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    INHIBITION OF THE FORMATION OF VASCULAR HYPERPERMEABILITY
    3.
    发明申请
    INHIBITION OF THE FORMATION OF VASCULAR HYPERPERMEABILITY 审中-公开
    抑制血管超敏反应性的形成

    公开(公告)号：WO0027414A3

    公开(公告)日：2000-09-08

    申请号：PCT/US9925903

    申请日：1999-11-03

    Applicant: BASF AG ,  ARNOLD LEE D ,  BOUSQUET PETER F

    Inventor： ARNOLD LEE D ,  BOUSQUET PETER F

    IPC: A61K45/00 ,  A61K31/7105 ,  A61K38/00 ,  A61K38/17 ,  A61K38/19 ,  A61K39/395 ,  A61K48/00 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P7/10 ,  A61P9/00 ,  A61P9/02 ,  A61P9/10 ,  A61P11/06 ,  A61P11/16 ,  A61P13/00 ,  A61P13/02 ,  A61P15/00 ,  A61P17/02 ,  A61P19/00 ,  A61P27/00 ,  A61P27/06 ,  A61P27/12 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07K14/71 ,  A61K31/415

    CPC classification number: C07K14/71 ,  A61K38/00 ,  A61K39/39533 ,  A61K45/06 ,  A61K2039/505 ,  C12N15/1137 ,  C12N15/1138 ,  C12N2310/11 ,  C12N2310/12 ,  A61K2300/00

    Abstract: Vascular hyperpermeability and the subsequent events such as macular edema, retinoblastoma, ocular ischemia, ocular inflammatory disease or infection, choroidal melanoma, edematous side-effects induced by iron chelation therapy, pulmonary edema, myocardial infarction, rheumatoid diseases, anaphylaxis, allergies, hypersensitive reactions, cerebral edema, brain tumor fluid-filled cysts, communicating hydrocephalus, carpal tunnel syndrome, organ damage resulting from a burn, irritation or infection, erythema multiforme, edematous macules and other disorders, brain tumors, tumor effusions, lung or breast carcinomas, ascites, pleural effusions, pericardial effusions, high altitude "sickness", radioanaphylaxis, radiodermatitis, glaucoma, conjunctivitis, choroidal melanoma, adult respiratory distress syndrome, asthma, bronchitis, ovarian hyperstimulation syndrome, polycystic ovary syndrome, menstrual swelling, menstrual cramps, stroke, head trauma, cerebral infarct or occlusion, hyotension, ulcerations, sprains, fractures, effusions associated with synovitis, diabetic complications, hyperviscosity syndrome, liver cirrhosis, microalbuminuria, proteinuria, oliguria, electrolyte imbalance, nephrotic syndrome, exudates, fibroses, keloid, can be inhibited by the administration of a compound that inhibits the enzyme activity of the VEGF tyrosine kinase receptor known as KDR tyrosine kinase. The preferred compound 4,5-dihydro-3-pyridin-4-yl-1(2)H-benzo[g]indazole selectively inhibits the function of KDR tyrosine kinase but do not block the activity of Flt-1 tyrosine kinase which is another VEGE tyrosine kinase receptor.

    Abstract translation: 血管渗透性过高以及随后的事件，如黄斑水肿，视网膜母细胞瘤，眼部缺血，眼部炎性疾病或感染，脉络膜黑色素瘤，铁螯合疗法引起的水肿副作用，肺水肿，心肌梗塞，类风湿性疾病，过敏反应，过敏，过敏反应 ，脑水肿，脑肿瘤充满液体的囊肿，交通性脑积水，腕管综合征，由烧伤，刺激或感染引起的器官损伤，多形性红斑，水肿性斑疹和其他疾病，脑肿瘤，肿瘤积液，肺癌或乳腺癌，腹水 ，胸膜积液，心包积液，高原“疾病”，放射性过敏反应，放射性皮炎，青光眼，结膜炎，脉络膜黑素瘤，成人呼吸窘迫综合征，哮喘，支气管炎，卵巢过度刺激综合征，多囊卵巢综合征，月经肿胀，月经来潮， 外伤，脑梗塞或闭塞，高血压， 可以通过施用抑制滑膜炎的化合物来抑制与滑膜炎，糖尿病并发症，高粘滞综合征，肝硬化，微量白蛋白尿，蛋白尿，少尿，电解质失衡，肾病综合征，渗出物，纤维化，瘢痕瘤相关的炎症，损伤，扭伤，骨折， 被称为KDR酪氨酸激酶的VEGF酪氨酸激酶受体的酶活性。 优选的化合物4,5-二氢-3-吡啶-4-基-1（2）H-苯并[g]吲唑选择性地抑制KDR酪氨酸激酶的功能，但不阻断Flt-1酪氨酸激酶的活性， 另一种VEGE酪氨酸激酶受体。

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