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    Tricyclic pteridinones and a process for their preparation
    1.
    发明授权
    Tricyclic pteridinones and a process for their preparation 失效
    三环蝶啶酮及其制备方法

    公开(公告)号：US6025489A

    公开(公告)日：2000-02-15

    申请号：US216552

    申请日：1998-12-18

    申请人： David D. Davey ,  John W. Lampe

    发明人： David D. Davey ,  John W. Lampe

    IPC分类号： C07D487/14 ,  C07D417/00

    CPC分类号： C07D487/14

    摘要： This invention is directed to tricyclic pteridinones of formula (I): ##STR1## where R, R.sup.1, A, B and D are described herein. These compounds and their pharmaceutically acceptable salts are disclosed as being combined inotropic and vasodilator agents.

    摘要翻译： 本发明涉及式（I）的三环蝶啶酮：其中R，R 1，A，B和D如本文所述。 这些化合物及其药学上可接受的盐被公开为组合的肌力和血管舒张剂。

    METHOD FOR TREATING PULMONARY DISEASES USING RHO KINASE INHIBITOR COMPOUNDS
    7.
    发明申请
    METHOD FOR TREATING PULMONARY DISEASES USING RHO KINASE INHIBITOR COMPOUNDS 失效
    使用RHO激酶抑制剂化合物治疗肺部疾病的方法

    公开(公告)号：US20090325958A1

    公开(公告)日：2009-12-31

    申请号：US12492494

    申请日：2009-06-26

    申请人： Tomas Navratil ,  Ward M. Peterson ,  John W. Lampe ,  Emilee H. Fulcher ,  Scott D. Sorensen

    发明人： Tomas Navratil ,  Ward M. Peterson ,  John W. Lampe ,  Emilee H. Fulcher ,  Scott D. Sorensen

    IPC分类号： A61K31/5377 ,  A61K31/454 ,  A61K31/416 ,  A61K31/496 ,  A61K31/4725 ,  A61P11/00

    CPC分类号： A61K31/4545 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12

    摘要： This invention is directed to methods of preventing or treating diseases or conditions of the lungs associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema. Particularly, this invention is directed to methods of treating pulmonary diseases such as asthma; chronic obstructive pulmonary disease; respiratory tract illness caused by respiratory syncytial virus; pulmonary arterial hypertension; acute respiratory distress syndrome and ventilator induced lung injury; cystic fibrosis; bronchiectasis; alpha-1-antitrypsin deficiency; rhinitis; rhinosinusitis; primary ciliary dyskinesia; pneumonia; bronchiolitis caused by agents other than respiratory syncytial virus; and interstitial lung disease including lymphangioleiomyomatosis; idiopathic pulmonary fibrosis; obliterative bronchiolitis or bronchiolitis obliterans organizing pneumonia due to lung transplantation or HSCT; nonspecific interstitial pneumonia; cryptogenic organizing pneumonia; acute interstitial pneumonia; respiratory bronchiolitis-associated interstitial lung disease; or pulmonary sarcoidosis. The method comprises administering to a subject an effective amount of a rho kinase inhibitor compound to treat the disease.

    摘要翻译： 本发明涉及预防或治疗与过度细胞增殖，重塑，炎症，血管收缩，支气管收缩，气道高反应性和水肿相关的肺的疾病或病症的方法。 特别地，本发明涉及治疗肺部疾病如哮喘的方法; 慢性阻塞性肺疾病; 呼吸道合胞病毒引起的呼吸道疾病; 肺动脉高压; 急性呼吸窘迫综合征和呼吸机诱发肺损伤; 囊性纤维化; 支气管扩张 α-1-抗胰蛋白酶缺乏症; 鼻炎; 鼻鼻窦炎 原发性纤毛运动障碍; 肺炎; 由呼吸道合胞病毒以外的药剂引起的细支气管炎; 间质性肺病包括淋巴管平滑肌瘤病; 特发性肺纤维化; 闭塞性细支气管炎或闭塞性细支气管炎由于肺移植或HSCT而组织肺炎; 非特异性间质性肺炎 隐源性机体性肺炎 急性间质性肺炎 呼吸性细支气管炎相关性间质性肺病; 或肺结节病。 该方法包括向受试者施用有效量的rho激酶抑制剂化合物以治疗该疾病。

    Bridged bicyclic RHO kinase inhibitor compounds, composition and use
    9.
    发明授权
    Bridged bicyclic RHO kinase inhibitor compounds, composition and use 有权
    桥联双环RHO激酶抑制剂化合物，组成和用途

    公开(公告)号：US08476295B2

    公开(公告)日：2013-07-02

    申请号：US12965615

    申请日：2010-12-10

    申请人： John W. Lampe ,  Paul S. Watson ,  David J. Slade

    发明人： John W. Lampe ,  Paul S. Watson ,  David J. Slade

    IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00

    CPC分类号： C07D451/04 ,  A61K31/46 ,  A61K31/4725 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08

    摘要： The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.

