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    Therapeutic morpholino-substituted compounds
    2.
    发明授权
    Therapeutic morpholino-substituted compounds 失效
    治疗性吗啉取代的化合物

    公开(公告)号：US06977255B2

    公开(公告)日：2005-12-20

    申请号：US10181485

    申请日：2001-01-24

    申请人： Alan D. Robertson ,  Shaun Jackson ,  Vijaya Kenche ,  Cindy Yap ,  Hishani Parbaharan ,  Phil Thompson

    发明人： Alan D. Robertson ,  Shaun Jackson ,  Vijaya Kenche ,  Cindy Yap ,  Hishani Parbaharan ,  Phil Thompson

    IPC分类号： A61K9/02 ,  A61K9/08 ,  A61K9/12 ,  A61K9/20 ,  A61K9/48 ,  A61K31/5377 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/04 ,  A61P37/06 ,  A61P43/00 ,  C07D215/38 ,  C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D471/04 ,  A61K31/352

    CPC分类号： C07D215/38 ,  C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D471/04

    摘要： Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer, and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

    摘要翻译： 吗啉取代的吡啶并嘧啶，喹诺酮和苯并吡喃酮衍生物抑制磷酸肌醇（PI）3-激酶，其是调节血小板粘附过程的酶。 因此，所讨论的化合物具有抗血栓形成活性以及其它药物性质。 所要求的化合物由式（I），（II）和（III）表示。 PI 3激酶产生在血液流动条件下刺激血小板粘附的3-磷酸化PI第二信使。 因为血小板粘附是形成血栓的必要步骤，所以这些条件下这些PI3-激酶化合物的抑制可抑制或预防血栓形成。 该化合物可用于治疗PI 3激酶依赖性疾病，包括心血管疾病如冠状动脉闭塞，中风，急性冠状动脉综合征，急性心肌梗塞，血管再狭窄，动脉粥样硬化和不稳定型心绞痛; 呼吸系统疾病如哮喘，慢性阻塞性肺疾病（COPD）和支气管炎; 炎症性疾病; 包括诸如神经胶质瘤，前列腺癌，小细胞肺癌和乳腺癌等癌症的肿瘤，以及与无序白细胞功能相关的疾病，例如自身免疫性和炎性疾病。

    Therapeutic morpholino-substituted compounds
    6.
    发明授权
    Therapeutic morpholino-substituted compounds 失效
    治疗性吗啉取代的化合物

    公开(公告)号：US07572791B2

    公开(公告)日：2009-08-11

    申请号：US12019061

    申请日：2008-01-24

    申请人： Alan D. Robertson ,  Shaun Jackson ,  Vijaya Kenche ,  Cindy Yaip ,  Hishani Parbaharan ,  Phil Thompson

    发明人： Alan D. Robertson ,  Shaun Jackson ,  Vijaya Kenche ,  Cindy Yaip ,  Hishani Parbaharan ,  Phil Thompson

    IPC分类号： A61K31/5375 ,  C07D413/02

    CPC分类号： C07D215/38 ,  C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D471/04

    摘要： Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer; and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

    摘要翻译： 吗啉取代的吡啶并嘧啶，喹诺酮和苯并吡喃酮衍生物抑制磷酸肌醇（PI）3-激酶，其是调节血小板粘附过程的酶。 因此，所讨论的化合物具有抗血栓形成活性以及其它药物性质。 所要求的化合物由式（I），（II）和（III）表示。 PI 3激酶产生在血液流动条件下刺激血小板粘附的3-磷酸化PI第二信使。 因为血小板粘附是形成血栓的必要步骤，所以这些条件下这些PI3-激酶化合物的抑制可抑制或预防血栓形成。 该化合物可用于治疗PI 3激酶依赖性疾病，包括心血管疾病如冠状动脉闭塞，中风，急性冠状动脉综合征，急性心肌梗塞，血管再狭窄，动脉粥样硬化和不稳定型心绞痛; 呼吸系统疾病如哮喘，慢性阻塞性肺疾病（COPD）和支气管炎; 炎症性疾病; 肿瘤包括癌症，如胶质瘤，前列腺癌，小细胞肺癌和乳腺癌; 以及与无序白细胞功能相关的疾病，如自身免疫性疾病和炎性疾病。

