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    Tetrahydroisoquinolines as PRMT5 inhibitors
    6.
    发明授权
    Tetrahydroisoquinolines as PRMT5 inhibitors 有权

    公开(公告)号：US10421743B2

    公开(公告)日：2019-09-24

    申请号：US16081696

    申请日：2017-03-09

    申请人： CTXT PTY LTD

    发明人： Ylva Elisabet Bergman ,  Michelle Ang Camerino ,  Scott Raymond Walker ,  Paul Anthony Stupple

    IPC分类号： C07D217/16 ,  A61K31/472 ,  C07D401/14 ,  C07D405/14 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D498/08 ,  C07D217/24 ,  C07D491/08 ,  A61P35/00

    摘要： A compound of formula (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from the group consisting of H, halo, C1-4 alkoxy, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH—C1-4 alkyl and cyano; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl; wherein when R2e is H, at least one of R1a, R1b, R1c and R1d is selected from C1-4 alkoxy, C2-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, NH—C1-4 alkyl and cyano.

    Benzopiperdine derivatives and their use in the treatment of cancer and hemoglobinopathies
    8.
    发明授权
    Benzopiperdine derivatives and their use in the treatment of cancer and hemoglobinopathies 有权

    公开(公告)号：US10787434B2

    公开(公告)日：2020-09-29

    申请号：US16082196

    申请日：2017-03-09

    申请人： CTXT PTY LTD

    发明人： Ylva Elisabet Bergman ,  Michelle Ang Camerino ,  Paul Anthony Stupple

    IPC分类号： C07D401/14 ,  C07D413/14

    摘要： A compound of formula I: (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH—C1-4 alkyl and cyano; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (IIa), where R7a is selected from N-linked N-containing C5-7 heterocycyl and (A); or (ii) (IIb), where X is selected from CH2, NH and O, one of R8a and R8b is selected from CI and ethoxy and the other of R8a and R8b is H.

    BENZOPIPERDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES
    9.
    发明申请
    BENZOPIPERDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES 审中-公开

    公开(公告)号：US20200010451A1

    公开(公告)日：2020-01-09

    申请号：US16082196

    申请日：2017-03-09

    申请人： CTXT PTY LTD

    发明人： Ylva Elisabet Bergman ,  Michelle Ang Camerino ,  Paul Anthony Stupple

    IPC分类号： C07D401/14 ,  C07D413/14

    摘要： A compound of formula I: (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH—C1-4 alkyl and cyano; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (IIa), where R7a is selected from N-linked N-containing C5-7 heterocycyl and (A); or (ii) (IIb), where X is selected from CH2, NH and O, one of R8a and R8b is selected from CI and ethoxy and the other of R8a and R8b is H.

    PRMT5 INHIBITORS
    10.
    发明申请
    PRMT5 INHIBITORS 审中-公开

    公开(公告)号：US20200002355A1

    公开(公告)日：2020-01-02

    申请号：US16082230

    申请日：2017-03-09

    申请人： CTXT PTY LTD

    发明人： Paul Anthony Stupple ,  Scott Raymond Walker ,  Michelle Ang Camerino

    IPC分类号： C07D498/08 ,  C07D237/32

    摘要： A compound of formula (Ia), (Ib) or (Ic) wherein: n is 1 or 2; RN is H or Me; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4a is selected from OH, —NH2, —C(═O)NH2, and —CH2OH; R4b is either H or Me; X is either N or CH; R7 is selected from H and C1-4 alkyl; (a) one of R8a, R8b, R8c and R8d is selected from H, halo, C1-4 alkyl, C1-4 alkoxy, NHC1-4 alkyl; (b) another of R8a, R8b, R8c and R8d is selected from H, C1-4 alkyl, C1-4 fluoroalkyl, C3-6 cycloalkyl, C5-6 heteroaryl, C5-6 heteroaryl methyl, C4-6 heterocyclyl, C4-6 heterocyclyl methyl, phenyl, benzyl, halo, amido, amidomethyl, acylamido, acylamidomethyl, C1-4 alkyl ester, C1-4 alkyl ester methyl, C1-4 alkyl carbamoyl, C1-4 alkyl carbamoyl methyl, C1-4 alkylacyl, C1-4 alkylacyl methyl, phenylcarbonyl, carboxy, carboxymethyl, ether, amino, amino methyl, sulfonamido, sulfonamino, sulfone, sulfoxide, nitrile and nitrilemethyl; (c) the others of R8a, R8b, R8c and R8d are H.