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    S-IMINO-S-OXO IMINOTHIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    1.
    发明授权
    S-IMINO-S-OXO IMINOTHIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权

    公开(公告)号：EP2968357B1

    公开(公告)日：2018-07-04

    申请号：EP14770391.2

    申请日：2014-03-11

    申请人： Merck Sharp & Dohme Corp.

    发明人： KHAN, Tanweer, A. ,  SCOTT, Jack, D. ,  CUMMING, Jared, N.

    IPC分类号： C07D279/12 ,  C07D417/12 ,  A61K31/55 ,  A61P25/28

    CPC分类号： C07D279/12 ,  C07D417/12

    摘要： In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

    SELECTIVE INHIBITION OF MALT1 PROTEASE BY PHENOTHIAZINE DERIVATIVES
    8.
    发明公开
    SELECTIVE INHIBITION OF MALT1 PROTEASE BY PHENOTHIAZINE DERIVATIVES 有权
    选择性INHIBITING MALT1蛋白酶的研究吩噻嗪

    公开(公告)号：EP2739285A1

    公开(公告)日：2014-06-11

    申请号：EP12741012.4

    申请日：2012-08-01

    申请人： Helmholtz Zentrum München Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH)

    发明人： KRAPPMANN, Daniel ,  NAGEL, Daniel ,  SCHENDEL, Dolores ,  SPRANGER, Stefani

    IPC分类号： A61K31/5415 ,  A61K31/546 ,  A61P35/00

    CPC分类号： A61K31/5415 ,  A61K31/546 ,  A61K45/06 ,  C07D279/12

    摘要： The invention relates to a compound for use in treating a cancer, wherein the cancer depends on the proteolytic activity of the MALT1 protease, and wherein the compound has the general formula (I) wherein X is N or C; Y is S, O, SO2, SO, NH, CO, CH2, CH═CH, CH2═CH2; ( )z is a C1-C5 linear or branched alkyl chain; A is NR3R4, or OR5, or HET; R1 and R2 in each occurrence are independently selected from —H, —CH3, —OH, —OCH3, —SCH3, —F, —Cl, —CF3, —NH2, and —COOH; R3, R4, and R5 are H, or C1-C5 linear or branched alkyl groups, and HET is a heterocyclic ring of 5, 6, or 7 members, wherein the ring atoms can be C, O, N, or S, the ring can be saturated or aromatic, and the ring can be substituted with H or C1-C5 linear or branched alkyl groups; or a pharmaceutically acceptable salt, prodrug, enantiomer, diastereomer, racemic mixture, crystalline form, amorphous form, unsolvated form or solvate of said compound. The compound of the invention may further be used in the treatment of MALT1-dependent immune diseases.