    摘要翻译： 本发明涉及作为rho相关蛋白激酶抑制剂的合成桥联双环化合物。 本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。 本发明另外涉及预防或治疗与细胞骨架重组相关的疾病或病症的方法。 该方法包括向受试者施用治疗有效量的式I的Rho激酶抑制性化合物，其中所述量有效地影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞 - 基底粘连的改变。 在一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。 在另一个实施方案中，该方法治疗与过度细胞增殖，重塑，炎症，血管收缩，支气管收缩，气道高反应性和水肿相关的肺的疾病或病症。

    Method for treating pulmonary diseases using rho kinase inhibitor compounds
    10.
    发明授权
    Method for treating pulmonary diseases using rho kinase inhibitor compounds 失效
    使用rho激酶抑制剂化合物治疗肺部疾病的方法

    公开(公告)号：US08299096B2

    公开(公告)日：2012-10-30

    申请号：US12492494

    申请日：2009-06-26

    申请人： Tomas Navratil ,  Ward M. Peterson ,  John W. Lampe ,  Emilee H. Fulcher ,  Scott D. Sorensen

    发明人： Tomas Navratil ,  Ward M. Peterson ,  John W. Lampe ,  Emilee H. Fulcher ,  Scott D. Sorensen

    IPC分类号： A01N43/40 ,  A61K31/445 ,  C07D211/32 ,  C07D231/56 ,  C07D207/00 ,  C07D295/00

    CPC分类号： A61K31/4545 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12

    摘要： This invention is directed to methods of preventing or treating diseases or conditions of the lungs associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema. Particularly, this invention is directed to methods of treating pulmonary diseases such as asthma; chronic obstructive pulmonary disease; respiratory tract illness caused by respiratory syncytial virus; pulmonary arterial hypertension; acute respiratory distress syndrome and ventilator induced lung injury; cystic fibrosis; bronchiectasis; alpha-1-antitrypsin deficiency; rhinitis; rhinosinusitis; primary ciliary dyskinesia; pneumonia; bronchiolitis caused by agents other than respiratory syncytial virus; and interstitial lung disease including lymphangioleiomyomatosis; idiopathic pulmonary fibrosis; obliterative bronchiolitis or bronchiolitis obliterans organizing pneumonia due to lung transplantation or HSCT; nonspecific interstitial pneumonia; cryptogenic organizing pneumonia; acute interstitial pneumonia; respiratory bronchiolitis-associated interstitial lung disease; or pulmonary sarcoidosis. The method comprises administering to a subject an effective amount of a rho kinase inhibitor compound to treat the disease.

    摘要翻译： 本发明涉及预防或治疗与过度细胞增殖，重塑，炎症，血管收缩，支气管收缩，气道高反应性和水肿相关的肺的疾病或病症的方法。 特别地，本发明涉及治疗肺部疾病如哮喘的方法; 慢性阻塞性肺疾病; 呼吸道合胞病毒引起的呼吸道疾病; 肺动脉高压; 急性呼吸窘迫综合征和呼吸机诱发肺损伤; 囊性纤维化; 支气管扩张 α-1-抗胰蛋白酶缺乏症; 鼻炎; 鼻鼻窦炎 原发性纤毛运动障碍; 肺炎; 由呼吸道合胞病毒以外的药剂引起的细支气管炎; 间质性肺病包括淋巴管平滑肌瘤病; 特发性肺纤维化; 闭塞性细支气管炎或闭塞性细支气管炎由于肺移植或HSCT而组织肺炎; 非特异性间质性肺炎 隐源性机体性肺炎 急性间质性肺炎 呼吸性细支气管炎相关间质性肺病; 或肺结节病。 该方法包括向受试者施用有效量的rho激酶抑制剂化合物以治疗该疾病。