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    NOVEL THIADIAZOLYL DERIVATIVES OF DNA POLYMERASE THETA INHIBITORS
    1.
    发明申请
    NOVEL THIADIAZOLYL DERIVATIVES OF DNA POLYMERASE THETA INHIBITORS 审中-公开

    公开(公告)号：WO2023060573A1

    公开(公告)日：2023-04-20

    申请号：PCT/CN2021/124155

    申请日：2021-10-15

    Applicant: BEIJING DANATLAS PHARMACEUTICAL CO., LTD.

    Inventor： LI, Helen

    IPC: C07D285/02 ,  C07D285/04 ,  C07D417/12 ,  A61K31/433 ,  A61P35/00

    Abstract: Poly theta inhibitor (I), X is -N-or -C-; ring A is phenyl or a five to ten membered heteroaryl ring containing, inclusive of X, one to four heteroatoms independently selected from nitrogen, oxygen, or sulfur, Ar1 is phenyl, heteroaryl, heterocyclyl, bicyclic heterocyclyl, bridged heterocyclyl, or spiroheterocyclyl, wherein each of the aforementioned ring is substituted with Ra, Rb, and/or Rc,wherein Ra and Rb are independently selected from hydrogen, alkyl, halo, haloalkyl, alkoxy, haloalkoxy, cycloalkyloxy, acyl, acylamino, monoalkylamino, dialkylamino, alkylsulfonyl,cyano, and hydroxy; or Ra and Rb, when on adjacent ring vertices, combine to form a C3-6 cycloalkyl, or Ra and Rb, when on the same ring vertex, combine to form oxo, and Rc is selected from hydrogen, alkyl, halo, haloalkyl, alkoxy, haloalkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, aminoalkyl, heterocyclylalkyl, heterocyclyloxy, aminocarbonyl; Ar2 is phenyl, heteroaryl, or cycloalkyl, wherein said phenyl and heteroaryl are substituted with Rd, Re and/or Rf, wherein Rd and Re are independently selected from hydrogen, alkyl, halo, haloalkyl, alkoxy, haloalkoxy, hydroxy, and cyano and Rf is selected from hydrogen, alkyl, cycloalkyl, halo, haloalkyl, alkoxy, haloalkoxy, hydroxy, cyano, cyanomethyl, aminocarbonylmethyl, heteroaryl, and heterocyclyl, wherein said heteroaryl and heterocyclyl of Rf are unsubstituted or substituted with one, two, or three substituents independently selected from alkyl, halo, haloalkyl, and hydroxy; R1 is hydrogen, alkyl, halo, haloalkyl, haloalkoxy, alkoxy, hydroxy, cyano, cyanoalkyl,carboxy, alkoxycarbonyl, acylamino, aminocarbonyl optionally substituted heteroaryl, hydroxyalkyl, cycloalkyl, hydroxyalkynyl, alkoxyalkyl, aminoalkyl, aminocarbonylalkyl,sulfonylalkyl, aminosulfonylalkyl, optionally substituted heteroaralkyl, or optionally substituted heterocyclylalkyl; and R2 is hydrogen, alkyl, halo, haloalkyl, haloalkoxy, or cyano; Y is O or S or NH or NRg, Rg is a C1 to C3 aliphatic group; R3 and R4 are H, C1-6 aliphatic group.

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