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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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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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.</description><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>2022</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20221020&DB=EPODOC&CC=US&NR=2022332690A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20221020&DB=EPODOC&CC=US&NR=2022332690A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>NILSSON, Magnus</creatorcontrib><creatorcontrib>GRABOWSKA, Urszula</creatorcontrib><creatorcontrib>SAMUELSSON, Bertil</creatorcontrib><creatorcontrib>ODEN, Lourdes Salvador</creatorcontrib><creatorcontrib>KAHNBERG, Pia</creatorcontrib><title>PROTEASE INHIBITORS</title><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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2022</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZBAOCPIPcXUMdlXw9PPwdPIM8Q8K5mFgTUvMKU7lhdLcDMpuriHOHrqpBfnxqcUFicmpeakl8aHBRgZGRsbGRmaWBo6GxsSpAgDkEx9m</recordid><startdate>20221020</startdate><enddate>20221020</enddate><creator>NILSSON, Magnus</creator><creator>GRABOWSKA, Urszula</creator><creator>SAMUELSSON, Bertil</creator><creator>ODEN, Lourdes Salvador</creator><creator>KAHNBERG, Pia</creator><scope>EVB</scope></search><sort><creationdate>20221020</creationdate><title>PROTEASE INHIBITORS</title><author>NILSSON, Magnus ; 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; 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.</abstract><oa>free_for_read</oa></addata></record> |
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subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS METALLURGY ORGANIC CHEMISTRY |
title | PROTEASE INHIBITORS |
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