Pfizer Corporation

Agouron Pharmaceuticals, Inc.

Anthony Wood

Manoussos Perros

Mark Edward Bunnage

John Paul Mathias

Stephen Derek Albert Street

David Anthony Price

Blanda Luzia Christa Stammen

Alexander Roderick MacKenzie

Paul Alan Glossop

Simon John Mantell

Peter Thomas Stephenson

Patricia Ann Basford

Stefan Colin John Taylor

Duncan Robert Armour

Martin Paul Edwards

Christine Anne Louise Watson

Simon F Campbell

Paul Anthony Stupple

Charles Eric Mowbray

Romuald Gaston Corbau

David James Rawson

Graham Nigel Maw

Robert J Bass

Ross Sinclair Strang

Blanda Luzia Stammen

Christine Anne Watson

Stefan Colin Taylor

The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.

Carboxamide derivatives as muscarinic receptor antagonists

The present invention provides compounds of formula (I) wherein X, Y, R, Rand Rare as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

Tropane derivatives useful in therapy

The present invention provides compounds of the formula: 

The present invention provides compounds of the formula: wherein Ris Ccycloalkyl optionally substituted by one or more fluorine atoms, or Calkyl optionally substituted by one or more fluorine atoms, or Ccycloalkylmethyl optionally ring-substituted by one or more fluorine atoms; and

Compounds of Formula 1[R&#x3b1;]&#x2212;[R&#x3b2;]&#x2212;[R&#x3b3;]&#x2212;[R&#x3b4;] &#x2003;&#x2003;(I)which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

CCR5 modulators

This invention relates to the use of pyrazole derivatives of the formula  and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.

Pyrazole derivatives

Compounds of Formula 1[R&#x3b1;]&#x2014;[R&#x3b2;]&#x2014;[R&#x3b3;]&#x2014;[R&#x3b4;]&#x2003;&#x2003;(1)which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein Ris Cto Calkyl substituted with Cto Ccycloalkyl, CONRRor a N-linked heterocyclic group; (CH)Het or (CH)Ar, Ris Cto Calkyl; Ris Cto Calkyl optionally substituted with Cto Calkoxy; Ris SONRR; Rand Rare each independently selected from H and Cto Calkyl optionally substituted with Cto Calkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; Rand R, together with the nitrogen atom to which they are attached, form a 4-R-piperazinyl group; Ris H or Cto Calkyl optionally substituted with OH, Cto Calkoxy or CONH; Het is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction

Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3',5&#x2032;-monophosphate phosphodiesterase (cGMP-PDE5) for the treatment of sexual dysfunction

The present invention provides compounds of formula (I)wherein X, Y, R, Rand Rare as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R is C to C alkyl substituted with C to C cycloalkyl, CONR R or a N-linked heterocyclic group; (CH ) Het or (CH ) Ar; R is C to C alkyl; R is C to C alkyl optionally substituted with C to C alkoxy; R is SO NR R ; R and R are each independently selected from H and C to C alkyl optionally substituted with C to C alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R and R , together with the nitrogen atom to which they are attached, form a 4-R -piperazinyl group; R is H or C to C alkyl optionally substituted with OH, C to C alkoxy or CONH ; H is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction.

Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3&prime;,5&prime;&mdash;monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction

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Sandwich, United Kingdom

Anthony Wood