Protease inhibitors

Compounds of the formula II:whereinR1 and R2 are independently H, F or CH3; orR1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo;R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of wh...

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Bibliographic Details
Main Authors Nilsson, Magnus, Oden, Lourdes Salvador, Kahnberg, Pia, Samuelsson, Bertil, Grabowska, Urszula
Format Patent
LanguageEnglish
Published 28.07.2020
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:Compounds of the formula II:whereinR1 and R2 are independently H, F or CH3; orR1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo;R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem subsituted with fluoro;R4 is methyl or fluoro; m is 0, 1 or 2;E is a bond, or thiazolyl, optionally substituted with methyl or fluoro;A1 is CH or N,A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N;R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O-C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy or F;R7 is H, C1-C4 alkyl or For a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
Bibliography:Application Number: US201916449850