Novel 3-substituted urea derivatives and medicinal use thereof

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 275/28 (2006.01) A61K 31/17 (2006.01) A61K 31/216 (2006.01) A61K 31/235 (2006.01) A61K 31/275 (2006.01) A61K 31/36 (2006.01) A61K 31/4045 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) A61K 31/4439 (2006.01) A61K 31/5375 (2006.01) A61P 9/10 (2006.01) A61P 11/00 (2006.01) A61P 11/06 (2006.01) A61P 17/02 (2006.01) A61P 17/06 (2006.01) A61P 25/28 (2006.01) A61P 31/04 (2006.01) A61P 31/12 (2006.01) A61P 37/06 (2006.01) A61P 37/08 (2006.01) C07C 275/30 (2006.01) C07C 275/34 (2006.01) C07C 275/40 (2006

Patent

CA 2418652

The present invention relates to a urea derivative of the formula (1) (see formula 1) wherein each symbol is as described in the specification, a pharmaceutically acceptable salt thereof and pharmaceutical use thereof. The compound of the present invention has a C5a receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of diseases or syndromes due to inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis, pancreatitis and the like) due to activation of leukocytes caused by ischemia, trauma, burn, surgical invasion and the like]. In addition, it is useful as an agent for the prophylaxis or treatment of infectious diseases caused by bacteria or virus that invades via a C5a receptor.

L'invention concerne des nouveaux dérivés d'urée correspondant à la formule générale (1), ou bien des sels pharmaceutiquement acceptables de ceux-ci. Dans ladite formule (1), chaque symbole correspond à la définition donnée dans la description. Etant donné qu'ils constituent des antagonistes vis-à-vis du récepteur de C5a, ces composés sont utiles pour soigner et prévenir des maladies ou des syndromes induits par C5a, par exemple, des maladies auto-immunes telles que le rhumatisme et le lupus érythémateux systémique, des maladies de nature allergique telles que la septicémie, le syndrome de détresse respiratoire de l'adulte, la broncho-pneumopathie chronique obstructive et l'asthme, l'athérosclérose, l'infarctus cardiaque, l'infarctus cérébral, le psoriasis, la maladie d'Alzheimer, et des lésions graves d'organes dues à l'activation de leucocytes résultant d'une ischémie, d'un traumatisme, d'une brûlure, d'une effraction chirurgicale, etc., par exemple la pneumonie, la néphrite, l'hépatite et la pancréatite. En outre, ces composés peuvent être utiles pour soigner et prévenir des infections bactériennes et virales induites par le récepteur de C5a.

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