Novel amide derivatives and medicinal use thereof

Details Novel amide derivatives and medicinal use thereof Novel amide derivatives and medicinal use thereof

C - Chemistry, Metallurgy

07

C

C07C 233/59 (2006.01) A61K 31/275 (2006.01) A61K 31/351 (2006.01) A61K 31/353 (2006.01) A61K 31/357 (2006.01) A61K 31/36 (2006.01) A61K 31/381 (2006.01) A61K 31/382 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/4155 (2006.01) A61K 31/4164 (2006.01) A61K 31/426 (2006.01) A61K 31/429 (2006.01) A61K 31/44 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61K 31/4453 (2006.01) A61K 31/4545 (2006.01) A61K 31/4704 (2006.01) A61K 31/5375 (2006.01) A61K 31/5377 (2006.01) A61K 31/67 (2006.01) A6

Patent

CA 2422342

The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action (see formula 1) wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an optically active form thereof and a pharmaceutically acceptable salt thereof are promising as an agent for the treatment or prophylaxis of diseases or syndromes caused by 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 and pancreatitis and the like) due to activation of leukocytes caused by ischemia reperfusion, trauma, burn, surgical invasion and the like]. Moreover, they are useful as a therapeutic or prophylactic agent for the infectious diseases caused by bacteria and virus that invade via a C5a receptor.

L'invention concerne des dérivés amides représentés par la formule générale suivante (1) qui possèdent un antagonisme vis à vis du récepteur C5 alpha : dans laquelle chaque symbole a la signification définie dans la description. Ces dérivés amides, leurs isomères optiquement actifs ou des sels de ces dérivés acceptables sur le plan pharmaceutique, sont utiles dans la prévention et dans le traitement de maladies ou de syndromes inflammatoires induits par C5 alpha [par exemple, maladies immunologiques telles que le lupus érythémateux systémique et rhumatismal, des maladies allergiques telles que, état septique, syndrome de détresse respiratoire de l'adulte, broncho-pneumopathie obstructive pulmonaire et asthme, athérosclérose, infarctus cardiaque, infarctus cérébral, psoriasis, maladie d'Alzheimer et des effondrements importants de l'organisme (tels que pneumonie, néphrite, hépatite, pancréatite) induits par une activation leucocytaire provoquée par une reperfusion ischémique, une brûlure ou une invasion chirurgicale]. En outre, ces dérivés sont utiles dans la prévention et le traitement d'infection par bactéries et virus dont la médiation est réalisée par le récepteur C5 alpha .

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