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    Novel SIK Inhibitors
    1.
    发明公开
    Novel SIK Inhibitors 审中-公开

    公开(公告)号：US20240124450A1

    公开(公告)日：2024-04-18

    申请号：US18466034

    申请日：2023-09-13

    Applicant: Pfizer Inc.

    Inventor： Andrea Nicole Bootsma ,  David Christopher Ebner ,  Daniel Wei-Shung Kung ,  Matthew Alexander Perry ,  Daniel Copley Schmitt ,  Joseph Walter Strohbach ,  Atli Thorarensen

    IPC: C07D471/04

    CPC classification number: C07D471/04

    Abstract: A compound of formula I having the structure:




    or a pharmaceutically acceptable salt thereof, wherein A1 and A2 are independently O or S; X is selected from CH2, CD2, NR3, O, and S, where R3 is selected from hydrogen, C1-C4 linear or branched chain alkyl, halo(C1-C4)linear or branched chain alkyl, and hydroxyl(C1-C4)linear or branched chain alkyl; Y and Z are selected from C and N, where when Y is C, then Z is N, and when Y is N, then Z is C; R1 and R2 are independently selected from hydrogen, deuterium, C1-C4 linear or branched chain alkyl, etc.; or a C1-C2 alkyl substituted with a C3-C5 cycloalkyl ring; or taken together to form a C3-C6 cycloalkyl ring; or where X is CH2 or CD2, then R1 and R2 are independently selected from hydrogen, deuterium, halogen, hydroxyl, C1-C4 linear or branched chain alkyl, etc.; R4 is selected from hydrogen, deuterium, cyano, halogen, (C1-C3) alkoxy, etc.; R5 is selected from hydrogen, deuterium, halogen, C1-C3 alkoxy, amino, (C1-C4 linear or branched chain alkyl)amino, etc.; R6 is selected from hydrogen, deuterium, halogen, CO2R7 where R7 is selected from H and C1-C4 linear or branched chain alkyl, etc.; R8 is selected from hydrogen, deuterium, and C1-C3 linear or branched chain alkyl; R9 is selected from C1-C3 linear or branched chain alkyl, and a halo(C1-C3)linear or branched chain alkyl; and, n and m are independently selected from 0, 1 and 2. The invention also relates to pharmaceutical compositions thereof and therapeutic methods of use therewith.

    NOVEL ACC INHIBITORS
    6.
    发明公开
    NOVEL ACC INHIBITORS 审中-公开

    公开(公告)号：US20240109915A1

    公开(公告)日：2024-04-04

    申请号：US18359709

    申请日：2023-07-26

    Applicant: Pfizer Inc.

    Inventor： Scott William Bagley ,  Andrea Nicole Bootsma ,  Chulho Choi ,  Robert Lee Dow ,  David James Edmonds ,  Carmen Noemi Garcia-Irizarry ,  Brian Stephen Gerstenberger ,  Gajendra Ingle ,  Jessica Gloria Katherine O'Brien ,  Mihir Dineshkumar Parikh ,  Gwenaella Christine Rescourio ,  Daniel Copley Schmitt

    IPC: C07D513/10

    CPC classification number: C07D513/10

    Abstract: A compound having the structures:




    or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein; R selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy and —(CH2)m—W, where W is C3-C8 cycloalkyl, bicycloalkyl, bridged bicycloalkyl, phenyl, 5- or 6-membered heteroaryl or heterocyclic containing one, two or three heteroatoms selected from the group consisting of N, S and O atoms; wherein each of said alkyl, cycloalkyl, alkoxy, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, halo, cyano, deuterium, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, —SO2—R′, —CONR′R″, NR′COR″, —NR′CONR′R″, —NR′CO2R″, —(CH2)n—SO2—R′, —NHSO2—R′, —NR″SO2—R′, —SO2NR′R″, NR′R″ or SR′ where R′ and R″ are independently H, C1-C6 alkyl or C3-C8 cycloalkyl; R1 selected from the group consisting of phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing one, two, three or four heteroatoms selected from the group consisting of N, S and O atoms; and, a 9- or 10-membered bicyclic aryl, heteroaryl or heterocyclic containing one, two or three heteroatoms selected from the group consisting of N, S and O atoms; wherein each of said phenyl, naphthyl, aryl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, deuterium, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, phenyl, —SO2—R′, —CONR′R″, NR′COR″, —NR′CONR′R″, —NR′CO2R″, —(CH2)n—SO2—R′, —NHSO2—R′, —NR″SO2—R, —SO2NR′R″, —P(O)R′R″,




    or NR′R″′ or SR′ where R′ and R″ are independently H, C1-C6 alkyl or C3-C8 cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly acne.

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