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公开(公告)号:US20110112089A1
公开(公告)日:2011-05-12
申请号:US13009773
申请日:2011-01-19
申请人: Magnus NILSSON , Xiao-Xiong ZHOU , Lourdes ODEN , Bjorn CLASSON , Rolf NOREN , Urszula GRABOWSKA , Philip JACKSON , Philip FALLON , Andrew CARR , Mark LILEY , Matt TOZER , Tony JOHNSON , Victor DIAZ , Laia CRESPO , Jussi KANGASMETSA , Thierry BONNAUD
发明人: Magnus NILSSON , Xiao-Xiong ZHOU , Lourdes ODEN , Bjorn CLASSON , Rolf NOREN , Urszula GRABOWSKA , Philip JACKSON , Philip FALLON , Andrew CARR , Mark LILEY , Matt TOZER , Tony JOHNSON , Victor DIAZ , Laia CRESPO , Jussi KANGASMETSA , Thierry BONNAUD
IPC分类号: A61K31/5365 , A61K31/407 , A61K31/427 , A61K31/454 , A61K31/497 , A61K31/4439 , A61K31/4178 , A61P19/10 , A61P35/00 , A61P37/00 , A61P19/08
CPC分类号: C07D491/04 , A61K31/407
摘要: 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.
摘要翻译: 式II的化合物,其中R 1和R 2中的一个是卤素,另一个是H或卤素; R3是C1-C4直链或支链,任选氟化的烷基; R4是H; 或R 3与R 4一起,相邻的主链碳定义:任选被1至3个选自卤素,羟基,C 1 -C 4烷基或C 1 -C 4卤代烷基的取代基取代的螺C5-C7环烷基; 或任选地与亚甲基桥连; 或具有选自O,NR a,S,S(= O)2的杂原子的C 4 -C 6饱和杂环; 其中R a是H,C 1 -C 4烷基或CH 3 C(= O); R5独立地选自H或甲基; E是-C(= O) - , - S(= O)m - , - NR 5 S(= O)m - , - NR 5 C(= O) - , - OC(= O) 取代的,单环或双环的,碳环或环状的; m独立地为0,1或2; 是组织蛋白酶K的抑制剂,可用于治疗或预防骨质疏松症。