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17 条记录 (耗时 0.03 秒)

    NOVEL SOFT PDE4 INHIBITORS
    1.
    发明申请
    NOVEL SOFT PDE4 INHIBITORS 有权
    新型软PDE4抑制剂

    公开(公告)号：US20140187555A1

    公开(公告)日：2014-07-03

    申请号：US14237381

    申请日：2012-08-09

    申请人： Dirk Leysen ,  Olivier Defert ,  Sandro Boland

    发明人： Dirk Leysen ,  Olivier Defert ,  Sandro Boland

    IPC分类号： C07D213/04 ,  C07D405/12

    CPC分类号： C07D213/04 ,  C07D213/75 ,  C07D401/12 ,  C07D405/12

    摘要： The present invention relates to new phosphodiesterase inhibitors, more specifically soft PDE4 inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new soft PDE4 inhibitors compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including inflammatory diseases.

    摘要翻译： 本发明涉及新的磷酸二酯酶抑制剂，更具体地说是软的PDE4抑制剂，包含这种抑制剂的组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 特别地，本发明涉及包含这种抑制剂的新的软的PDE4抑制剂组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括炎性疾病）的药物中的方法。

    NOVEL ROCK KINASE INHIBITORS
    2.
    发明申请
    NOVEL ROCK KINASE INHIBITORS 有权
    新型摇滚激酶抑制剂

    公开(公告)号：US20140228408A1

    公开(公告)日：2014-08-14

    申请号：US14241092

    申请日：2012-08-31

    申请人： Jo Alen ,  Sandro Boland ,  Arnaud Pierre, Jean Bourin ,  Olivier Defert ,  Dirk Leysen

    发明人： Jo Alen ,  Sandro Boland ,  Arnaud Pierre, Jean Bourin ,  Olivier Defert ,  Dirk Leysen

    IPC分类号： C07D213/75 ,  C07D405/12 ,  C07D401/12

    CPC分类号： C07D213/74 ,  A61K31/44 ,  A61K31/443 ,  C07D213/75 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and respiratory diseases.

    摘要翻译： 本发明涉及新的激酶抑制剂，更具体地涉及包含这种抑制剂的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 特别地，本发明涉及包含这种抑制剂的新的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括性功能障碍，炎性疾病，眼科疾病和呼吸系统疾病）的药物中的方法。

    NOVEL ROCK INHIBTORS
    4.
    发明申请
    NOVEL ROCK INHIBTORS 有权
    新的岩石抑制剂

    公开(公告)号：US20150299173A1

    公开(公告)日：2015-10-22

    申请号：US14437919

    申请日：2013-10-31

    申请人： Amakem NV

    发明人： Arnaud Pierre, Jean Bourin ,  Dirk Leysen ,  Oilvier Defert ,  Sandro Boland

    IPC分类号： C07D405/14 ,  C07D217/04 ,  C07D405/12 ,  C07D401/12

    CPC分类号： C07D405/14 ,  C07D217/04 ,  C07D401/12 ,  C07D405/12

    摘要： The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors.

    摘要翻译： 本发明涉及新的激酶抑制剂，更具体地涉及包含这种抑制剂的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 特别地，本发明涉及包含这种抑制剂的新的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括性功能障碍，炎性疾病，眼科疾病和呼吸系统疾病）的药物中的方法。 本发明的化合物显示软的药物特征，即它们在进入体循环时迅速失活。 因此，它们允许减少全身暴露于功能活性的ROCK抑制剂。

    Rock inhibitors
    7.
    发明授权
    Rock inhibitors 有权
    岩石抑制剂

    公开(公告)号：US08912209B2

    公开(公告)日：2014-12-16

    申请号：US13897524

    申请日：2013-05-20

    申请人： Amakem NV

    发明人： Dirk Leysen ,  Oliver Defert ,  Nadzeya Kaval ,  Petra Blom ,  Sandro Boland

    IPC分类号： A01N43/40 ,  A61K31/435 ,  A61K31/44 ,  A01N43/42 ,  C07D401/12 ,  C07D239/42 ,  C07D213/75 ,  C07D471/04 ,  C07D409/12 ,  C07D405/12 ,  C07D493/04

    CPC分类号： C07D213/75 ,  C07D239/42 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D493/04

    摘要： The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

    摘要翻译： 本发明涉及新的激酶抑制剂，更具体地涉及包含这种抑制剂的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 特别地，本发明涉及包含这种抑制剂的新的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括性功能障碍，炎性疾病，眼科疾病和呼吸系统疾病）的药物中的方法。

    Rock inhibitors
    8.
    发明授权
    Rock inhibitors 有权
    岩石抑制剂

    公开(公告)号：US09394286B2

    公开(公告)日：2016-07-19

    申请号：US14437919

    申请日：2013-10-31

    申请人： Amakem NV

    发明人： Arnaud Pierre Jean Bourin ,  Dirk Leysen ,  Olivier Defert ,  Sandro Boland

    IPC分类号： C07D401/12 ,  C07D405/14 ,  A61K31/4725 ,  A61K31/454 ,  C07D217/04 ,  C07D405/12

    CPC分类号： C07D405/14 ,  C07D217/04 ,  C07D401/12 ,  C07D405/12

    摘要： The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors.

