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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Hauptverfasser: NILSSON, Magnus, GRABOWSKA, Urszula, SAMUELSSON, Bertil, ODEN, Lourdes Salvador, KAHNBERG, Pia
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creator NILSSON, Magnus
GRABOWSKA, Urszula
SAMUELSSON, Bertil
ODEN, Lourdes Salvador
KAHNBERG, Pia
description 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.
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GRABOWSKA, Urszula ; SAMUELSSON, Bertil ; ODEN, Lourdes Salvador ; KAHNBERG, Pia</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US2022332690A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2022</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>NILSSON, Magnus</creatorcontrib><creatorcontrib>GRABOWSKA, Urszula</creatorcontrib><creatorcontrib>SAMUELSSON, Bertil</creatorcontrib><creatorcontrib>ODEN, Lourdes Salvador</creatorcontrib><creatorcontrib>KAHNBERG, Pia</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>NILSSON, Magnus</au><au>GRABOWSKA, Urszula</au><au>SAMUELSSON, Bertil</au><au>ODEN, Lourdes Salvador</au><au>KAHNBERG, Pia</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PROTEASE INHIBITORS</title><date>2022-10-20</date><risdate>2022</risdate><abstract>Compounds of the formula II:whereinR1 and R2 are independently H, F or CH3; 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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title PROTEASE INHIBITORS
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