Nitrogenous heterocyclic derivative and medicine containing...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 211/58 (2006.01) A61K 31/444 (2006.01) A61K 31/4468 (2006.01) A61K 31/453 (2006.01) A61K 31/454 (2006.01) A61K 31/4545 (2006.01) A61K 31/5377 (2006.01) A61K 45/00 (2006.01) A61P 11/06 (2006.01) A61P 29/00 (2006.01) A61P 31/04 (2006.01) A61P 31/18 (2006.01) A61P 37/00 (2006.01) A61P 37/06 (2006.01) A61P 43/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/06 (2006.01) C07D 405/14 (2006.01)

Patent

CA 2579501

Compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof, (wherein the characters are as defined in the description). The compounds of the general formula (I) have a CCR5 antagonistic activity, so that they are useful in the prevention and/or therapy for CCR5 mediated diseases, for example, various inflammatory diseases (asthma, gastritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis and other inflammatory intestinal failure, etc.), immunologic diseases (autoimmune disease, rejection of transplanted organ (rejection of solid organ transplant graft, rejection of pancreatic islet cell transplant in diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (human immunodeficiency virus infection, acquired immunodeficiency syndrome, RSV infection, etc.), allergoses (atopic dermatitis, hives, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), cardiovascular risks (arteriosclerosis, suppression of ischemic reperfusion injury, etc.), acute respiratory distress syndrome, shock caused by bacterial infection, diabetes, cancer metastasis, etc.

Cette invention concerne les composés de formule générale (I), leurs sels et N-oxydes, et les solvates et pro-médicaments de ceux-ci. (Dans la formule (I) les caractères sont conformes à la définition de la description). Les composés répondant à la formule générale (I) présentent une activité antagoniste sur CCR5 de sorte à être utiles dans la prévention et/ou la thérapie des maladies médiées par CCR5, par exemple, diverses maladies inflammatoires (asthme, gastrite, néphropathie, hépatite, arthrite, polyarthrite rhumatoïde, rhinite, conjonctivite, recto-colite hémorragique et autres dysfonctionnements intestinaux inflammatoires, etc.), maladies immunologiques (maladie auto-immune, rejet d'organe transplanté (rejet lors d'une greffe d'organe solide, rejet lors d'une greffe des îlots de Langerhans pancréatiques chez des diabétiques, réaction de greffe contre hôte, etc.), immunosuppression, psoriasis, sclérose en plaques, etc.), maladies infectieuses (infection par le virus de l'immunodéficience humaine, syndrome de l'immunodéficience acquise, infection par le VRS, etc.), maladies allergiques (dermatites atopiques, urticaires, aspergillose broncho-pulmonaire allergique, gastro-entérite allergique à éosinophiles, etc.), risques cardiovasculaires (artériosclérose, suppression de la lésion de reperfusion ischémique, etc.), syndrome de détresse respiratoire aigu, choc dû à une infection bactérienne, diabète, métastases cancéreuses, etc.

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