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Cysteine protease inhibitors
专利权人:
Urszula Grabowska;Daniel Jonsson;Ellen Hewitt;Bjorn Klasson;Stina Lundgren;Pia Kahnberg;Jan Tejbrant;Susana Ayesa;Daniel Wiktelius
发明人:
Susana Ayesa,Urszula Grabowska,Ellen Hewitt,Daniel Jonsson,Bjorn Klasson,Pia Kahnberg,Stina Lundgren,Jan Tejbrant,Daniel Wiktelius
申请号:
US13704441
公开号:
US08859505B2
申请日:
2011.06.16
申请国别(地区):
US
年份:
2014
代理人:
摘要:
Compounds of the formula IwhereinR2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a andR2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl;R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; orR3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; orR3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy;R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or;R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy;n is 1, 2 or 3;for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
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