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    SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
    1.
    发明申请
    SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
    取代5-（吡嗪-2-基）-1H-吡唑并[3,4-B]吡啶和吡唑并[3,4-B]吡啶衍生物作为蛋白激酶抑制剂

    公开(公告)号：US20140309211A1

    公开(公告)日：2014-10-16

    申请号：US14290125

    申请日：2014-05-29

    申请人： Hariprasad Vankayalapati ,  Rajendra P. Appalaneni ,  Y. Venkata Krishna Reddy

    发明人： Hariprasad Vankayalapati ,  Rajendra P. Appalaneni ,  Y. Venkata Krishna Reddy

    IPC分类号： C07D471/04

    CPC分类号： A61K31/497 ,  A61K31/5377 ,  C07C249/00 ,  C07D471/04

    摘要： Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.

    摘要翻译： 取代5-（吡嗪-2-基）-1H-吡唑并[3,4-b]吡啶，5-（吡嗪-2-基）-1H-吡咯并[2,3-b]吡啶和吡唑并[3,4 -b]吡啶衍生物及其制备方法，其为组成型激活酪氨酸激酶（TKL），CMGC蛋白激酶家族成员的抑制剂，可用于治疗帕金森病， 阿尔茨海默病，唐氏综合症，亨廷顿病，其他神经变性和中枢神经系统疾病，癌症，代谢紊乱和炎性疾病。 还公开了包括这些化合物的化合物和抑制这些家族的野生型和/或突变的蛋白激酶活性的方法的药物组合物，以及使用包括该化合物的化合物和药物组合物治疗与其相关的病症。

    Continuous production of azines/hydrazine hydrate
    2.
    发明授权
    Continuous production of azines/hydrazine hydrate 失效
    连续生产吖嗪/水合肼

    公开(公告)号：US06605265B1

    公开(公告)日：2003-08-12

    申请号：US08217752

    申请日：1994-03-25

    申请人： Jean-Pierre Schirmann ,  Jean-Pierre Pleuvry ,  Pierre Tellier

    发明人： Jean-Pierre Schirmann ,  Jean-Pierre Pleuvry ,  Pierre Tellier

    IPC分类号： C01B2116

    CPC分类号： C01B21/16 ,  C07C249/00 ,  C07C251/88 ,  Y02P20/582

    摘要： Azines, e.g., ketazines, are continuously produced by (i) establishing a loop having an azine reaction medium circulating therein, such loop including an azine reaction zone, means for separating azine final product from the circulating reaction medium, means for heating the reaction medium and for purging water therefrom, and means for recycling heated and purged reaction medium to the azine reaction zone, (ii) introducing hydrogen peroxide, ammonia and a carbonyl compound into the circulating reaction medium in the azine reaction zone, (iii) withdrawing azine final product thus formed from the circulating reaction medium. downstream of the azine reaction zone, (iii) thereafter purging water from the circulating reaction medium to maintain the volume thereof essentially constant, (iv) heating the circulating reaction medium to a temperature of at least 130° C., (v) recycling thus heated reaction medium to the azine reaction zone, and (vi), at any point along the loop, introducing a reagent into the circulating reaction medium as to essentially maintain the equilibrium of the azine-forming reaction; the final product azines are conveniently hydrolyzed into hydrazine hydrate.

    摘要翻译： 通过（i）建立其中循环其中的吖嗪反应介质的环，包括吖嗪反应区的环路，用于从循环反应介质中分离吖嗪最终产物的装置，连续制备氮杂环丁烷，例如加入反应介质 和用于从其中清洗水的装置，以及用于将加热和净化的反应介质再循环到吖嗪反应区的装置，（ii）在吖嗪反应区中将过氧化氢，氨和羰基化合物引入循环反应介质中，（iii） 由循环反应介质形成的产物。 （iii）然后从循环反应介质中清洗水以使其体积保持基本恒定，（iv）将循环反应介质加热到至少130℃的温度，（v）由此回收 加热的反应介质到吖嗪反应区，和（vi）在沿着环的任何点，将试剂引入循环反应介质中，从而基本维持吖嗪形成反应的平衡; 最终产物吖嗪方便地水解成水合肼。

    SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
    4.
    发明申请
    SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
    取代5-（吡嗪-2-基）-1H-吡唑并[3,4-B]吡啶和吡唑并[3,4-B]吡啶衍生物作为蛋白激酶抑制剂

    公开(公告)号：US20130102586A1

    公开(公告)日：2013-04-25

    申请号：US13435327

    申请日：2012-03-30

    申请人： Hariprasad Vankayalapati ,  Rajendra P. Appalaneni ,  Y. Venkata Krishna Reddy

    发明人： Hariprasad Vankayalapati ,  Rajendra P. Appalaneni ,  Y. Venkata Krishna Reddy

    IPC分类号： C07D471/04

    CPC分类号： A61K31/497 ,  A61K31/5377 ,  C07C249/00 ,  C07D471/04

    摘要： Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.

