Pleuromutilin derivatives for the treatment of diseases...

C - Chemistry – Metallurgy – 07 – C

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C07C 323/52 (2006.01) A61K 31/215 (2006.01) A61P 31/00 (2006.01)

Patent

CA 2678795

A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m = 0 then R3 is in position 2', and if m = 1 then R3 is on position 1'); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl; R2 is hydrogen or - (C3-6)cycloalkyl, or - unsubstituted (C1-6)alkyl, or - (C1-6)alkyl substituted by one or more of - hydroxy; preferably one or two, - methoxy, - halogen, - (C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatome e. g. selected from N or O, or R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or - with the proviso that R3 is bound to 2' R3 represents -O-(CH2)P-O- with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl.

L'invention porte sur un composé de formule (I), dans laquelle n vaut 0 à 4; m vaut 0 ou 1, à la condition que l'atome de soufre et R3 soient en position voisine (si m = 0, R3 est en position 2', et si m = 1, R3 est en position 1'); R représente éthyle ou vinyle; R1 représente hydrogène ou alkyle en C1-6; R2 représente hydrogène ou cycloalkyle en C3-6 ou alkyle en C1-6 non substitué ou alkyle en C1-6 substitué par un ou plusieurs hydroxy; de préférence un ou deux méthoxy, halogène, cycloalkyle en C3-6, ou R1 et R2, conjointement avec l'atome d'azote auquel ils sont attachés, forment un noyau hétérocyclique de 5 à 7 chaînons contenant au moins 1 atome d'azote ou 1 azote et 1 hétéroatome supplémentaire, par exemple, choisi parmi N ou O, ou R1 représente hydroxy et R2 représente formyle; R3 représente OH, OR4, un atome d'halogène, ou à la condition que R3 soit lié en 2', R3 représente -O-(CH2)p-O-, avec p valant 2 ou 3; R4 représente alkyle en C1-6 non substitué ou cycloalkyle en C3-6.

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