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31 条记录 (耗时 0.032 秒)

    Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and CNS disorders
    1.
    发明授权
    Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and CNS disorders 有权
    用于治疗癌症，自身免疫性炎症和中枢神经系统疾病的二氟二恶烷 - 氨基 - 苯并咪唑激酶抑制剂

    公开(公告)号：US09580438B2

    公开(公告)日：2017-02-28

    申请号：US14411795

    申请日：2013-06-27

    申请人： 4SC DISCOVERY GMBH

    发明人： Johann Leban ,  Mirko Zaja

    IPC分类号： C07D491/056 ,  C07D519/00 ,  A61K31/4184 ,  A61K31/4188 ,  C07D491/02

    CPC分类号： C07D491/056 ,  C07D491/02 ,  C07D519/00

    摘要： The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof, wherein A, X, L, Y, R, and RN are as defined herein. The invention further relates to the use of the compounds of formula (I) as a medicament, a pharmaceutical composition comprising them, a method of treatment or prevention of a medical condition entailing the administration thereof, and the use thereof in the manufacture of a medicament for the treatment or prevention of a medical condition, particularly autoimmune inflammatory disorders, CNS disorders, sleeping disorders, or proliferative diseases including cancer. The invention further relates to a specific process for the preparation of said compounds.

    摘要翻译： 本发明涉及通式（I）的化合物或其生理功能衍生物，溶剂化物或盐，其中A，X，L，Y，R和RN如本文所定义。 本发明还涉及式（I）化合物作为药物，包含它们的药物组合物的用途，治疗或预防其施用的医学病症的方法及其在制备药物中的用途 用于治疗或预防医疗状况，特别是自身免疫性炎症性疾病，CNS障碍，睡眠障碍或包括癌症在内的增殖性疾病。 本发明还涉及制备所述化合物的具体方法。

    Imidazo[1,2-a]pyridine derivatives: preparation and pharmaceutical applications
    3.
    发明授权
    Imidazo[1,2-a]pyridine derivatives: preparation and pharmaceutical applications 有权
    咪唑并[1,2-a]吡啶衍生物：制备和药物应用

    公开(公告)号：US09266882B2

    公开(公告)日：2016-02-23

    申请号：US14517614

    申请日：2014-10-17

    申请人： MEI Pharma, Inc.

    发明人： Ken Chi Lik Lee ,  Eric T. Sun ,  Haishan Wang

    IPC分类号： A61K31/44 ,  C07D498/02 ,  C07D491/02 ,  C07D471/04

    CPC分类号： C07D471/04 ,  A61K31/44 ,  C07D491/02 ,  C07D498/02 ,  Y02A50/409 ,  Y02A50/411

    摘要： The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC).

    摘要翻译： 本发明涉及作为组蛋白脱乙酰酶抑制剂的异羟肟酸酯化合物。 更具体地，本发明涉及含咪唑并[1,2-a]吡啶的化合物及其制备方法。 这些化合物可用作治疗增殖性疾病的药物以及涉及与组蛋白脱乙酰酶活性（HDAC）的酶有关或与之有关的其它疾病。

    BIFLUORODIOXALANE-AMINO-BENZIMIDAZOLE KINASE INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNEINFLAMMATION AND CNS DISORDERS
    4.
    发明申请
    BIFLUORODIOXALANE-AMINO-BENZIMIDAZOLE KINASE INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNEINFLAMMATION AND CNS DISORDERS 有权
    用于治疗癌症，自身免疫性疾病和中枢神经系统疾病的双歧杆菌 - 氨基 - 苯并咪唑激酶抑制剂

    公开(公告)号：US20150158878A1

    公开(公告)日：2015-06-11

    申请号：US14411795

    申请日：2013-06-27

    申请人： 4SC DISCOVERY GMBH

    发明人： Johann Leban ,  Mirko Zaja

    IPC分类号： C07D491/056 ,  C07D519/00

    CPC分类号： C07D491/056 ,  C07D491/02 ,  C07D519/00

    摘要： The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof, wherein A, X, L, Y, R, and RN are as defined herein. The invention further relates to the use of the compounds of formula (I) as a medicament, a pharmaceutical composition comprising them, a method of treatment or prevention of a medical condition entailing the administration thereof, and the use thereof in the manufacture of a medicament for the treatment or prevention of a medical condition, particularly autoimmune inflammatory disorders, CNS disorders, sleeping disorders, or proliferative diseases including cancer. The invention further relates to a specific process for the preparation of said compounds.

