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    N6 heterocyclic 8-modified adenosine derivatives
    5.
    发明授权
    N6 heterocyclic 8-modified adenosine derivatives 有权
    N6杂环8修饰腺苷衍生物

    公开(公告)号：US06294522B1

    公开(公告)日：2001-09-25

    申请号：US09454485

    申请日：1999-12-03

    申请人： Jeff A. Zablocki ,  Venkata P. Palle ,  Prabha N. Ibrahim ,  Luiz Belardenelli

    发明人： Jeff A. Zablocki ,  Venkata P. Palle ,  Prabha N. Ibrahim ,  Luiz Belardenelli

    IPC分类号： A61K3170

    CPC分类号： C07H19/16

    摘要： N6 heterocyclic 8 modified adenosine derivatives that are selective, partial or full adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity, modifying adipocyte function, treating central nervous system disorders, and treating diabetic disorders and obesity in mammals, and especially in humans.

    摘要翻译： 作为选择性，部分或全部腺苷A1受体部分或全部激动剂的N6杂环8修饰的腺苷衍生物，因此可用于改善心脏活动，修饰脂肪细胞功能，治疗中枢神经系统疾病，以及治疗哺乳动物的糖尿病病症和肥胖症 ，特别是在人类。

    Pyrrolo[2,3-]pyridine kinase inhibitors
    9.
    发明授权
    Pyrrolo[2,3-]pyridine kinase inhibitors 有权
    吡咯并[2,3]吡啶激酶抑制剂

    公开(公告)号：US08901301B2

    公开(公告)日：2014-12-02

    申请号：US12721496

    申请日：2010-03-10

    申请人： Prabha N. Ibrahim ,  Wayne Spevak ,  Hanna Cho ,  Hongyao Zhu

    发明人： Prabha N. Ibrahim ,  Wayne Spevak ,  Hanna Cho ,  Hongyao Zhu

    IPC分类号： C07D417/04 ,  A61K31/437 ,  C07D471/04

    CPC分类号： C07D471/04 ,  A61K31/437

    摘要： Propane-1-sulfonic acid {2,4-difluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phenyl]-amide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-2,5-difluoro-benzenesulfonamide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-3-fluoro-benzenesulfonamide, pyrrolidine-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, N,N-dimethylamino-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including melanoma, glioma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, and biliary tract cancer.

    摘要翻译： 丙烷-1-磺酸{2,4-二氟-3- [5-（2-甲氧基 - 嘧啶-5-基）-1H-吡咯并[2,3-b]吡啶-3-羰基] - 苯基} 酰胺，丙烷-1-磺酸[3-（5-氰基-1H-吡咯并[2,3-b]吡啶-3-羰基）-2,4-二氟 - 苯基] - 酰胺，丙烷-1-磺酸 [3-（5-氰基-1H-吡咯并[2,3-b]吡啶-3-羰基）-2-氟 - 苯基] - 酰胺，N- [3-（5-氰基-1H-吡咯并[ 3-b]吡啶-3-羰基）-2,4-二氟 - 苯基] -2,5-二氟 - 苯磺酰胺，N- [3-（5-氰基-1H-吡咯并[2,3-b] 吡咯-3-羰基）-2,4-二氟 - 苯基] -3-氟 - 苯磺酰胺，吡咯烷-1-磺酸[3-（5-氰基-1H-吡咯并[2,3-b]吡啶-3-羰基） -2,4-二氟 - 苯基] - 酰胺，N，N-二甲基氨基磺酸[3-（5-氰基-1H-吡咯并[2,3-b]吡啶-3-羰基）-2,4-二氟 - 苯基] - 酰胺及其盐，其制剂，其缀合物，其衍生物，其形式及其用途。 在某些方面和实施方案中，所述的化合物或其盐，其制剂，其缀合物，其衍生物及其形式在至少一种Raf蛋白激酶上具有活性。 还描述了其用于治疗疾病和病症的方法，包括与Raf蛋白激酶（包括黑素瘤，神经胶质瘤，结肠直肠癌，甲状腺癌，肺癌，卵巢癌，前列腺癌和胆道癌）的活性相关的疾病和病症。

    Compounds and methods for kinase modulation, and indications therefor
    10.
    发明授权
    Compounds and methods for kinase modulation, and indications therefor 有权
    用于激酶调节的化合物和方法及其适应症

    公开(公告)号：US08673928B2

    公开(公告)日：2014-03-18

    申请号：US12949741

    申请日：2010-11-18

    申请人： Prabha N. Ibrahim ,  Wayne Spevak ,  Hanna Cho ,  Songyuan Shi ,  Chao Zhang ,  Ying Zhang

    发明人： Prabha N. Ibrahim ,  Wayne Spevak ,  Hanna Cho ,  Songyuan Shi ,  Chao Zhang ,  Ying Zhang

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  A61P25/16 ,  A61P35/00 ,  A61P37/06 ,  A61P31/18

    CPC分类号： C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5377 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04

    摘要： and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds of Formula (I) or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease.

    摘要翻译： 及其盐，其制剂，其缀合物，其衍生物，其形式及用途。 在某些方面和实施方案中，所述式（I）化合物或其盐，其制剂，其缀合物，其衍生物，其形式在至少一种Raf蛋白激酶上具有活性。 在某些方面和实施方案中，所述化合物在抑制Ras突变细胞系的增殖中是有活性的。 还描述了其用于治疗疾病和病症的方法，包括与B-Raf V600E突变蛋白激酶（包括黑素瘤，神经胶质瘤，多形性成胶质细胞瘤，纤维细胞性星形细胞瘤，结肠直肠癌，甲状腺癌，肺癌，卵巢）的活动相关的疾病和病症 癌症，前列腺癌，肝癌，胆囊癌，胃肠道间质瘤，胆道癌和胆管癌。 还描述了其用于治疗疾病和病症的方法，包括与c-Raf-1蛋白激酶的活性相关的疾病和病症，包括急性疼痛，慢性疼痛或多囊肾病。