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    PHARMACEUTICAL COMPOSITIONS FOR USE IN THE PREVENTION AND TREATMENT OF A DISEASE OR DISORDER CAUSED BY OR ASSOCIATED WITH ONE OR MORE PREMATURE TERMINATION CODONS
    4.
    发明公开
    PHARMACEUTICAL COMPOSITIONS FOR USE IN THE PREVENTION AND TREATMENT OF A DISEASE OR DISORDER CAUSED BY OR ASSOCIATED WITH ONE OR MORE PREMATURE TERMINATION CODONS 审中-公开

    公开(公告)号：US20240216355A1

    公开(公告)日：2024-07-04

    申请号：US18471563

    申请日：2023-09-21

    申请人： Monte Rosa Therapeutics, Inc.

    发明人： Bernhard Fasching ,  Gerald Gavory ,  Lev Osherovich

    IPC分类号： A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/7048 ,  A61P11/00 ,  A61P35/00

    CPC分类号： A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/7048 ,  A61P11/00 ,  A61P35/00

    摘要： The present disclosure relates to a compound of formula I or a pharmaceutically acceptable salt thereof




    wherein A is




    X1 is linear or branched C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-8 membered heterocycloalkyl, wherein X1 is unsubstituted or substituted with one or more of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, CMeF2, —O—CHF2, —O—(CH2)2—OMe, OCF3, C1-6 alkylamino, —CN, —N(H)C(O)—C1-6alkyl, —OC(O)—C1-6alkyl, —OC(O)—C1-4alkylamino, —C(O)O—C1-6alkyl, —COOH, —CHO, —C1-6alkylC(O)OH, —C1-6alkylC(O)O—C1-6alkyl, NH2, C1-6 alkoxy or C1-6 alkylhydroxy; or X1 together with X4 forms a 4-8 membered heterocycloalkyl, which is unsubstituted or substituted with one or more of halogen, linear or branched —C1-6 alkyl, CF3, CHF2, CMeF2, —O—(CH2)2—OMe, OCF3, OCHF2, C1-6 alkylamino, —CN, —N(H)C(O)—C1-6alkyl, —OC(O)—C1-6alkyl, —C(O)O—C1-6alkyl, —COOH, —C1-6alkylC(O)OH, —C1-6alkylC(O)O—C1-6alkyl, NH2, C1-4 alkylhydroxy, or C1-6 alkoxy; X2 is hydrogen, C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-8 membered heterocycloalkyl, wherein X2 is unsubstituted or substituted with one or more of linear or branched C1-6 alkyl, —C1-4 alkoxy, NH2, NMe2, halogen, CF3, CHF2, CMeF2, —O—(CH2)2—OMe, OCF3, OCHF2, C1-4 alkylhydroxy; X3 is —NH—, —O—; X4 is —NH—, —CH2—; L1 is a covalent bond, C1-6 alkyl, which is unsubstituted or substituted with one or more of C1-4 alkyl, halogen; L2 is a covalent bond, C1-6 alkyl, which is unsubstituted or substituted with one or more of C1-4 alkyl, halogen; L3 is a covalent bond, —O—, —C1-4 alkoxy or C1-6 alkyl, which is unsubstituted or substituted with one or more of C1-4 alkyl, halogen, for use in the prevention and treatment of a disease or disorder caused by or associated with one or more premature termination codons in a monotherapy or in a combined therapy with an aminoglycoside or a pharmaceutically acceptable salt thereof.

    ISOINDOLINONE COMPOUNDS
    5.
    发明公开
    ISOINDOLINONE COMPOUNDS 审中-公开

    公开(公告)号：US20240051936A1

    公开(公告)日：2024-02-15

    申请号：US18485766

    申请日：2023-10-12

    申请人： Monte Rosa Therapeutics, Inc.

    发明人： Bernhard Fasching ,  Thomas Ryckmans ,  Alexander Flohr

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  A61P35/00

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  A61P35/00

    摘要： Disclosed herein are compound or pharmaceutically acceptable salts or stereoisomers thereof of formula I:






