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    Tyrosine kinase inhibitors
    3.
    发明授权
    Tyrosine kinase inhibitors 有权
    酪氨酸激酶抑制剂

    公开(公告)号：US07893081B2

    公开(公告)日：2011-02-22

    申请号：US12316868

    申请日：2008-12-17

    申请人： Paolo Avalle ,  Jennifer R. Foley ,  Peter Mullens ,  Yaling Wang ,  Peter Yehl

    发明人： Paolo Avalle ,  Jennifer R. Foley ,  Peter Mullens ,  Yaling Wang ,  Peter Yehl

    IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D221/00

    CPC分类号： C07D405/14

    摘要： This invention relates to salt forms of the compound N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N′-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide, an inhibitor of tyrosine kinases, in particular the receptor tyrosine kinase MET, that are useful in the treatment of cellular proliferative diseases, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. In particular, the invention relates to the sodium salt of N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N′-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide.

    摘要翻译： 本发明涉及化合物N - [（2R）-1,4-二恶烷-2-基甲基] -N-甲基-N' - [3-（1-甲基-1H-吡唑-4-基） -5-氧代-5H-苯并[4,5]环庚并[1,2-b]吡啶-7-基]磺酰胺，酪氨酸激酶抑制剂，特别是受体酪氨酸激酶MET，可用于治疗 细胞增殖性疾病，例如癌症，增生，再狭窄，心脏肥大，免疫疾病和炎症。 特别地，本发明涉及N - [（2R）-1,4-二恶烷-2-基甲基] -N-甲基-N' - [3-（1-甲基-1H-吡唑-4-基） 吡啶-7-基）-5-氧代-5H-苯并[4,5]环庚并[1,2-b]吡啶-7-基]磺酰胺。

    Pharmaceutically acceptable salts of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide
    4.
    发明授权
    Pharmaceutically acceptable salts of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide 有权
    2- {4 - [（3S） - 哌啶-3-基]苯基} -2H-吲唑-7-甲酰胺的药学上可接受的盐

    公开(公告)号：US08436185B2

    公开(公告)日：2013-05-07

    申请号：US12811922

    申请日：2009-01-08

    申请人： Jennifer R. Foley ,  Robert Darrin Wilson

    发明人： Jennifer R. Foley ,  Robert Darrin Wilson

    IPC分类号： C07D211/32 ,  A61K31/445

    CPC分类号： C07D401/10

    摘要： The present invention relates to pharmaceutically acceptable salts of an amide substituted indazole which are inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), previously known as poly(ADP-ribose)synthase and poly(ADP-ribosyl) transferase. The compounds of the present invention are useful as mono-therapies in tumors with specific defects in DNA-repair pathways and as enhancers of certain DNA-damaging agents such as anticancer agents and radiotherapy. Further, the compounds of the present invention are useful for reducing cell necrosis (in stroke and myocardial infarction), down regulating inflammation and tissue injury, treating retroviral infections and protecting against the toxicity of chemotherapy.

    摘要翻译： 本发明涉及酰胺取代的吲唑的药学上可接受的盐，其是聚（ADP-核糖）聚合酶（PARP）的酶的抑制剂，先前称为聚（ADP-核糖）合成酶和聚（ADP-核糖基）转移酶。 本发明的化合物可用作在DNA修复途径中具有特定缺陷的肿瘤中的单一疗法，并且可用作某些DNA损伤剂如抗癌剂和放射疗法的增强剂。 此外，本发明的化合物可用于减少细胞坏死（中风和心肌梗塞），下调调节炎症和组织损伤，治疗逆转录病毒感染并防止化疗的毒性。

    PHARMACEUTICALLY ACCEPTABLE SALTS OF 2--2H-INDAZOLE-7-CARBOXAMIDE
    5.
    发明申请
    PHARMACEUTICALLY ACCEPTABLE SALTS OF 2--2H-INDAZOLE-7-CARBOXAMIDE 有权
    2--2H-吲唑-7-羧酰胺的药学上可接受的盐

    公开(公告)号：US20100286203A1

    公开(公告)日：2010-11-11

    申请号：US12811922

    申请日：2009-01-08

    申请人： Jennifer R. Foley ,  Robert Darrin Wilson

    发明人： Jennifer R. Foley ,  Robert Darrin Wilson

    IPC分类号： A61K31/454 ,  C07D401/10 ,  A61P35/00 ,  A61P29/00 ,  A61P9/10 ,  A61P3/10 ,  A61P25/28 ,  A61P31/12

    CPC分类号： C07D401/10

    摘要： The present invention relates to pharmaceutically acceptable salts of an amide substituted indazole which are inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), previously known as poly(ADP-ribose)synthase and poly(ADP-ribosyl) transferase. The compounds of the present invention are useful as mono-therapies in tumors with specific defects in DNA-repair pathways and as enhancers of certain DNA-damaging agents such as anticancer agents and radiotherapy. Further, the compounds of the present invention are useful for reducing cell necrosis (in stroke and myocardial infarction), down regulating inflammation and tissue injury, treating retroviral infections and protecting against the toxicity of chemotherapy.

    摘要翻译： 本发明涉及酰胺取代的吲唑的药学上可接受的盐，其是聚（ADP-核糖）聚合酶（PARP）的酶的抑制剂，先前称为聚（ADP-核糖）合成酶和聚（ADP-核糖基）转移酶。 本发明的化合物可用作在DNA修复途径中具有特定缺陷的肿瘤中的单一疗法，并且可用作某些DNA损伤剂如抗癌剂和放射疗法的增强剂。 此外，本发明的化合物可用于减少细胞坏死（中风和心肌梗塞），下调调节炎症和组织损伤，治疗逆转录病毒感染并防止化疗的毒性。

    Tyrosine kinase inhibitors
    6.
    发明申请
    Tyrosine kinase inhibitors 有权
    酪氨酸激酶抑制剂

    公开(公告)号：US20090182002A1

    公开(公告)日：2009-07-16

    申请号：US12316868

    申请日：2008-12-17

    申请人： Paolo Avalle ,  Jennifer R. Foley ,  Peter Mullens ,  Yaling Wang ,  Peter Yehl

    发明人： Paolo Avalle ,  Jennifer R. Foley ,  Peter Mullens ,  Yaling Wang ,  Peter Yehl

    IPC分类号： A61K31/435 ,  C07D221/16 ,  A61P35/00

    CPC分类号： C07D405/14

    摘要： This invention relates to salt forms of the compound N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N′-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide, an inhibitor of tyrosine kinases, in particular the receptor tyrosine kinase MET, that are useful in the treatment of cellular proliferative diseases, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. in particular, the invention relates to the sodium salt of N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N′-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide.

    摘要翻译： 本发明涉及化合物N - [（2R）-1,4-二恶烷-2-基甲基] -N-甲基-N' - [3-（1-甲基-1H-吡唑-4-基） -5-氧代-5H-苯并[4,5]环庚并[1,2-b]吡啶-7-基]磺酰胺，酪氨酸激酶抑制剂，特别是受体酪氨酸激酶MET，可用于治疗 细胞增殖性疾病，例如癌症，增生，再狭窄，心脏肥大，免疫疾病和炎症。 特别是本发明涉及N - [（2R）-1,4-二恶烷-2-基甲基] -N-甲基-N' - [3-（1-甲基-1H-吡唑-4-基） 吡啶-7-基）-5-氧代-5H-苯并[4,5]环庚并[1,2-b]吡啶-7-基]磺酰胺。