C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 239/42 (2006.01) A61K 31/506 (2006.01) A61P 11/06 (2006.01) C07D 239/34 (2006.01) C07D 239/48 (2006.01) C07D 401/12 (2006.01) C07D 403/04 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01)
Patent
CA 2523439
The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.
L'invention concerne un dérivé de pyrimidine de formule (I) et ses sels, utiles comme principe actif de préparations pharmaceutiques. Ledit dérivé de pyrimidine présente une excellente activité antagoniste vis-à-vis du CRTH2 (récepteur chimio-attractif couplé aux protéines G, exprimé sur les cellules Th2) et peut être utilisé pour la prophylaxie et le traitement de maladies liées à l'activité du CRTH2, en particulier pour le traitement de maladies allergiques, telles que l'asthme, la rhinite allergique, la dermatite atopique, et la conjonctivite allergique; de maladies à éosinophiles, telles que le syndrome de Churg et Strauss et la sinusite; de maladies à basophiles, telles que la leucémie à basophiles, l'urticaire chronique, et la basophilie chez les humains ou d'autres mammifères; et de maladies inflammatoires caractérisées par des infiltrats de lymphocytes T et d'importants infiltrats de leucocytes, telles que le psoriasis, l'eczéma, la maladie intestinale inflammatoire, la colite ulcéreuse, la maladie de Crohn, la BPCO (broncopneumopathie chronique obstructive) et l'arthrite.
Bacon Kevin
Koriyama Yuji
Ly Tai-Wei
Manabe Yoshihisa
Sato Hiroki
Actimis Pharmaceuticals Inc.
Osler Hoskin & Harcourt Llp
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