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1. 发明申请

WO1994023721A1 NOVEL MEDICINAL USE OF DIHYDROPYRIDINE DERIVATIVE 审中-公开
标题翻译：二氢吡啶衍生物的新药物使用
公开(公告)号：WO1994023721A1
公开(公告)日：1994-10-27
申请号：PCT/JP1994000460
申请日：1994-03-22
申请人： THE GREEN CROSS CORPORATION , NAKAJIMA, Masahide , NAKAMURA, Norifumi , WANG, Feng , YAMANOUCHI, Koichi , HAYASHI, Kazutaka , KIDO, Hideaki , KUBO, Yoshiji , OKITA, Minori , UCHIDA, Takeshi , WATANABE, Masahiro , YAMANAGA, Katsumi , SHINYAMA, Hiroshi , KAWAMURA, Toru , NARITA, Yuji
发明人： THE GREEN CROSS CORPORATION
IPC分类号： A61K31/455
CPC分类号： A61K31/44 , A61K31/495 , Y10S514/824 , Y10S514/87 , Y10S514/925 , Y10S514/929
摘要： Novel medicinal uses of a dihydropyridine derivative represented by general formula (I) or an acid-addition salt thereof for promoting PGI2 production and preventing or treating hyperlipemia, arteriosclerosis and brain diseases. In said formula (I), R1, R2 and R3 represent each independently alkyl, etc.; R4 represents hydrogen, etc.; R5 represents nitro, haloalkyl, cyano, etc.; X represents vinylene or azomethine; A represents alkylene; and B represents -NR6R7 or a group (a) wherein R6 and R7 represent each independently alkyl, aralkyl, aryl, etc.; R8 and Ar represent each aryl, etc.; and n represents 0, 1 or 2.
摘要翻译：用于促进PGI 2产生和预防或治疗高脂血症，动脉硬化和脑疾病的由通式（I）表示的二氢吡啶衍生物或其酸加成盐的新药物用途。在所述式（I）中，R 1，R 2和R 3各自独立地表示烷基等。 R4代表氢等; R5代表硝基，卤代烷基，氰基等; X表示亚乙烯基或偶氮甲碱; A表示亚烷基; 和B代表-NR6R7或（a）其中R6和R7各自表示烷基，芳烷基，芳基等; R8和Ar表示各芳基等; n表示0,1或2。

2. 发明申请

WO1992001468A1 ENDOSERINE CONVERTING ENZYME INHIBITOR OR VASCULAR TWITCH REMEDY 审中-公开
标题翻译：内酯转化酶抑制剂或血管舒张补救
公开(公告)号：WO1992001468A1
公开(公告)日：1992-02-06
申请号：PCT/JP1991000808
申请日：1991-06-15
申请人： THE GREEN CROSS CORPORATION , MORIMOTO, Shiro , MATSUMURA, Yasuo , UCHIDA, Takeshi; , KIDO, Hideaki; , SHINYAMA, Hiroshi; , WATANABE, Masahiro;
发明人： THE GREEN CROSS CORPORATION
IPC分类号： A61K37/64
CPC分类号： C07K5/06191 , A61K38/55 , C07K9/001
摘要： An endoserine converting enzyme inhibitor, a vascular twitching agent or a vascular twitch remedy containing a compound represented by general formula (I) or its salt as the active ingredient, wherein A1 and A2 represent each amino acid residue, X represents hydroxy or monosaccharide residue, and R1 represents hydroxy, alkyl, alkoxy, allyl or -NR2R3 wherein R2 and R3 represent each hydrogen or alkyl. A pharmaceutical preparation containing the compound (I) or its salt as the active ingredient has an activity of inhibiting an endoserine converting enzyme or controlling vascular twitch. Therefore, it is effective in preventing or treating hypertension, bronchial asthma, peripheral circulatory disturbance, cerebrovascular spasm (occurring after cerebral hemorrhage, subarachnoid hemorrhage, etc.), coronary twitch (including attack caused by twitch occurring when a constricted site is reopened by, for example, laser cautery, especially one which is difficultly curable and for which even nitroglycerol is inefficacious, that is, attack caused by postoperational coronary twitch and angina pectoris induced by coronary twitch) and other vascular twitches of mammals including man, pig, cattle, horse, dog, rat and mouse.
摘要翻译：含有由通式（I）表示的化合物或其盐作为活性成分的内丝氨酸转化酶抑制剂，血管抽搐剂或血管抽搐药，其中A1和A2表示各氨基酸残基，X表示羟基或单糖残基，并且R 1表示羟基，烷基，烷氧基，烯丙基或-NR 2 R 3，其中R 2和R 3表示各自的氢或烷基。含有化合物（I）或其盐作为活性成分的药物制剂具有抑制内丝蛋白转化酶或控制血管抽搐的活性。因此，有效预防或治疗高血压，支气管哮喘，周围循环障碍，脑血管痉挛（脑出血，蛛网膜下腔出血等发生），冠状动脉抽搐（包括由收缩部位重新开放引起的抽搐引起的攻击，例如，激光烧灼，特别是难以固化的，甚至硝酸甘油无效，即由冠状动脉抽搐引起的术后冠状动脉抽搐和心绞痛引起的攻击）以及哺乳动物的其他血管抽搐，包括人，猪，牛，马，狗，老鼠和老鼠。

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