    wherein X1 is selected from the group consisting of linear or branched C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, and 4-8 membered heterocycloalkyl, wherein X1 is unsubstituted or substituted with one or more substituents independently selected from the group consisting of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, CMeF2, —O—CHF2, —O—(CH2)2—OMe, OCF3, C1-6 alkylamino, —CN, NH2, C1-4 alkoxy and C1-4 alkylhydroxy; X2 is selected from the group consisting of H, C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, and 4-8 membered heterocycloalkyl, wherein X2 is unsubstituted or substituted with one or more substituents independently selected from the group consisting of linear or branched C1-6 alkyl, —C1-4 alkoxy, NH2, NMe2, halogen, CF3, CHF2, CMeF2, —O—(CH2)2—OMe, OCF3, OCHF2, and C1-4 alkylhydroxy; Y is selected from the group consisting of linear or branched C1-6 alkyl, —C1-4 alkoxy, —CN, halogen, CF3, CHF2, CMeF2, OCF3, and OCHF2; L1 is linear or branched C1-6 alkyl; L2 is selected from a covalent bond, and linear or branched C1-6 alkyl; and L3 is selected from the group consisting of a covalent bond, linear or branched C1-6 alkyl, —O—, and —C1-4 alkoxy. Disclosed herein is also their use as modulators of cereblon, methods of preparation of these compounds, compositions comprising these compounds, and methods of using them in the treatment of abnormal cell growth in mammals, especially humans.

    ISOINDOLINONE COMPOUNDS
    6.
    发明公开
    ISOINDOLINONE COMPOUNDS 审中-公开

    公开(公告)号：US20240083869A1

    公开(公告)日：2024-03-14

    申请号：US18496504

    申请日：2023-10-27

    申请人： Monte Rosa Therapeutics, Inc.

    发明人： Bernhard Fasching ,  Thomas Ryckmans ,  Alexander Flohr ,  Andreas Ritzén ,  Freya Harvey ,  Laura McAllister

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04

    摘要： Disclosed herein are compound or pharmaceutically acceptable salts or stereoisomers thereof of formula I:




    X1 is linear or branched C1-6 alkyl, C3-8 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-8 membered heterocycloalkyl, wherein X1 is unsubstituted or substituted with one or more of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, CMeF2, —O—CHF2, —O—(CH2)2—OMe, OCF3, C1-6 alkylamino, —CN, —N(H)C(O)—C1-6alkyl, —OC(O)—C1-6alkyl, —OC(O)—C1-4alkylamino, —C(O)O—C1-6alkyl, —COOH, —C1-6alkylC(O)OH, —C1-6alkylC(O)O—C1-6alkyl, NH2, C1-4 alkoxy, C1-4 alkylhydroxy, —CH2F, —N(H)C(O)—O—C1-6 alkyl, and C(OH)(CF3); or X1 together with the N atom of the carbamate forms a 4-8 membered heterocycloalkyl, which is unsubstituted or substituted with one or more of halogen, linear or branched —C1-6 alkyl, CF3, CHF2, CMeF2, —O—(CH2)2—OMe, OCF3, OCHF2, C1-6 alkylamino, —CN, —N(H)C(O)—C1-6alkyl, —OC(O)—C1-6alkyl, —C(O)O—C1-6alkyl, —COOH, —C1-6alkylC(O)OH, —C1-6alkylC(O)O—C1-6alkyl, NH2, C1-4 alkylhydroxy, and C1-4 alkoxy; X2 is H, C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-8 membered heterocycloalkyl, wherein X2 is unsubstituted or substituted with one or more of linear or branched C1-6 alkyl, —C1-4 alkoxy, NH2, NMe2, halogen, CF3, CHF2, CMeF2, —O—(CH2)2—OMe, OCF3, OCHF2, and C1-4 alkylhydroxy; L1 is a covalent bond, linear or branched C1-6 alkyl; L2 is a covalent bond, linear or branched C1-6 alkyl; and L3 is a covalent bond, linear or branched C1-6 alkyl, —O—, or —C1-4 alkoxy, wherein linear or branched C1-6 alkyl is unsubstituted or substituted with one or more of halogen. Disclosed herein is also their use as modulators of cereblon, methods of preparation of these compounds, compositions comprising these compounds, and methods of using them in the treatment of abnormal cell growth in mammals, especially humans.

    Isoindolinone compounds
    7.
    发明授权
    Isoindolinone compounds 有权

    公开(公告)号：US11912682B2

    公开(公告)日：2024-02-27

    申请号：US18349634

    申请日：2023-07-10

    申请人： Monte Rosa Therapeutics, Inc.

