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    POLYMORPHS OF BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AND USES THEREOF
    2.
    发明公开
    POLYMORPHS OF BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AND USES THEREOF 审中-公开

    公开(公告)号：US20230357167A1

    公开(公告)日：2023-11-09

    申请号：US18023767

    申请日：2021-09-02

    申请人： Bristol-Myers Squibb Company

    发明人： Marta DABROS ,  Joshua ENGSTROM ,  Daniel Richard ROBERTS

    IPC分类号： C07D243/24

    CPC分类号： C07D243/24 ,  C07B2200/13

    摘要： The present invention provides a crystalline form of (2R,3S)-N-((3S)-5-(3-fluorophenyl)-9-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinimide, represented by the structure of Compound (1), wherein the crystalline form comprises N-2 crystalline form, IPA2-1 crystalline form, M3-1 crystalline form, P4 crystalline form, P5 crystalline form, P6 crystalline form, or any combination thereof. The present invention also provides processes for the preparation of a the crystalline form, and pharmaceutical compositions comprising one or more of the crystalline forms.

    1,4-benzodiazepin-2-one derivatives and use thereof
    3.
    发明授权
    1,4-benzodiazepin-2-one derivatives and use thereof 有权

    公开(公告)号：US11358939B2

    公开(公告)日：2022-06-14

    申请号：US16766649

    申请日：2018-12-29

    申请人： INNOVATION PHARMACOLOGY RESEARCH OOO (“IPHAR”)

    发明人： Viktor Ivanovich Pavlovsky ,  Veniamin Abramovich Khazanov ,  Sergey Aleksandrovich Stankevich

    IPC分类号： A61K31/5513 ,  A61P25/04 ,  A61P25/24 ,  A61P25/28 ,  C07D243/24

    摘要： The invention relates to novel compounds that are derivatives of 1,4-benzodiazepin-2-one, having the general formula I: and being limited to structural variants 1-6: on condition that: a) structures 1 (R1=Br, R4=F), 3 (R1=OCF3, R4=H), 5 (R1=NO2, R4=Cl) and 6 (R1=NO2, R4=F) have the following substituents R2 and R3: R2=H, CH2COCH3, CH2COOCH3, CH2CONHNH2; R3=OAlk, NHAr, where Alk=C2H5, C3H7, C4H9, (CH2)2OH, (CH2)2OCH3, R5=o-, m-, p-COCH3, Cl, F, Br, NO2, CF3; b) structure 2 (R1=Cl, R4=H) has the following substituents R2 and R3: if R2=H, then R3=OAlk, NHAr, where Alk=(CH2)2OCH3, R5=m-, p-COCH3, o-, m-, p-F, Br, CF3;  if R2=CH2COCH3, CH2COOCH3, CH2CONHNH2, then R3=OAlk, NHAr, where Alk=C2H5, C3H7, C4H9, (CH2)2OH, (CH2)2OCH3, R5=o-, m-, p-COCH3, Cl, F, Br, NO2, CF3; c) structure 4 (R1=NO2, R4=H) has the following substituents R2 and R3: if R2=H, then R3=OAlk, NHAr, where Alk=(CH2)2OCH3, R5=o-, m-, p-COCH3, Cl, F, Br, NO2, CF3;  if R2=CH2COCH3, CH2COOCH3, CH2CONHNH2, then R3=OAlk, NHAr, where Alk=C2H5, C3H7, C4H9, (CH2)2OH, (CH2)2OCH3, R5=o-, m-, p-COCH3, Cl, F, Br, NO2, CF3 and the use of said compounds in the field of medicine as analgesics, anorexigenic or orexigenic agents for weight regulation (loss or gain), antidepressants and anxiolytics for treating psychological disorders, and also antihypoxic and nootropic agents for the prophylaxis and treatment of central nervous system disorders.