Peptidyl compounds and their therapeutic use as inhibitors...

Details Peptidyl compounds and their therapeutic use as inhibitors... Peptidyl compounds and their therapeutic use as inhibitors...

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) A61K 38/05 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2173470

A compound of formula (I), wherein R1 is C1-6 alkyl, C2-6 alkenyl, aryl, (C1-6 alkyl)aryl or C1-6 alkyl-AR9 where A is O, NR9 or S(O)m, where m = 0-2, and the or each R9 is H, C1-4 alkyl, aryl or (C1-4 alkyl)aryl; R2 is H or C1-6 alkyl; either R4 is H or C1-6 alkyl optionally substituted by amino (NH2), arylamino, protected amino, aryl, di(C1-6 alkyl)amino, mono(C1-6 alkyl)amino, CO2H, protected carboxyl, carbamoyl, mono(C1-6 alkyl)carbamoyl or di(C1-6 alkyl)carbamoyl, and R5 is H or C1-6 alkyl, or NR4R5 is pyrrolidino, piperidino or morpholino; R6 is optionally-substituted C3-6 cycloalkyl, C3-6 cycloalkenyl, C1-6 alkyl, benzyl, (C1-6 alkoxy)benzyl, benzyloxybenzyl or 3- indolylmethyl; Alk is C1-6 alkyl or C2-6 alkenyl and n = 0 or 1; R7 is H or R10CO where R10 is C1-4 alkyl, (C1-4 alkyl)aryl, C3-6 cycloalkyl, (C3-6 cycloalkyl)C1-4 alkyl, C2-6 alkenyl or (C2-6 alkenyl)aryl; and R8 is H, C1-4 alkyl, (C1-4 alkyl)aryl or aryl; or a salt, solvate or hydrate thereof. Such compounds may be used to treat conditions associated with metalloproteinase, TNF and/or other activity.

L'invention se rapporte à des composés de la formule (I) ainsi qu'à leurs sels, solvates ou hydrates. Dans cette formule, R?1¿ est alkyle C¿1-6?, alcényle C¿2-6?, aryle, (alkyle C¿1-6?)aryle ou alkyle C¿1-6? -AR?9¿ dans laquelle A est O, NR?9¿ ou S(O)¿m?, dans laquelle m=0-2, et R?9¿ ou chaque R?9¿ est H, alkyle C¿1-4?, aryle ou (alkyle C¿1-4?)aryle; R?2¿ est H ou alkyle C¿1-6?; soit R?4¿ est H ou alkyle C¿1-6? facultativement substitué par amino (NH¿2?), arylamino, amino protégé, aryle, di(alkyle C¿1-6?)amino, mono(alkyle C¿1-6?)amino, CO¿2?H, carboxyle protégé, carbamyle, mono(alkyle C¿1-6?)carbamyle ou di(alkyle C¿1-6?)carbamyle, et R?5¿ est H ou alkyle C¿1-6?, soit NR¿4?R¿5? est pyrrolidino, pipéridino ou morpholino; R?6¿ est cycloalkyle C¿3-6? facultativement substitué, cycloalcényle C¿3-6?, alkyle C¿1-6?, benzyle, (alcoxy C¿1-6?)benzyle, benzyloxybenzyle ou 3-indolylméthyle; Alk est alkyle C¿1-6? ou alcényle C¿2-6? et n=0 ou 1; R?7¿ est H ou R?10¿CO dans laquelle R?10¿ est alkyle C¿1-4?, (alkyle C¿1-4?)aryle, cycloalkyle C¿3-6?)alkyle C¿1-4?, alcényle C¿2-6? ou (alcényle C¿2-6?)aryle; et R?8¿ est H, alkyle C¿1-4?, (alkyle C¿1-4?)aryle ou aryle. On peut utiliser de tels composés dans le traitement d'états associés à la métalloprotéase, à l'activité du facteur de nécrose des tumeurs (TNF) et/ou d'un autre facteur.

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