首页> 外国专利> SPIROCYCLIC COMPOUNDS CONTAINING SPIROINDOLYL-3,1'-PYRROLO3,4-CPYRROLE CORE AND SULPHUR-CONTAINING AMINO ACID RESIDUES

SPIROCYCLIC COMPOUNDS CONTAINING SPIROINDOLYL-3,1'-PYRROLO3,4-CPYRROLE CORE AND SULPHUR-CONTAINING AMINO ACID RESIDUES

机译:包含螺[吲哚基-3,1'-吡咯[3,4-C]吡咯]核和含硫氨基酸残基的螺环化合物

摘要

The present invention relates to spirocyclic compounds on the basis of 2-oxindole derivatives containing a spiro[indolyl-3,1′-pyrrolo[3,4-c]-pyrrole] core and biogenic sulphur-containing amino acid residues, which display a glucocorticoid-mimicking action by influencing 11β-HSD1 enzyme cortisone-cortisol conversion, or by inhibiting GRs- or GITR- or mineralocorticoid receptors, or other targets, but do not interfere with steroidal haemostasis in HPA; and compositions containing same and their use for therapy as part of undifferentiated stroke therapy (in the absence of final verification of the stroke subtype) at various stages of acute ischemic stroke (AIS), during the period of recovery from stroke and craniocerebral trauma, in patients with chronic cerebrovascular pathology (against a background of diabetes), in combinational therapy for Alzheimer's disease and encephalopathy of various origin (discirculatory, alcoholic, infectious-toxic), and diabetes, combinational therapy for retinal degenerative eye diseases, as part of combinational therapy for metabolic syndrome (obesity, in patients suffering from Cushing's syndrome, Reaven metabolic syndrome (also known as syndrome X or insulin resistance syndrome) and other diseases where GCs hormones play a key role.
机译:本发明涉及基于2-氧吲哚衍生物的螺环化合物,其包含螺[吲哚基-3,1'-吡咯并[3,4-c]-吡咯]核心和生物来源的含硫氨基酸残基,其显示通过影响11β-HSD1酶可的松->皮质醇的转化,或通过抑制GRs-或GITR-或盐皮质激素受体或其他靶标来模拟糖皮质激素的作用,但不干扰HPA中的类固醇止血。以及从中风和颅脑外伤恢复期间,在急性缺血性中风(AIS)各个阶段中,作为未分化中风治疗的一部分(未对中风亚型进行最终鉴定)的药物及其组合物,患有慢性脑血管病变(针对糖尿病的患者),针对多种来源的阿尔茨海默氏病和脑病(循环系统,酒精中毒,感染毒性)和糖尿病的联合治疗,以及视网膜变性眼病的联合治疗,作为联合治疗的一部分用于代谢综合征(肥胖症,患有库欣综合征的患者,瑞文代谢综合征(也称为X综合征或胰岛素抵抗综合征)和其他由GC激素起关键作用的疾病。

著录项

  • 公开/公告号US2016297828A1

    专利类型

  • 公开/公告日2016-10-13

    原文格式PDF

  • 申请/专利权人 GLEB VLADIMIROVICH ZAGORII;

    申请/专利号US201415100543

  • 发明设计人 GLEB VLADIMIROVICH ZAGORII;

    申请日2014-12-03

  • 分类号C07D487/20;C07C55/10;C07D307/62;

  • 国家 US

  • 入库时间 2022-08-21 14:39:22

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