    发明人： Bernhard Fasching ,  Thomas Ryckmans ,  Alexander Flohr

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04

    摘要： Disclosed herein are compound or pharmaceutically acceptable salts or stereoisomers thereof of formula I:




    X1 is linear or branched C1-6 alkyl, C3-8 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-8 membered heterocycloalkyl, wherein X1 is unsubstituted or substituted with one or more of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, CMeF2, —O—CHF2, —O—(CH2)2—OMe, OCF3, C1-6 alkylamino, —CN, —N(H)C(O)—C1-6alkyl, —OC(O)—C1-6alkyl, —OC(O)—C1-4alkylamino, —C(O)O—C1-6alkyl, —COOH, —C1-6alkylC(O)OH, —C1-6alkylC(O)O—C1-6alkyl, NH2, C1-4 alkoxy, C1-4 alkylhydroxy, —CH2F, —N(H)C(O)—O—C1-6 alkyl, and C(OH)(CF3); or X1 together with the N atom of the carbamate forms a 4-8 membered heterocycloalkyl, which is unsubstituted or substituted with one or more of halogen, linear or branched —C1-6 alkyl, CF3, CHF2, CMeF2, —O—(CH2)2—OMe, OCF3, OCHF2, C1-6 alkylamino, —CN, —N(H)C(O)—C1-6alkyl, —OC(O)—C1-6alkyl, —C(O)O—C1-6alkyl, —COOH, —C1-6alkylC(O)OH, —C1-6alkylC(O)O—C1-6alkyl, NH2, C1-4 alkylhydroxy, and C1-4 alkoxy; X2 is H, C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-8 membered heterocycloalkyl, wherein X2 is unsubstituted or substituted with one or more of linear or branched C1-6 alkyl, —C1-4 alkoxy, NH2, NMe2, halogen, CF3, CHF2, CMeF2, —O—(CH2)2—OMe, OCF3, OCHF2, and C1-4 alkylhydroxy; L1 is a covalent bond, linear or branched C1-6 alkyl; L2 is a covalent bond, linear or branched C1-6 alkyl; and L3 is a covalent bond, linear or branched C1-6 alkyl, —O—, or —C1-4 alkoxy, wherein linear or branched C1-6 alkyl is unsubstituted or substituted with one or more of halogen. Disclosed herein is also their use as modulators of cereblon, methods of preparation of these compounds, compositions comprising these compounds, and methods of using them in the treatment of abnormal cell growth in mammals, especially humans.

    ISOINDOLINONE COMPOUNDS
    8.
    发明公开
    ISOINDOLINONE COMPOUNDS 审中-公开

    公开(公告)号：US20230348418A1

    公开(公告)日：2023-11-02

    申请号：US18349634

    申请日：2023-07-10

    申请人： Monte Rosa Therapeutics, Inc.

    发明人： Bernhard Fasching ,  Thomas Ryckmans ,  Alexander Flohr

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04

    摘要： Disclosed herein are compound or pharmaceutically acceptable salts or stereoisomers thereof of formula I.






    X1 is linear or branched C1-6 alkyl, C3-8 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-8 membered heterocycloalkyl, wherein X1 is unsubstituted or substituted with one or more of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, CMeF2, —O—CHF2, —O—(CH2)2-OMe, OCF3, C1-6 alkylamino, —CN, —N(H)C(O)—C1-6alkyl, —OC(O)—C1-6alkyl, —OC(O)—C1-4alkylamino, —C(O)O—C1-6alkyl, —COOH, —C1-6 alkylC(O)OH, —C1-6alkylC(O)O—C1-6alkyl, NH2, C1-4 alkoxy, C1-4 alkylhydroxy, —CH2F, —N(H)C(O)—O—C1-6 alkyl, and C(OH)(CF3); or X1 together with the N atom of the carbamate forms a 4-8 membered heterocycloalkyl, which is unsubstituted or substituted with one or more of halogen, linear or branched —C1-6 alkyl, CF3, CHF2, CMeF2, —O—(CH2)2-OMe, OCF3, OCHF2, C1-6 alkylamino, —CN, —N(H)C(O)—C1-6alkyl, —OC(O)—C1-6alkyl, —C(O)O—C1-6alkyl, —COOH, —C1-6alkylC(O)OH, —C1-6alkylC(O)O—C1-6alkyl, NH2, C1-4 alkylhydroxy, and C1-4 alkoxy; X2 is H, C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-8 membered heterocycloalkyl, wherein X2 is unsubstituted or substituted with one or more of linear or branched C1-6 alkyl, —C1-4 alkoxy, NH2, NMe2, halogen, CF3, CHF2, CMeF2, —O—(CH2)2—OMe, OCF3, OCHF2, and C1-4 alkylhydroxy; L1 is a covalent bond, linear or branched C1-6 alkyl; L2 is a covalent bond, linear or branched C1-6 alkyl; and L3 is a covalent bond, linear or branched C1-6 alkyl, —O—, or —C1-4 alkoxy, wherein linear or branched C1-6 alkyl is unsubstituted or substituted with one or more of halogen. Disclosed herein is also their use as modulators of cereblon, methods of preparation of these compounds, compositions comprising these compounds, and methods of using them in the treatment of abnormal cell growth in mammals, especially humans.