    摘要翻译： 本发明涉及通式（I）的化合物或其生理功能衍生物，溶剂化物或盐，其中A，X，L，Y，R和RN如本文所定义。 本发明还涉及式（I）化合物作为药物，包含它们的药物组合物的用途，治疗或预防其施用的医学病症的方法及其在制备药物中的用途 用于治疗或预防医疗状况，特别是自身免疫性炎症性疾病，CNS障碍，睡眠障碍或包括癌症在内的增殖性疾病。 本发明还涉及制备所述化合物的具体方法。

    Furo[3. 2-B] pyrrol derivatives
    7.
    发明授权
    Furo[3. 2-B] pyrrol derivatives 有权
    Furo [3。 2-B]吡咯衍生物

    公开(公告)号：US08053437B2

    公开(公告)日：2011-11-08

    申请号：US12773524

    申请日：2010-05-04

    申请人： Martin Quibell ,  John Paul Watts

    发明人： Martin Quibell ,  John Paul Watts

    IPC分类号： A61K31/496 ,  A61K31/454

    CPC分类号： C07D491/02

    摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

    摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中：R3是叔丁基甲基，仲丁基或叔丁基; X是CH或N; 且R 4为任选取代的C 1-8烷基或任选取代的C 3-8环烷基。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及 基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

    Furo[3, 2-b] pyrrol derivatives
    8.
    发明授权
    Furo[3, 2-b] pyrrol derivatives 失效
    呋喃并[3,2-b]吡咯衍生物

    公开(公告)号：US07737150B2

    公开(公告)日：2010-06-15

    申请号：US12319557

    申请日：2009-01-08

    申请人： Martin Quibell ,  John Paul Watts

    发明人： Martin Quibell ,  John Paul Watts

    IPC分类号： A61K31/496 ,  A61K31/454 ,  C07D491/08 ,  C12Q1/37

    CPC分类号： C07D491/02

    摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.

    摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中：R3是叔丁基甲基，仲丁基或叔丁基; X是CH或N; 且R 4为任选取代的C 1-8烷基或任选取代的C 3-8环烷基。 本发明还涉及包含式（I）化合物的药物组合物，以及这些化合物在治疗选自骨质疏松症，佩吉特氏病，恰加斯病，疟疾，牙龈疾病，高钙血症，代谢性骨病，涉及 基质或软骨降解，以及骨癌症如骨转移和相关的疼痛。

    Imidazo[1,2-a]pyridine derivatives: preparation and pharmaceutical applications
    10.
    发明授权
    Imidazo[1,2-a]pyridine derivatives: preparation and pharmaceutical applications 有权
    咪唑并[1,2-a]吡啶衍生物：制备和药物应用

    公开(公告)号：US08901149B2

    公开(公告)日：2014-12-02

    申请号：US14147290

    申请日：2014-01-03

    申请人： MEI Pharma, Inc.

    发明人： Ken Chi Lik Lee ,  Eric T. Sun ,  Haishan Wang

    IPC分类号： C07D471/04 ,  A61K31/44 ,  C07D498/02 ,  C07D491/02

    CPC分类号： C07D471/04 ,  A61K31/44 ,  C07D491/02 ,  C07D498/02 ,  Y02A50/409 ,  Y02A50/411

    摘要： The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC).

    摘要翻译： 本发明涉及作为组蛋白脱乙酰酶抑制剂的异羟肟酸酯化合物。 更具体地，本发明涉及含咪唑并[1,2-a]吡啶的化合物及其制备方法。 这些化合物可用作治疗增殖性疾病的药物以及涉及与组蛋白脱乙酰酶活性（HDAC）的酶有关或与之有关的其它疾病。