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治疗中枢神经障碍、胃肠障碍和心血管障碍的吲哚－2－酮衍生物

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摘要

本发明涉及新的通式(I)的3，3-二取代的吲哚-2-酮衍生物。这些新化合物可用于治疗或预防中枢神经系统、胃肠系统或心血管系统障碍。

著录项

公开/公告号CN100572377C

专利类型发明授权
公开/公告日2009-12-23

原文格式PDF
申请/专利权人埃吉斯药物工厂;
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申请/专利号CN200580020271.2
发明设计人 B·沃尔克;J·鲍尔科齐;G·希米格;T·梅泽伊;R·卡皮莱尔尼德热菲;I·高恰伊;K·保罗吉;G·吉格雷;G·莱沃伊;K·莫里茨;C·莱韦莱基;N·西拉雷;G·塞纳希;A·埃杰德;L·G·哈尔申;
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申请日2005-05-11
分类号
代理机构中国国际贸易促进委员会专利商标事务所;
代理人李华英
地址匈牙利布达佩斯
入库时间 2022-08-23 09:03:51

法律信息

法律状态公告日

法律状态信息

法律状态
2011-07-20

未缴年费专利权终止 IPC(主分类):C07D 401/06 授权公告日:20091223 终止日期:20100511 申请日:20050511

专利权的终止
2009-12-23

授权

授权
2007-09-26

实质审查的生效

实质审查的生效
2007-08-01

公开

公开

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1. 治疗中枢神经障碍、胃肠障碍和心血管障碍的吲哚－2－酮衍生物 [P] . 中国专利： CN100572377C . 2009.12.23
2. 治疗中枢神经系统障碍的3-(((4-苯基)-哌嗪-1-基)-烷基)-3-烷基-1,3-二氢-2H-吲哚-2-酮衍生物和相关化合物 [P] . 中国专利： CN1993324B . 2010.12.15
3. In view of their capability to antagonize the actions of neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control. [P] . EA009217B1 . 2007-12-28

机译：考虑到它们通过阻断神经激肽受体来拮抗神经激肽的作用，特别是通过阻断NK1受体来拮抗P物质的作用的能力，根据本发明的化合物可用作药物，特别是在预防和治疗中。治疗神经激肽介导的疾病，例如中枢神经系统疾病，尤其是抑郁症，焦虑症，与压力有关的疾病，睡眠障碍，认知障碍，人格障碍，精神分裂性障碍，进食障碍，神经退行性疾病，成瘾障碍，情绪疾病，性功能障碍，疼痛和其他中枢神经系统相关疾病;炎;过敏性疾病呕吐胃肠道疾病，特别是肠易激综合症（IBS）;皮肤疾病;血管痉挛性疾病;纤维化和胶原蛋白疾病;与免疫增强或抑制，风湿性疾病和体重控制有关的疾病。
4. compound of formula i; pharmaceutical composition; method of treating disorders that are related to or affected by inhibition of norepinephrine reuptake, the 5-ht6 receptor or the 5-ht2a receptor; a method of treating a learning disorder, a cognitive disorder, a memory disorder, a personality disorder, a behavioral disorder, a movement disorder, a neurodegenerative disorder, drug withdrawal disorder, sleep, an eating disorder, acute drug toxicity, a cardiovascular disorder, a sexual dysfunction, a gastrointestinal disorder, a genitourinary disorder, a pain disorder, a nervous disorder or a symptom disorder vasomotor; method of treating alzheimer's disease, attention deficit disorder, schizophrenia, parkinson's disease, tardive dyskinesia, ataxia, bradykinesia, paroxysmal dyskinesias, restless leg syndrome, tremor, essential tremor epilepsy, stroke or head trauma; method of treating coronary artery disease, myocardial infarction, transient ischemic attack, angina, atrial fibrillation, p [P] . BRPI0706523A2 . 2011-01-04

机译：式I化合物;药物组合物;治疗与去甲肾上腺素再摄取，5-ht6受体或5-ht2a受体相关或受其抑制的疾病的方法;一种治疗学习障碍，认知障碍，记忆障碍，人格障碍，行为障碍，运动障碍，神经退行性疾病，戒断药物，睡眠，进食障碍，急性药物毒性，心血管疾病的方法，性功能障碍，胃肠道疾病，泌尿生殖系统疾病，疼痛疾病，神经疾病或症状-血管舒缩;治疗阿尔茨海默氏病，注意力缺陷障碍，精神分裂症，帕金森氏病，迟发性运动障碍，共济失调，运动迟缓，阵发性运动障碍，不安腿综合征，震颤，原发性震颤癫痫，中风或头部外伤的方法;治疗冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，心房颤动，p的方法
5. spirocyclic heterocyclic compound, pharmaceutical composition, method to bind opioid receptors, methods to prevent or treat pain, gastrointestinal dysfunction, a urogenital tract disorder, an immunomodulatory disorder, an inflammatory disorder, a respiratory function disorder, anxiety, mood disorder, a stress-related disorder, sympathetic nervous system disorder, cough, and a motor disorder, method for treating traumatic injury to the central nervous system, methods for preventing or treating stroke, cardiac arrhythmia, glaucoma, and sexual dysfunction, methods for treating a condition selected from the group consisting of shock, cerebral edema, cerebral ischemia, cerebral deficit after cardiac surgery (bypass) and graft, systemic lupus erythematosus, hodgkin's disease, sjogren's disease, epilepsy, and rejection in organ transplants and skin grafts, and to treat substance dependence, method to improve organ and cell survival, and cardioprotection after myocardial infarction, methods to [P] . BRPI0415165A . 2007-01-09

机译：螺环杂环化合物，药物组合物，阿片受体的结合方法，预防或治疗疼痛，胃肠道功能障碍，泌尿生殖道疾病，免疫调节疾病，炎性疾病，呼吸功能疾病，焦虑症，情绪障碍，与压力有关的方法疾病，交感神经系统疾病，咳嗽和运动障碍，治疗中枢神经系统创伤的方法，预防或治疗中风，心律不齐，青光眼和性功能障碍的方法，治疗选自以下组的疾病的方法包括休克，脑水肿，脑缺血，心脏手术（旁路）和移植后脑缺损，系统性红斑狼疮，霍奇金病，干燥综合征，癫痫和器官移植和皮肤移植排斥反应，以及治疗药物依赖的方法改善器官和细胞存活率以及心肌梗死后的心脏保护作用，