Cysteine protease inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 491/04 (2006.01) A61K 31/407 (2006.01)

Patent

CA 2552739

A compound of the formula (II) wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(=O)2 ; where Ra is H, C1-C4 alkyl or CH3C(=O); R5 is independently selected from H or methyl; E is -C(=O)- , -S(=O)m-, -NR5S(=O)m-, -NR5C(=O)-, -OC(=O)-, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.

L'invention concerne un composé représenté par la formule (II) dans laquelle R?1¿ ou R?2 ¿est halo et l'autre est H ou halo; R?3¿ est un C¿1?-C¿4?-alkyle linéaire ou ramifié, éventuellement fluoré; R?4¿ est H; ou R?3¿ et R?4¿ et la structure carbone adjacente forment un spiro-C¿5?-C¿7?-cycloalkyle éventuellement substitué avec 1 à 3 substituants sélectionnés parmi halo, hydroxyle, C¿1?-C¿4?-alkyl ou C¿1?-C¿4?-haloalkyle, éventuellement ponté avec un groupe méthylène, ou un hétérocycle C¿4?-C¿6 ?saturé portant un hétéroatome choisi parmi O, NRa, S, S(=O)¿2?, Ra étant H, C¿1?-C¿4?-alkyle ou CH¿3?C(=O); R?5 ¿est choisi indépendamment parmi H ou méthyle, E est -C(=O)-, -S(=O)¿m?-, -NR?5¿S(=O)¿m?-, -NR?5¿C(=O)-, -OC(=O)-; R?6 ¿est un carbocycle ou héréocycle monocyclique ou bicyclique stable, éventuellement substitué; et M est indépendamment 0, 1 ou 2. Le composé selon l'invention est un inhibiteur de cathépsine K et sert au traitement et à la prophylaxie de l'ostéoporose.

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