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9 条记录 (耗时 0.024 秒)

    BET-PROTEIN-INHIBITING DIHYDROPYRIDOPYRAZINONES
    1.
    发明申请
    BET-PROTEIN-INHIBITING DIHYDROPYRIDOPYRAZINONES 审中-公开
    β-蛋白抑制二氢吡咯烷酮

    公开(公告)号：US20160193206A1

    公开(公告)日：2016-07-07

    申请号：US14654572

    申请日：2013-12-17

    申请人： BAYER PHARMA AKTIENGESELLSCHAFT

    发明人： Norbert SCHMEES ,  Benjamin BADER ,  Bernard HAENDLER ,  Detlef STÖCKIGT ,  Pascale LEJEUNE ,  Amaury Ernesto FERNANDEZ-MONTALVAN ,  Timo STELLFELD ,  Daniel GALLENKAMP

    IPC分类号： A61K31/4985 ,  C07D493/10 ,  C07D495/10 ,  C07D471/04 ,  A61K31/5377

    CPC分类号： A61K31/4985 ,  A61K31/5377 ,  C07D471/04 ,  C07D493/10 ,  C07D495/10

    摘要： The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory, dihydropyridopyrazinones of the general formula (I) in which A, X, R1, R2, R3, R4, R4, R6, R7 and n have the meanings given in the description, to intermediates for preparation of the compounds according to the invention, to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders.This invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammation diseases, in atherosclerotic disorders and in male fertility control.

    摘要翻译： 本发明涉及通式（I）的BET蛋白抑制性特别是BRD4抑制性二氢吡啶并吡嗪酮，其中A，X，R 1，R 2，R 3，R 4，R 4，R 6，R 7和n具有 描述根据本发明的化合物的制备中间体，包含根据本发明的化合物的药物组合物，以及在过度增殖性疾病的情况下的预防和治疗用途，特别是在肿瘤性疾病的情况下。 本发明还涉及BET蛋白抑制剂在病毒感染，神经变性疾病，炎症疾病，动脉粥样硬化疾病和雄性生育调控中的用途。

    PYRROLO- AND PYRAZOLO-TRIAZOLODIAZEPINES AS BET-PROTEIN INHIBITORS FOR TREATING HYPERPROLIFERATIVE DISEASES
    3.
    发明申请
    PYRROLO- AND PYRAZOLO-TRIAZOLODIAZEPINES AS BET-PROTEIN INHIBITORS FOR TREATING HYPERPROLIFERATIVE DISEASES 审中-公开
    作为用于治疗高增殖性疾病的β-蛋白酶抑制剂的吡咯并 - 吡喃并吡唑并嘧啶

    公开(公告)号：US20160009725A1

    公开(公告)日：2016-01-14

    申请号：US14770000

    申请日：2014-02-17

    申请人： BAYER PHARMA AKTIENGESELLSCHAFT

    发明人： Norbert SCHMEES ,  Bernd BUCHMANN ,  Bernard HAENDLER ,  Roland NEUHAUS ,  Pascale LEJEUNE ,  Martin KRÜGER ,  Amaury Ernesto FERNANDEZ-MONTALVAN ,  Hermann KÜNZER

    IPC分类号： C07D487/14 ,  C07D498/08 ,  C07D495/10 ,  C07D491/08 ,  C07D491/107 ,  A61K31/551

    CPC分类号： C07D487/14 ,  A61K31/551 ,  C07D487/04 ,  C07D491/08 ,  C07D491/107 ,  C07D495/10 ,  C07D498/08

    摘要： What is described are BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, bicyclo- and spino-substituted pyrrolo- and pyrazolodiazepines of the general formula I in which X, Y, n, m, R1, R2, R3, R4 and R5 are each as defined in the description, to intermediates for preparation of the inventive compounds, to pharmaceutical compositions comprising the inventive compounds, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for tumour disorders. Also described is the use of the compounds according to the invention as BET protein inhibitors for benign hyperplasias, for atherosclerotic disorders, for sepsis, for autoimmune disorders, for vascular disorders, for viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for male fertility control.

    摘要翻译： 描述了通式I的其中X，Y，n，m，R 1，R 2，R 3，R 3，R 4，R 4，R 6，R 6， ，R4和R5各自如本说明书所定义，中间体用于制备本发明化合物，包含本发明化合物的药物组合物，以及用于过度增殖性疾病，特别是肿瘤病症的预防和治疗应用。 还描述了根据本发明的化合物作为用于良性增生，动脉粥样硬化性疾病，败血症，血管疾病，病毒感染，神经变性疾病，炎症性疾病，动脉粥样硬化性疾病的BET蛋白抑制剂的用途 并为男性生育控制。

    BET-PROTEIN-INHIBITING DIHYDROXYQUINOXALINONES
    4.
    发明申请
    BET-PROTEIN-INHIBITING DIHYDROXYQUINOXALINONES 审中-公开
    BET蛋白抑制二羟基喹喔啉酮

