Mark Ian Lansdell

Alan Daniel Brown

Mark David Andrews

Gavin Alistair Whitlock

David Hepworth

Alan Stobie

Michael J Fray

Paul Vincent Fish

Andrew Antony Calabrese

Florian Michel Wakenhut

Nicholas William Summerhill

David Sebastien Fradet

The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.

Melanocortin type 4 receptor agonist piperidinoylpyrrolidines

The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein R, R, R, Rand Rare as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.

(3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists

A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein Ris H, Calkyl, &#x2014;C(X)Y, Ccycloalkyl, aryl, het, aryl-Calkyl or het-Calkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from Calkyl, Calkoxy, OH, halo, CF, OCF, SCF, hydroxy-Calkyl, Calkoxy-Calkyl and Calkyl-S&#x2014;Calkyl; Ris aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from Calkyl, Calkoxy, OH, halo, CF, OCF, SCF, hydroxy-Calkyl, Calkoxy-Calkyl and Calkyl-S&#x2014;Calkyl; Ris Calkyl, Ccycloalkyl, Ccycloalkyl-Calkyl, aryl, het, aryl-Calkyl or het-Calkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from Calkyl, Calkoxy, OH, halo, CF, OCF, SCF, hydroxy-Calkyl, Calkoxy &#x2014;Calkyl and Calkyl-S&#x2014;Calkyl; X is S or O; Y is H, Calkyl, aryl, het, aryl-Calkyl or het-Calkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

Compounds

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Sandwich, United Kingdom

Mark Ian Lansdell