    摘要翻译： 取代5-（吡嗪-2-基）-1H-吡唑并[3,4-b]吡啶，5-（吡嗪-2-基）-1H-吡咯并[2,3-b]吡啶和吡唑并[3,4 -b]吡啶衍生物及其制备方法，其为组成型激活酪氨酸激酶（TKL），CMGC蛋白激酶家族成员的抑制剂，可用于治疗帕金森病， 阿尔茨海默病，唐氏综合症，亨廷顿病，其他神经变性和中枢神经系统疾病，癌症，代谢紊乱和炎性疾病。 还公开了包括这些化合物的化合物和抑制这些家族的野生型和/或突变的蛋白激酶活性的方法的药物组合物，以及使用包括该化合物的化合物和药物组合物治疗与其相关的病症。

    SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
    5.
    发明申请
    SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
    取代5-（吡嗪-2-基）-1H-吡唑并[3,4-B]吡啶和吡唑并[3,4-B]吡啶衍生物作为蛋白激酶抑制剂

    公开(公告)号：US20160074395A1

    公开(公告)日：2016-03-17

    申请号：US14871285

    申请日：2015-09-30

    申请人： Arrien Pharmaceuticals LLC

    发明人： Hariprasad Vankayalapati ,  Rajendra P. Appalaneni ,  Y. Venkata Krishna Reddy

    IPC分类号： A61K31/497 ,  A61K31/5377

    CPC分类号： A61K31/497 ,  A61K31/5377 ,  C07C249/00 ,  C07D471/04

    摘要： Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3, 4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.

    摘要翻译： 取代5-（吡嗪-2-基）-1H-吡唑并[3,4-b]吡啶，5-（吡嗪-2-基）-1H-吡咯并[2,3-b]吡啶和吡唑并[3,4 -b]吡啶衍生物及其制备方法，其为组成型激活酪氨酸激酶（TKL），CMGC蛋白激酶家族成员的抑制剂，可用于治疗帕金森病， 阿尔茨海默病，唐氏综合症，亨廷顿病，其他神经变性和中枢神经系统疾病，癌症，代谢紊乱和炎性疾病。 还公开了包括这些化合物的化合物和抑制这些家族的野生型和/或突变的蛋白激酶活性的方法的药物组合物，以及使用包括该化合物的化合物和药物组合物治疗与其相关的病症。

    Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
    6.
    发明授权
    Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors 有权
    取代5-（吡嗪-2-基）-1H-吡唑并[3,4-b]吡啶和吡唑并[3,4-b]吡啶衍生物作为蛋白激酶抑制剂

    公开(公告)号：US09187473B2

    公开(公告)日：2015-11-17

    申请号：US14290125

    申请日：2014-05-29

    申请人： Arrien Pharmaceuticals LLC

    发明人： Hariprasad Vankayalapati ,  Rajendra P. Appalaneni ,  Y. Venkata Krishna Reddy

    IPC分类号： C07D401/14 ,  A61K31/437 ,  C07D471/04

    CPC分类号： A61K31/497 ,  A61K31/5377 ,  C07C249/00 ,  C07D471/04

    摘要： Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.

    摘要翻译： 取代5-（吡嗪-2-基）-1H-吡唑并[3,4-b]吡啶，5-（吡嗪-2-基）-1H-吡咯并[2,3-b]吡啶和吡唑并[3,4 -b]吡啶衍生物及其制备方法，其为组成型激活酪氨酸激酶（TKL），CMGC蛋白激酶家族成员的抑制剂，可用于治疗帕金森病， 阿尔茨海默病，唐氏综合症，亨廷顿病，其他神经变性和中枢神经系统疾病，癌症，代谢紊乱和炎性疾病。 还公开了包括这些化合物的化合物和抑制这些家族的野生型和/或突变的蛋白激酶活性的方法的药物组合物，以及使用包括该化合物的化合物和药物组合物治疗与其相关的病症。