    公开(公告)号：US20150344444A1

    公开(公告)日：2015-12-03

    申请号：US14654576

    申请日：2013-12-17

    申请人： BAYER PHARMA AKTIENGESELLSCHAFT

    发明人： Norbert SCHMEES ,  Bernard HAENDLER ,  Detlef STÖCKIGT ,  Daniel GALLENKAMP

    IPC分类号： C07D241/44 ,  C07D405/12 ,  C07D495/10 ,  A61K31/5377 ,  C07D403/12 ,  C07D405/04 ,  A61K31/498 ,  C07D401/12 ,  C07D491/107

    CPC分类号： C07D241/44 ,  A61K31/498 ,  A61K31/5377 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D471/04 ,  C07D491/107 ,  C07D495/10

    摘要： The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory, dihydroquinoxalinones of the general formula (I) in which A, X, R1, R2, R3, R4, R5, R6, R7 and n are each as defined in the description, to intermediates for preparation of the inventive compounds, to pharmaceutical compositions comprising the inventive compounds, and to the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. This invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammation disorders, in atherosclerotic disorders and in male fertility control.

    摘要翻译： 本发明涉及通式（I）的BET蛋白抑制性特别是BRD4抑制性二氢喹喔啉酮，其中A，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和n各自如 描述，用于制备本发明化合物的中间体，包含本发明化合物的药物组合物，以及在过度增殖性疾病的情况下的预防和治疗用途，特别是在肿瘤性疾病的情况下。 本发明还涉及BET蛋白抑制剂在病毒感染，神经变性疾病，炎症疾病，动脉粥样硬化疾病和雄性生育控制中的用途。

    4-SUBSTITUTED PYRROLO- AND PYRAZOLO-DIAZEPINES
    6.
    发明申请
    4-SUBSTITUTED PYRROLO- AND PYRAZOLO-DIAZEPINES 审中-公开
    4-取代的吡咯并 - 吡唑并 - 二氮杂

    公开(公告)号：US20150376196A1

    公开(公告)日：2015-12-31

    申请号：US14769921

    申请日：2014-02-18

    申请人： BAYER PHARMA AKTIENGESELLSCHAFT

    发明人： Norbert SCHMEES ,  Bernd BUCHMANN ,  Bernard HAENDLER ,  Roland NEUHAUS ,  Pascale LEJEUNE ,  Martin KRÜGER ,  Amaury Ernesto FERNANDEZ-MONTALVAN ,  Hermann KÜNZER ,  Hartmut REHWINKEL

    IPC分类号： C07D487/14 ,  C07D519/00 ,  A61K31/5517

    CPC分类号： C07D487/14 ,  A61K31/5517 ,  C07D519/00

    摘要： BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, 4-substituted pyrrolo- and pyrazolodiazepines of the general formula I are described, in which X, Y, n, m, p, R1, R2, R3, R4 and R5 are each as defined in the description, as are pharmaceutical compositions comprising the inventive compounds, and the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. Also described is the use of the inventive compounds as BET protein inhibitors in benign hyperplasias, in atherosclerotic disorders, in sepsis, in autoimmune disorders, in vascular disorders, in viral infections, in neurodegenerative disorders, in inflammatory disorders and in male fertility control.

    摘要翻译： 描述了通式I中的β蛋白抑制特别是BRD2-，BRD3-和BRD4抑制性4-取代的吡咯并 - 吡唑并二氮杂，其中X，Y，n，m，p，R1，R2，R3，R4 和R5各自如说明书中所定义，以及包含本发明化合物的药物组合物，以及在过度增殖性疾病的情况下的预防和治疗用途，特别是在肿瘤性疾病的情况下。 还描述了本发明化合物作为良性增生中的BET蛋白抑制剂，动脉粥样硬化病症，败血症，自身免疫性疾病，血管病症，病毒感染，神经变性疾病，炎症性疾病和雄性生育控制中的用途。

    COMBINATION OF A PI3K-INHIBITOR WITH AN ANDROGEN RECEPTOR ANTAGONIST
    7.
    发明申请
    COMBINATION OF A PI3K-INHIBITOR WITH AN ANDROGEN RECEPTOR ANTAGONIST 审中-公开

    公开(公告)号：US20200222414A1

    公开(公告)日：2020-07-16

    申请号：US16624156

    申请日：2018-06-21

    申请人： BAYER CONSUMER CARE AG ,  BAYER PHARMA AKTIENGESELLSCHAFT

    发明人： Bernard HAENDLER

    IPC分类号： A61K31/5377 ,  A61K31/4155 ,  A61K31/4152 ,  A61K45/06

    摘要： The present invention relates to: * combinations of: * a component A: which is a PI3K kinase inhibitor, such as co-panlisib, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, in particular a physiologically acceptable salt, or a mixture of same, for example; * a component B: which is an androgen receptor antagonist, such as darolutamide or enzalutamide for example; and, optionally, * one or more pharmaceutical agents C; in which optionally either or both of said components A and B are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially; * use of such combinations: * in the treatment or prophylaxis of a cancer, particularly prostate cancer, or * for the preparation of a medicament for the treatment or prophylaxis of a cancer, particularly prostate cancer; * methods of treatment or prophylaxis of a cancer, particularly prostate cancer, in a subject, comprising administering to said subject a therapeutically effective amount of such a combination; * compositions containing such a combination, together with pharmaceutically acceptable ingredients; and * kits comprising such a combination.