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1. 发明申请

WO1995028387A1 BENZAMIDE COMPOUND AND MEDICINAL USE THEREOF 审中-公开
标题翻译：苯并噻唑类化合物及其药物用途
公开(公告)号：WO1995028387A1
公开(公告)日：1995-10-26
申请号：PCT/JP1995000747
申请日：1995-04-17
申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , ARITA, Masafumi , SAITOH, Tadamasa , MINOGUCHI, Masanori , YAMAGAMI, Keiji , SATOH, Hiroyuki
发明人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07D213/82 , C07D215/42 , C07D239/42 , C07D239/48 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D473/34 , C07D487/04
摘要： A benzamide compound represented by general formula (I), (wherein each symbol is as defined in the specification); an isomer or pharmaceutically acceptable acid-addition salt thereof; a medicinal composition comprising a therapeutically available dose of the compound and pharmaceutically acceptable fillers; and remedies for hypertension, angina pectoris, asthma, and renal and peripheral circulation disturbances, and a cerebral vasospasm depressant, each containing the above compound. This compound has a potent smooth muscle relaxant effect and, similar to conventional calcium antagonists, a hypotensive effect and a cerebral and coronary vasodilator effect. Furthermore it has a persistent renal and peripheral circulation ameliorant effect and, as different from the calcium antagonists, the effect of the inhibiting vasoconstriction caused by various agonists, and is perorally administrable. Hence it is useful as a preventive or remedy for diseases of circulatory organs including coronary, cerebral, renal and peripheral arteries, for example, remedies for hypertension, anginal pectoris, and renal and peripheral circulation disturbances, and a cerebral vasospasm depressant. Also it is useful as an asthma remedy.
摘要翻译：由通式（I）表示的苯甲酰胺化合物（其中各符号如说明书中所定义）; 其异构体或药学上可接受的酸加成盐; 药物组合物，其包含治疗可用剂量的化合物和药学上可接受的填充剂; 以及高血压，心绞痛，哮喘，肾脏和周围循环障碍的补救措施，以及含有上述化合物的脑血管痉挛抑制剂。该化合物具有强效的平滑肌松弛作用，与常规钙拮抗剂相似，具有降血压作用和脑和冠状血管扩张作用。此外，它具有持久的肾和外周循环改善效果，并且与钙拮抗剂不同，是由各种激动剂引起的抑制血管收缩的作用，并且是经口给药的。因此，作为包括冠状动脉，脑，肾和外周动脉在内的循环器官疾病的预防或补救措施是有用的，例如高血压，心绞痛和肾脏和周围循环障碍的补救措施，以及脑血管痉挛抑制剂。也可作为哮喘的治疗方法。

2. 发明申请

WO1998029397A1 FUSED PYRIMIDINE COMPOUNDS AND MEDICINAL USE THEREOF 审中-公开
标题翻译：熔融吡嗪化合物及其药物用途
公开(公告)号：WO1998029397A1
公开(公告)日：1998-07-09
申请号：PCT/JP1997004782
申请日：1997-12-22
申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , TANAKA, Hiroshi , SEIO, Koji , KIMURA, Koreichi , MINOGUCHI, Masanori , UEHATA, Masayoshi , KOHARA, Toshiyuki , OHASHI, Yoshitaka , MORIO, Yasunori , YAMAGAMI, Keiji
发明人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
IPC分类号： C07D239/94
CPC分类号： C07D487/04 , C07D239/94 , C07D239/95 , C07D495/04
摘要： Fused pyrimidine compounds represented by general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, drugs containing the compounds of general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, and medicinal compositions containing the compounds of general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein each symbol is as defined in the specification. Because of having an excellent CRF receptor antagonism, these compounds are useful as drugs, in particular, remedies for human depression, eating disturbance including dietary negativism and overeating, Alzheimer's disease, schizophrenia, Parkinson's disease, Huntington's chorea, amyotrophic lateral sclerosis, mania, psychophysiologic disorder, senile dementia, panic disorder, cerebral attack, inflammation in autoimmune diseases such as rheumatoid arthritis, pain, obesity, Gilles de la Tourette's disease, alcohol dependence, climacteric disturbance and premenstrual tension syndrome, cardiac circulatory drugs such as hypotensive drugs, immunopotentiators, immunosuppressors and drugs for improving the conditions of patients in intensive care units (ICU).
摘要翻译：由通式（I）表示的稠合嘧啶化合物，其药学上可接受的盐或其水合物，含有通式（I）的化合物的药物，其药学上可接受的盐或其水合物，以及含有一般化合物的药物组合物式（I），其药学上可接受的盐或其水合物，其中每个符号如说明书中所定义。由于具有优异的CRF受体拮抗作用，这些化合物可用作药物，特别是用于人类抑郁症，饮食障碍，饮食消极反应和暴饮暴食，阿尔茨海默病，精神分裂症，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化，躁狂症，心理生理疾病，老年性痴呆，恐慌症，脑部发作，自身免疫性疾病如类风湿性关节炎，疼痛，肥胖，杜伊勒图雷特氏病，酒精依赖性，更年期障碍和经前期紧张综合征，心脏循环药物如降血压药物，免疫增强剂，免疫抑制剂和药物，用于改善重症监护病房（ICU）患者的病情。

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