    摘要翻译： 本发明涉及新的激酶抑制剂，更具体地涉及包含这种抑制剂的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 特别地，本发明涉及包含这种抑制剂的新的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括性功能障碍，炎性疾病，眼科疾病和呼吸系统疾病）的药物中的方法。 本发明的化合物显示软的药物特征，即它们在进入体循环时迅速失活。 因此，它们允许减少全身暴露于功能活性的ROCK抑制剂。

    Rock inhibitors
    9.
    发明授权
    Rock inhibitors 有权
    岩石抑制剂

    公开(公告)号：US09073905B2

    公开(公告)日：2015-07-07

    申请号：US14113941

    申请日：2012-04-27

    申请人： Dirk Leysen ,  Olivier Defert ,  Sandro Boland ,  Jo Alen ,  Arnaud Pierre Jean Bourin

    发明人： Dirk Leysen ,  Olivier Defert ,  Sandro Boland ,  Jo Alen ,  Arnaud Pierre Jean Bourin

    IPC分类号： C07D409/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D451/04 ,  A61K31/4725 ,  A61K31/439 ,  A61K31/4468

    CPC分类号： C07D409/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D451/04

    摘要： The present invention relates to new kinase inhibitors of Formula (I), wherein X is oxygen, —NH—, or a direct bond; Y is —NH— or a direct bond; n is an integer from 0 to 4; m is an integer from 0 to 4; Cy represents a bivalent radical consisting of a satured (poly)cycle, including fused, bi-, spiro or bridged carbocycles and heterocycles; in particular selected from the group consisting of: Formula (II), Ar is selected from the group comprising: Formula (III), R2 is hydrogen or methyl; R8 is hydrogen, methyl, halogen, or alkynyl; R1 is an aryl or heteroaryl more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

    摘要翻译： 本发明涉及式（I）的新的激酶抑制剂，其中X是氧，-NH-或直接键; Y是-NH-或直接键; n为0〜4的整数; m为0〜4的整数; Cy表示由包括稠合，双，螺或桥连的碳环和杂环的一个（多）周期组成的二价基团; 特别是选自由式（II）组成的组，Ar选自：式（III），R 2是氢或甲基; R8是氢，甲基，卤素或炔基; R1是芳基或杂芳基更具体地是ROCK抑制剂，组合物，特别是药物，包含这种抑制剂，以及这些抑制剂在治疗和预防疾病中的用途。 特别地，本发明涉及包含这种抑制剂的新的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括性功能障碍，炎性疾病，眼科疾病和呼吸系统疾病）的药物中的方法。

    BIPHENYLCARBOXAMIDES AS ROCK KINASE INHIBITORS
    10.
    发明申请
    BIPHENYLCARBOXAMIDES AS ROCK KINASE INHIBITORS 有权
    作为岩石激酶抑制剂的双嘧达莫

    公开(公告)号：US20140371268A1

    公开(公告)日：2014-12-18

    申请号：US14241093

    申请日：2012-08-31

    申请人： Jo Alen ,  Sandro Boland ,  Arnaud Pierre Jean Bourin ,  Olivier Defert ,  Dirk Leysen

    发明人： Jo Alen ,  Sandro Boland ,  Arnaud Pierre Jean Bourin ,  Olivier Defert ,  Dirk Leysen

    IPC分类号： C07D213/74 ,  C07D401/12 ,  C07D409/12 ,  C07D405/12

    CPC分类号： C07D213/74 ,  A61K31/44 ,  A61K31/443 ,  C07D213/75 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases, gastrointestinal diseases and respiratory diseases.

    摘要翻译： 本发明涉及新的激酶抑制剂，更具体地涉及包含这种抑制剂的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 特别地，本发明涉及包含这种抑制剂的新的ROCK抑制剂，组合物，特别是药物，以及这些抑制剂在治疗和预防疾病中的用途。 此外，本发明涉及治疗和使用所述化合物在制备用于应用于许多治疗适应症（包括性功能障碍，炎性疾病，眼科疾病，胃肠道疾病和呼吸系统疾病）的药物中的方法。