Pfizer Corporation

Other

Mark Anthony Dombroski

Michael Anthony Letavic

Kim F McClure

Allen Jacob Duplantier

Kevin Koch

Anthony D Piscopio

James F Eggler

Ellen Ruth Laird

Chakrapani Subramanyam

Kieran F Geoghegan

Christopher A Gabel

Richard J Griffiths

The present invention relates to novel triazolo-pyridines of the formula I  wherein Ris fluoro; s is an integer from two to three; Ris (C-C)cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C-C)alkyl, hydroxy, (C-C)alkoxy and (C-C)alkyl-(C&#x2550;O)&#x2014;O&#x2014;; or Ris (C-C)alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C-C)alkyl, hydroxy, (C-C)alkoxy and (C-C)alkyl-(C&#x2550;O)&#x2014;O&#x2014;; with the proviso that said compound of formula I cannot be 6-[4-(2,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; or 6-[4-(3,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Di and trifluoro-triazolo-pyridines anti-inflammatory compounds

The present invention provides benzamide inhibitors of the P2Xreceptor of the formula: wherein R&#x2013;Rare as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

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The present invention provides benzamide inhibitors of the P2Xreceptor of the formula:  wherein R&#x2013;Rare as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen;

Benzimidazole anti-inflammatory compounds

The present invention relates to novel alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates and methods for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines

The present invention relates to novel cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines

The present invention relates to novel cycloalkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines

The present invention provides benzamide inhibitors of the P2Xreceptor of the formula:wherein R-Rare as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Benzamide inhibitors of the P2X7 Ereceptor

Triazolo-pyridines anti-inflammatory compounds

Benzotriazoles anti-inflammatory compounds

The present invention relates to the identification of diarylsulfonylurea binding proteins (DBPs) as therapeutic targets for agents that suppress the release of inflammatory mediators such as interleukin IL-1 and IL-1&bgr;.

Methods of screening compounds for their ability to inhibit the production of inflammatory cytokines

Sulfonyl urea derivatives and their use in the control of interleukin-1 activity

Sulfonyl urea derivatives and their use in the control of interleukin-1

This invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds or a pharmaceutically acceptable salt thereof, and to methods of using such compounds as LTB.sub.4 antagonists. The compounds and the pharmaceutically acceptable salts of this invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.

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Waterford, CT, United States of America

Mark Anthony Dombroski