Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists...

C - Chemistry – Metallurgy – 07 – C

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C07C 217/10 (2006.01) A61K 31/135 (2006.01) A61K 31/415 (2006.01) A61K 31/47 (2006.01) A61P 11/00 (2006.01) C07C 217/26 (2006.01) C07C 233/43 (2006.01) C07C 275/32 (2006.01) C07D 215/26 (2006.01) C07D 233/74 (2006.01)

Patent

CA 2608493

The present invention provides a compound of formula (I) wherein: R1 is a group selected from -CH2OH, -NHC(O)H and R2 is a hydrogen atom; or R1 together with R2 form the group -NH-C(O)-CH=CH- wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is selected from hydrogen and halogen atoms or groups selected from -SO-R5, -SO2- R5, -NH-CO-NH2, -CO- NH2, hydantoino, C1-4alkyl, C1-4alkoxy and -SO2NR5R6; R4 is selected from hydrogen atoms, halogen atoms and C1-4alkyl groups; R5 is a C1-4alkyl group or C3-8 cycloalkyl; R6 is independently selected from hydrogen atoms and C1- 4alkyl groups; n, p and q are independently 0, 1 , 2, 3 or 4; m and s are independently 0, 1 , 2 or 3; r is 0, 1 or 2; with the provisos that: at least one of m and r is not 0; the sum n+m+p+q+r+s is 7, 8, 9, 10, 11 , 12 or 13; the sum q+r+s is 2, 3, 4, 5 or 6 or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof.

La présente invention concerne un composé représenté par la formule (I) dans laquelle R1 est un groupe sélectionné parmi -CH2OH, -NHC(O)H et R2 est un atome d'hydrogène; ou R1 et R2 forment le groupe -NH-C(O)-CH=CH- dans lequel l'atome d'hydrogène est lié à l'atome de carbone dans le noyau phényle supportant R1 et l'atome de carbone est lié à l'atome de carbone dans le noyau phényle supportant R2; R3 est sélectionné parmi des atomes d'hydrogène et d'halogène ou des groupes sélectionnés parmi -SO-R5, -SO2- R5, -NH-CO-NH2, -CO-NH2, hydantoïne, alkyle C1-4, alkoxy C1-4 et -SO2NR5R6; R4 est sélectionné parmi des atomes d'hydrogène, des atomes d'halogène, et des groupes alkyle C1-4; R5 est un groupe alkyle C1-4 ou cycloalkyle C3-8; R6 est indépendamment sélectionné parmi des atomes d'hydrogène et des groupes alkyle C1-4; n, p et q sont indépendamment 0, 1, 2, 3 ou 4; m et s sont indépendamment 0, 1, 2 ou 3; r est 0, 1 ou 2, à condition qu'au moins m ou r ne soit pas 0, la somme n+m+p+q+r+s soit 7, 8, 9, 10, 11, 12 ou 13, la somme q+r+s soit 2, 3, 4, 5 ou 6; ou un sel, un solvate ou un stéréoisomère acceptable d'un point de vue pharmaceutique dudit composé.

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