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563 条记录 (耗时 0.045 秒)

    PROTEASE INHIBITORS
    5.
    发明申请
    PROTEASE INHIBITORS 有权

    公开(公告)号：US20220332690A1

    公开(公告)日：2022-10-20

    申请号：US17728943

    申请日：2022-04-25

    申请人： MEDIVIR AB

    发明人： Lourdes Salvador ODEN ,  Magnus NILSSON ,  Pia KAHNBERG ,  Bertil SAMUELSSON ,  Urszula GRABOWSKA

    IPC分类号： C07D277/40 ,  C07D491/048 ,  C07D495/04

    摘要： Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 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 F or 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.

    Ribonucleotide reductase inhibitors and methods of use
    8.
    发明授权
    Ribonucleotide reductase inhibitors and methods of use 有权

    公开(公告)号：US10155732B2

    公开(公告)日：2018-12-18

    申请号：US15725181

    申请日：2017-10-04

    申请人： City of Hope

    发明人： David Horne ,  Christopher Lincoln

    IPC分类号： C07D277/46 ,  C07C45/68 ,  C07D277/40 ,  C07D417/12

    摘要： Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.

    PROTEASE INHIBITORS
    9.
    发明申请
    PROTEASE INHIBITORS 审中-公开

    公开(公告)号：US20180327371A1

    公开(公告)日：2018-11-15

    申请号：US15941947

    申请日：2018-03-30

    申请人： MEDIVIR AB

    发明人： Lourdes Salvador ODEN ,  Magnus NILSSON ,  Pia KAHNBERG ,  Bertil SAMUELSSON ,  Urszula GRABOWSKA

    IPC分类号： C07D277/40 ,  C07D495/04 ,  C07D491/048

    CPC分类号： C07D277/40 ,  C07D491/048 ,  C07D495/04

    摘要： Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 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 substituted 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 F or 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.