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    • 101. 发明公开
    • PYRROLOAZEPINE DERIVATIVES
    • PYRROLOAZEPIN衍
    • EP0807632A4
    • 1998-12-09
    • EP96939340
    • 1996-12-02
    • SUNTORY LTD
    • MIZUNO AKIRASHIBATA MAKOTOIWAMORI TOMOESHIMAMOTO TETSUONAKANISHI KYOKOINOMATA NORIO
    • A61P7/00A61P9/00C07D207/34C07D487/04C07D495/20A61K31/55
    • C07D487/04C07D207/34
    • Disclosed is a pyrroloazepine derivative or a salt thereof. The pyrroloazepine derivative is represented by the following formula (I): wherein the ring P represented by means a pyrrole ring represented by the following structure: in which R1 represents alkyl, cycloalkyl or the like, and R2 represents H or alkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present/and Z1 represents H but, when the bond is absent, Z1 and Z2 are both H; Z1 represents H and Z2 represents a group OR3 in which R3 represents H, alkyl, aralkyl or the like; Z1 and Z2 both represent groups SR4 in which R4 represents alkyl, aralkyl or the like; or Z1 and Z2 are combined together to represent O, a group NOR5 in which R5 represents H, alkyl or the like, or a C2-C3 alkylenedithio; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C= or N, m stands for 0 or 1, n stands for 1, 2 or 3, G represents O, S, C=O, sulfinyl, sulfonyl, alkylene, alkenylene, acetal or the like; E1 and E2 represent H or lower alkyl group; and D represents an aromatic hydrocarbon or am aromatic heterocyclic ring. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
    • (1)表示的环P是指由(2)或(3)表示的吡咯环(其中R 1表示烷基,环烷基等,并且R 2表示H)表示的吡咯环,其中R表示吡咯并氮杂环庚烯衍生物或其盐, 或烷基); 虚线表示键的存在或不存在; 当键存在时,则Z 2不存在且Z 1表示H; 当键不存在时,则Z 1和Z 2各自表示H,Z 1表示H,Z 2表示OR 3(其中R 3表示H,烷基,芳烷基等)表示的基团,Z 1和Z 2各自表示SR 4 其中R 4代表烷基,芳烷基等),或Z 1和Z 2结合表示O,NOR 5(其中R 5代表H,烷基等)或C 2-3亚烷基二硫代表的基团; A代表亚烷基,亚烯基或亚炔基; Y代表由(4)表示的基团(其中W代表CH,C =或N; m为0或1; n为1,2或3; G代表O,S,C = O,亚磺酰基,磺酰基, 亚烷基,亚烯基,缩醛等; E1和E2各自表示H或低级烷基;并且D表示芳族烃基或杂芳基)。 化合物(I)具有有效的血清素-2受体拮抗作用,毒性和副作用减少,是缺血性心脏病,脑血管障碍等循环系统疾病的有用治疗剂; 和外周循环障碍。