Pfizer Corporation

Sandra Marina Monaghan

Simon John Mantell

Alexander Roderick MacKenzie

Peter Thomas Stephenson

Anthony Marfat

John Paul Mathias

David Alker

Thomas V Magee

Simon Bailey

Dale G McLeod

Elisabeth C L Gautier

Alan J Henderson

Blanda L C Stammen

Christopher John Burns

The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.

Purine derivatives

The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.

Nicotinamide derivatives useful as PDE4 inhibitors

The present invention relates to compounds of the formulaand pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.

The present invention relates to compounds of the formulaand pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds as adenosine A2a receptor agonists.

Quaternary ammonium compounds

The present invention provides compounds of formula (I):

Adenosine A2A receptor agonists as antiinflammatory agents

The present invention provides a compound of formula (I) wherein R is phenyl, C,-C,cycloalkyl or heteroaryl, each of which being optionally benzo- or C,-C,cycloalkyl-fused and optionally substituted, including in the benzo- or C,-C,cycloalkyl-fused portion, by from 1 to 3 substituents each independently selected from C,-C,alkyl, fluoro(C,-C,)alkyl, C,-C,alkoxy, fluoro(C,-C,)alkoxy, phenoxy, C,-C,alkanoyl, halo, C,-C,alkoxycarbonyl, C,-C,cycloalkyl, &mdash;S(O),(C,-C,alkyl), cyano, &mdash;NR,R,, &mdash;S(O),NR,R,, &mdash;NR,(C,-C,alkanoyl) and &mdash;CONR,R,, or R is 2,3-dihydrobenzo&lsqb;b&rsqb;furanyl or chromanyl; R,is H or C,-C,alkyl; W is a direct link, methylene or ethylene; X is unbranched C,-C,alkylene; Y is phenyl, naphthyl, benzyl, pyridyl, thienyl or C,-C,cycloalkyl, each of which being optionally substituted by from 1 to 3 substituents each independently selected from C,-C,alkyl, fluoro(C,-C,)alkyl, C,-C,alkoxy, fluoro(C,-C,)alkoxy, halo and cyano; Ar is phenyl, naphthyl, benzyl, thienyl, benzo&lsqb;b&rsqb;thienyl or indolyl, each of which being optionally substituted by from 1 to 3 substituents each independently selected from C,-C,alkyl, fluoro(C,-C,)alkyl, C,-C,alkoxy, fluoro(C,-C,)alkoxy, halo and cyano, or Ar is 1,3-benzodioxolan-4 or 5-yl or 1,4-benzodioxan-5 or 6-yl; Z,is a pharmaceutically acceptable anion; with the proviso that when W is a direct link and R is optionally fused and optionally substituted heteroaryl, said heteroaryl is linked by a ring carbon atom to the carbonyl group. The compounds are tachykinin antagonists.

Quaternary ammonium compounds as tachykinin antagonists

A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein X, O R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the specification; compositions containing such compounds; intermediates used in the preparation of such compounds; and methods for treating a disease associated with the altered tone and/or motility of smooth muscle, for example chronic obstructive airways disease, asthma, urinary incontinence, irritable bowel syndrome, diverticular disease, oesophageal achalasia, and hypertension.

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Sandwich, United Kingdom

Sandra Marina Monaghan