Glucocorticoid receptor agonist comprising...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 215/14 (2006.01) A61K 31/47 (2006.01) A61K 31/4709 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61P 1/02 (2006.01) A61P 1/04 (2006.01) A61P 1/16 (2006.01) A61P 3/08 (2006.01) A61P 5/14 (2006.01) A61P 5/16 (2006.01) A61P 5/38 (2006.01) A61P 5/44 (2006.01) A61P 7/00 (2006.01) A61P 7/04 (2006.01) A61P 7/06 (2006.01) A61P 9/00 (2006.01) A61P 11/00 (2006.01) A61P 11/02 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 15/00 (2006.01) A61P 17/00 (2006.01) A61P 17/02 (2006.01) A61P 17/04 (20

Patent

CA 2724055

The present invention is related to glucocorticoid receptor agonists comprised of a compound represented by formula (1) which is 2,2,4-trimethyl-6-phenyl-1,2- dihydroquinoline derivative or a salt thereof and novel pharmacological effects of the glucocorticoid receptor agonists. In the formula (1) , R1 represents formula (2a) ,(3a) , (4a) or (5a); R2 represents -(CO)-R8, -(CO)O-R9, or the like; R2-O- is substituted at the 4- or-5-position of benzene ring A; R3 represents a lower alkyl group; R4, R5, R6 or R7 represents a halogen atom, a lower alkyl group which may have a substituent, or the like; m, n, p or q represents 0,1 or the like; R8, R9 or the like represents a lower alkyl group which may have a substituent, a lower alkenyl group, or the like. Image (1) Image (2a) Image (4a) Image (3a) Image (5a) 265

L'invention porte sur un agoniste des récepteurs de glucocorticoïdes composé d'un composé représenté par la formule (1) ou d'un sel de celui-ci, qui est un dérivé de 2,2,4-triméthyl-6-phényl-1,2-dihydroquinoléine ayant un groupe oxy substitué. L'invention porte également sur un nouvel effet pharmacologique de l'agoniste. Dans la formule, R1 représente un groupe représenté par la formule (2a), (3a), (4a) ou (5a) ; R2 représente -(CO)-R8, -(CO)O-R9 ou similaire ; R2-O- est substitué au niveau de la position 4 ou de la position 5 du noyau benzénique A ; R3 représente un groupe alkyle inférieur ; R4, R5, R6 ou R7 représentent un atome d'halogène, un groupe alkyle inférieur facultativement substitué ou similaire ; m, n, p ou q représentent 0, 1 ou similaire ; et R8, R9 ou similaire représentent un groupe alkyle inférieur facultativement substitué, un groupe alcényle inférieur ou similaire.

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