Imidazo[1,2-c]pyrimidinylacetic acid derivatives

Details Imidazo[1,2-c]pyrimidinylacetic acid derivatives Imidazo[1,2-c]pyrimidinylacetic acid derivatives

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/519 (2006.01)

Patent

CA 2551778

The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo[1,2-c]pyrimidinylacetic acid 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 d'acide imidazo[1,2-c]pyrimidinylacétique et des sels de celui-ci, utiles sous forme de principe actif de préparations pharmaceutiques. Ce dérivé d'acide [1,2-c]pyrimidinylacétique possède une excellente activité antagoniste de CRTH2 (récepteur chimioattractif couplé à la protéine G, exprimé sur les cellules Th2) et peut être utilisé pour la prophylaxie et le traitement de maladies associées à l'activité de CRTH2, notamment pour le traitement de maladies allergiques, telles que l'asthme, la rhinite allergique, la dermite atopique et la conjonctivite allergique; les maladies liées aux éosinophiles, telles que le syndrome de Churg et Strauss et la sinusite; les maladies liées aux basophiles, telles que la leucémie à basophiles, l'urticaire chronique et la basophilie chez l'homme et d'autres mammifères; et des maladies inflammatoires caractérisées par des infiltrats de lymphocytes T et des leucocytes profus, tels que le psoriasis, l'eczéma, la maladie de Crohn, la MOR (maladie obstructive respiratoire chronique) et l'arthrite.

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