Indole derivatives in the treatment of emesis

Details Indole derivatives in the treatment of emesis Indole derivatives in the treatment of emesis

A - Human Necessities

61

K

A61K 31/40 (2006.01) A61K 31/404 (2006.01) A61K 31/445 (2006.01)

Patent

CA 2164286

Compounds of formula 1, Image wherein R1 represents hydrogen; R2 represents hydrogen, halogen, cyano, OR4, -(CH2)mCONR5R6, -(CH2)mSO2NR5R6, -(CH2)mNR7COR8, -(CH2)mS(O)XR8, -(CH2)mNR7CONR5R6, -(CH2)mNR7COOR9 or -CH=CH(CH2)yR10; R3 represents hydrogen or C1-6 alkyl; R4 represents hydrogen, C1-6 alkyl or aryl; R5 and R6 are independently represent hydrogen, C1-6 alkyl, aryl or (C1-3 alkyl)aryl; or R5 and R6 taken together may form a 4-, 5- or 6-membered ring; R7 and R8 independently represent hydrogen, C1-6 alkyl, aryl or (C1-3 alkyl)aryl; R9 represents hydrogen, C1-6 alkyl, aryl or (C1-3 alkyl)aryl; R10 represents -CONR5R6, -SO2NR5R6, -NR7COR8, -NR7SO2R8, -NR7CONR5R6, -S(O)XR8 or-NR7COOR9; m is 0, 1,2 or 3; n is 0, 1 or 2; y is 0, 1 or 2; x is 1 or 2; and pharmaceutically acceptable salts thereof; are useful in the treatment or prevention of emesis not associated with migraine.

Composés de formule 1 Image , dans laquelle : R1 représente de l'hydrogène; R2 représente de l'hydrogène, un halogène, un groupe cyano, OR4, -(CH2)mCONR5R6, -(CH2)mSO2NR5R6, -(CH2)mNR7COR8, -(CH2)mS(O)XR8, -(CH2)mNR7CONR5R6, -(CH2)mNR7COOR9 ou -CH=CH(CH2)yR10; R3 représente de l'hydrogène ou un alkyle C1-6; R4 représente de l'hydrogène, un alkyle C1-6 ou un aryle; R5 et R6 représentent chacun indépendamment de l'hydrogène, un alkyle C1-6, un aryle ou un (alkyle C1-3)aryle; ou, R5 et R6 pris ensemble peuvent former un cycle de 4, 5 ou 6 chaînons; R7 et R8 représentent chacun indépendamment de l'hydrogène, un groupe alkyle C1-6, aryle ou (alkyle C1-3)aryle; R9 représente de l'hydrogène, un groupe alkyle C1-6, aryle ou (alkyle C1-3)aryle; R10 représente -CONR5R6, -SO2NR5R6, -NR7COR8, -NR7SO2R8, -NR7CONR5R6, -S(O)XR8 ou -NR7COOR9; m est 0, 1, 2 ou 3; n est 0, 1 ou 2; y est 0, 1 ou 2; enfin, x est 1 ou 2. On décrit également les sels pharmacocompatibles de ces composés; ces derniers et leurs sels sont utiles pour la prévention ou le traitement des troubles émétisants, non associés à la migraine.

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