Pfizer Corporation

Warner-lambert Company

Pfizer Products Inc.

Paul Vincent Fish

Gavin Alistair Whitlock

Kim James

Simon Bailey

Alan Daniel Brown

Alan Stobie

Nicholas Murray Thomson

Mark David Andrews

Florian Michel Wakenhut

Andrew Michael Derrick

Usa Datta

Stephane Billotte

Jackie Diane Kendall

Roger P Dickinson

John C Danilewicz

Michael J Fray

Christopher Gordon Barber

Julian Blagg

Thomas Ryckmans

Michael Butters

Richard Anthony Storey

Trevor Jack Newbury

Mark Ian Lansdell

Julie Ann Macrae

Michael Paul Fitzgerald

Anne Bruckner

Paul Brennan

R Ian Storer

Malcolm Christian Mackenny

The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof wherein the variables R, R, R, R, R, R, and Rare as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a 5-HTreceptor-mediated disorders with a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).

[object Object]

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

Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP.

3-ox(adi)azolylpropanohydroxamic acids useful as procollagen C-proteinase inhibitors

A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein:

Amides useful as monoamine re-uptake inhibitors

Compounds of formula (I):and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.

3-heterocyclylpropanohydroxamic acids

3-heterocyclypropanohydroxamic acid PCP inhibitors

3-heterocyclylpropanohydroxamic acid PCP inhibitors

The invention described herein relates to a process for the preparation of (7-(3-carboxyphenyl)-4-chloroisoquinolin-1-yl)guanidine (I), intermediates thereto and new forms and formulations thereof, including the zwitterion monohydrate of (I), suitable for pharmaceutical use.

(7-(3-carboxyphenyl)-4-chloroisoquinolin-1-yl)guanidine

Procollagen C-proteinase inhibitors

Isoquinolines as urokinase inhibitors

Antithrombotic n-amidinopiperidine and benzamidine derivatives

Growing community of inventors

County of Kent, United Kingdom

Paul Vincent Fish