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    Crystal of fused pyridine compound salt
    2.
    发明授权
    Crystal of fused pyridine compound salt 有权
    稠合吡啶化合物的晶体

    公开(公告)号：US08779140B2

    公开(公告)日：2014-07-15

    申请号：US13806909

    申请日：2011-06-22

    申请人： Takashi Kikuchi ,  Katsuhiko Gato ,  Koichiro Mukoyoshi ,  Tsuyoshi Kitamura ,  Takeshi Kawakami ,  Hironobu Yasuda

    发明人： Takashi Kikuchi ,  Katsuhiko Gato ,  Koichiro Mukoyoshi ,  Tsuyoshi Kitamura ,  Takeshi Kawakami ,  Hironobu Yasuda

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04 ,  A61K31/437

    摘要： [Problem]A salt or crystal of a compound which is highly stable in a solid state and useful as a bulk material for the preparation of a pharmaceutical product is provided.[Means for Solution]4-{[(1R,2s,3S,5s,7s)-5-Hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide succinate, 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrobromide, and 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride and crystals thereof are useful as a bulk material for the preparation of a solid preparation, in particular, a solid dispersion preparation. Furthermore, the crystal of the hydrobromide has excellent stability in a solid state and is useful as a bulk material for the preparation of a pharmaceutical product.

    摘要翻译： [问题]提供了一种固体高度稳定并可用作制备药物的散装材料的化合物的盐或晶体。 [溶液的方法] 4 - {[（1R，2s，3S，5s，7s）-5-羟基-2-金刚烷基]氨基} -1H-吡咯并[2,3-b]吡啶-5-甲酰胺琥珀酸酯，4 - {[（1R，2s，3S，5s，7s）-5-羟基-2-金刚烷基]氨基} -1H-吡咯并[2,3-b]吡啶-5-甲酰胺氢溴酸盐和4 - {[ ，2s，3S，5s，7s）-5-羟基-2-金刚烷基]氨基} -1H-吡咯并[2,3-b]吡啶-5-甲酰胺盐酸盐及其晶体可用作制备 固体制剂，特别是固体分散体制剂。 此外，氢溴酸盐的结晶在固体状态下具有优异的稳定性，并且可用作制备药物的主体材料。

    CRYSTAL OF FUSED PYRIDINE COMPOUND SALT
    3.
    发明申请
    CRYSTAL OF FUSED PYRIDINE COMPOUND SALT 有权
    熔融吡啶化合物盐的晶体

    公开(公告)号：US20130102628A1

    公开(公告)日：2013-04-25

    申请号：US13806909

    申请日：2011-06-22

    申请人： Takashi Kikuchi ,  Katsuhiko Gato ,  Koichiro Mukoyoshi ,  Tsuyoshi Kitamura ,  Takeshi Kawakami ,  Hironobu Yasuda

    发明人： Takashi Kikuchi ,  Katsuhiko Gato ,  Koichiro Mukoyoshi ,  Tsuyoshi Kitamura ,  Takeshi Kawakami ,  Hironobu Yasuda

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04 ,  A61K31/437

    摘要： [Problem] A salt or crystal of a compound which is highly stable in a solid state and useful as a bulk material for the preparation of a pharmaceutical product is provided.[Means for Solution] 4-{[(1R,2s,3S,5s,7s)-5-Hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide succinate, 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrobromide, and 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride and crystals thereof are useful as a bulk material for the preparation of a solid preparation, in particular, a solid dispersion preparation. Furthermore, the crystal of the hydrobromide has excellent stability in a solid state and is useful as a bulk material for the preparation of a pharmaceutical product.

    摘要翻译： [问题]提供了一种固体高度稳定并可用作制备药物的散装材料的化合物的盐或晶体。 [溶液的方法] 4 - {[（1R，2s，3S，5s，7s）-5-羟基-2-金刚烷基]氨基} -1H-吡咯并[2,3-b]吡啶-5-甲酰胺琥珀酸酯，4 - {[（1R，2s，3S，5s，7s）-5-羟基-2-金刚烷基]氨基} -1H-吡咯并[2,3-b]吡啶-5-甲酰胺氢溴酸盐和4 - {[ ，2s，3S，5s，7s）-5-羟基-2-金刚烷基]氨基} -1H-吡咯并[2,3-b]吡啶-5-甲酰胺盐酸盐及其晶体可用作制备 固体制剂，特别是固体分散体制剂。 此外，氢溴酸盐的结晶在固体状态下具有优异的稳定性，并且可用作制备药物的主体材料。

    2,4-DIAMINOPYRIMIDINE COMPOUND
    5.
    发明申请
    2,4-DIAMINOPYRIMIDINE COMPOUND 审中-公开
    2,4-二氨基吡啶化合物

    公开(公告)号：US20110159019A1

    公开(公告)日：2011-06-30

    申请号：US13061311

    申请日：2009-08-31

    申请人： Akira Tanaka ,  Koichiro Mukoyoshi ,  Shigeki Kunikawa ,  Yuji Takasuna ,  Jun Maeda ,  Noboru Chida ,  Shinya Nagashima

    发明人： Akira Tanaka ,  Koichiro Mukoyoshi ,  Shigeki Kunikawa ,  Yuji Takasuna ,  Jun Maeda ,  Noboru Chida ,  Shinya Nagashima

    IPC分类号： A61K31/551 ,  C07D403/12 ,  C07D401/12 ,  C07D239/48 ,  C07D413/12 ,  C07D405/12 ,  C07D409/12 ,  C07D405/14 ,  C07D413/14 ,  A61K31/506 ,  A61K31/505 ,  A61K31/5377 ,  A61P37/06

    CPC分类号： C07D239/48

    摘要： Provided is a compound which is useful as an active ingredient for a pharmaceutical having a PKCθ inhibition activity, particularly a pharmaceutical composition for inhibiting acute rejection occurring in transplantation. The present inventors have conducted extensive studies on a compound having a PKCθ inhibition activity, and as a result, they have found that a compound having a structure such as aralkyl and the like on an amino group at the 2-position and also having a structure such as an adamantylalkyl group and the like on an amino group at the 4-position of 2,4-diaminopyrimidine, or a salt thereof has an excellent PKCθ inhibition activity, thereby completing the present invention. The 2,4-diaminopyrimidine compound of the present invention can be used as a PKCθ inhibitor or an inhibitor of acute rejection occurring in transplantation.

    摘要翻译： 提供可用作具有PKC和药物的药物的活性成分的化合物; 特别是用于抑制移植中发生急性排斥反应的药物组合物。 本发明人对具有PKC的化合物进行了广泛的研究; 抑制活性，结果发现，在2-位的氨基上具有芳烷基等结构的化合物，还具有金刚烷基烷基等的结构，氨基上的氨基上 2,4-二氨基嘧啶的4位或其盐具有优异的PKC和重量; 从而完成了本发明。 本发明的2,4-二氨基嘧啶化合物可以用作PKC＆amp; 抑制剂或移植中发生的急性排斥抑制剂。