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16 条记录 (耗时 0.042 秒)

    Therapeutic substituted indole compounds and compositions thereof
    11.
    发明授权
    Therapeutic substituted indole compounds and compositions thereof 失效
    治疗性取代的吲哚化合物及其组合物

    公开(公告)号：US5225431A

    公开(公告)日：1993-07-06

    申请号：US660966

    申请日：1991-02-26

    申请人： Alan D. Robertson ,  Graeme R. Martin ,  Janet S. Buckingham

    发明人： Alan D. Robertson ,  Graeme R. Martin ,  Janet S. Buckingham

    IPC分类号： C07D209/16 ,  C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06

    CPC分类号： C07D403/06 ,  C07D209/16 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06

    摘要： The present invention is concerned with compounds of formula (I) ##STR1## wherein R, R.sup.1 and R.sup.2 are independently selected from hydrogen and C.sub.1-4 alkyl;R.sup.3 and R.sup.4 are independently selected from hydrogen, C.sub.1-6 alkyl (including cycloalkyl) and aryl (wherein the alkyl or aryl group, which latter includes benzyl, is optionally substituted by one or more atoms or groups independently selected from halogen, C.sub.1-4 alkyl and aryl), provided R.sup.3 benzyl or substituted benzyl when R.sup.4 =H;m is an integer of from 0 to 2;n is an integer of from 0 to 3;(W) is a group of formula (i), (ii), (iii), or (iv) ##STR2## wherein Y is selected from oxygen, methylene and >N--R.sup.5, where R.sup.5 is hydrogen, C.sub.1-4 alkyl, or benzyl, Z and Z' are independently selected from >C.dbd.O, >C.dbd.S and methylene, and the chiral center * in formula (i) or (ii) is in its (S) or (R) form or is a mixture thereof in any proportions;X is a group selected fromaryl (including heteroaryl)xanthenyldibenzofuranyl which group is optionally substituted;and salts and solvates thereof, the preparation of these compounds, pharmaceutical formulations containing them and their use in medicine, particularly in the treatment of migraine.

    摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2和R 2独立地选自氢和C 1-4烷基; R 3和R 4独立地选自氢，C 1-6烷基（包括环烷基）和芳基（其中后者包括苄基的烷基或芳基任选被一个或多个独立地选自卤素，C 1-4的一个或多个原子或基团取代 烷基和芳基），当R 4 = H时提供R 3苄基或取代的苄基; m为0〜2的整数; n为0〜3的整数， （ⅰ）Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y Y 选自氧，亚甲基和> N-R5，其中R5是氢，C1-4烷基或苄基，Z和Z'独立地选自C = O，> C = S和亚甲基，手性中心* 在式（ⅰ）或（ⅱ）中为其（S）或（R）形式或其任何比例的混合物; X是选自基团任选取代的芳基（包括杂芳基）呫吨基二苯并呋喃基的基团; 其盐和溶剂合物，这些化合物的制备，含有它们的药物制剂及其在医药中的用途，特别是用于治疗偏头痛。

    PHOSPHOTETRAHYDROPYRAN COMPOUNDS FOR THE TREATMENT OF WOUNDS AND FIBROTIC DISORDERS
    12.
    发明申请
    PHOSPHOTETRAHYDROPYRAN COMPOUNDS FOR THE TREATMENT OF WOUNDS AND FIBROTIC DISORDERS 失效
    用于治疗伤口和纤维性疾病的磷酸三氢吡喃化合物

    公开(公告)号：US20120045455A1

    公开(公告)日：2012-02-23

    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： A61K39/395 ,  A61P17/02 ,  A61P11/00 ,  A61K31/665

    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
    14.
    发明申请
    Therapeutic Morpholino-Substituted Compounds 审中-公开

    公开(公告)号：US20080312233A1

    公开(公告)日：2008-12-18

    申请号：US12115563

    申请日：2008-05-06

    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 ,  A61P11/00 ,  A61P9/00

    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.

    Therapeutic morpholino-substituted compounds
    15.
    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：US07405211B2

    公开(公告)日：2008-07-29

    申请号：US10961062

    申请日：2004-10-12

    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

    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，包括癌症如神经胶质瘤，前列腺癌，小细胞肺癌和乳腺癌的肿瘤，以及与无序白细胞功能如自身免疫性和炎性疾病相关的疾病。