    Phosphotetrahydropyran compounds for the treatment of wounds and fibrotic disorders
    8.
    发明授权
    Phosphotetrahydropyran compounds for the treatment of wounds and fibrotic disorders 失效
    用于治疗伤口和纤维化疾病的磷酸四氢吡喃化合物

    公开(公告)号：US08557783B2

    公开(公告)日：2013-10-15

    申请号：US13318065

    申请日：2010-04-28

    申请人： Alan D. Robertson ,  Diego Silva ,  Ian Alexander McDonald

    发明人： Alan D. Robertson ,  Diego Silva ,  Ian Alexander McDonald

    IPC分类号： A61K31/70 ,  A61K31/7028

    CPC分类号： A61K31/665

    摘要： Methods of using phosphotetrahydropyran compounds for treatment of fibrotic and scarring disorders, e.g. pulmonary fibrosis, fibrosis associated with surgical procedures, wound healing disorders, scar formation, sclerotic disorders, ocular fibrotic disorders, ocular healing disorders, ocular fibrosis after surgery, glaucoma, tendon scarring disorders, joint scarring disorders, kidney interstitial fibrosis and glomerular fibrosis and tubular fibrosis of the kidney.

    摘要翻译： 使用磷酸四氢吡喃化合物治疗纤维化和瘢痕障碍的方法，例如 肺纤维化，与外科手术相关的纤维化，伤口愈合障碍，瘢痕形成，硬化性疾病，眼部纤维化病症，眼部愈合障碍，手术后眼部纤维化，青光眼，腱瘢痕障碍，关节瘢痕形成障碍，肾间质性纤维化和肾小球纤维化和肾小管 肾纤维化。

    Therapeutic Morpholino-Substituted Compounds
    9.
    发明申请
    Therapeutic Morpholino-Substituted Compounds 失效
    治疗性吗啉取代的化合物

    公开(公告)号：US20080206312A1

    公开(公告)日：2008-08-28

    申请号：US12019061

    申请日：2008-01-24

    申请人： Alan D. Robertson ,  Shaun Jackson ,  Vijaya Kenche ,  Cindy Yaip ,  Hishani Parbaharan ,  Phil Thompson

    发明人： Alan D. Robertson ,  Shaun Jackson ,  Vijaya Kenche ,  Cindy Yaip ,  Hishani Parbaharan ,  Phil Thompson

    IPC分类号： A61K31/5377 ,  C07D413/04 ,  A61K9/12 ,  A61K47/06 ,  A61P9/00 ,  A61P11/00 ,  A61P35/04 ,  A61P7/00

    CPC分类号： C07D215/38 ,  C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D471/04

    摘要： Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer; and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

    摘要翻译： 吗啉取代的吡啶并嘧啶，喹诺酮和苯并吡喃酮衍生物抑制磷酸肌醇（PI）3-激酶，其是调节血小板粘附过程的酶。 因此，所讨论的化合物具有抗血栓形成活性以及其它药物性质。 所要求的化合物由式（I），（II）和（III）表示。 PI 3激酶产生在血液流动条件下刺激血小板粘附的3-磷酸化PI第二信使。 因为血小板粘附是形成血栓的必要步骤，所以这些条件下这些PI3-激酶化合物的抑制可抑制或预防血栓形成。 该化合物可用于治疗PI 3激酶依赖性疾病，包括心血管疾病如冠状动脉闭塞，中风，急性冠状动脉综合征，急性心肌梗塞，血管再狭窄，动脉粥样硬化和不稳定型心绞痛; 呼吸系统疾病如哮喘，慢性阻塞性肺疾病（COPD）和支气管炎; 炎症性疾病; 肿瘤包括癌症，如胶质瘤，前列腺癌，小细胞肺癌和乳腺癌; 以及与无序白细胞功能相关的疾病，如自身免疫性疾病和炎性疾病。