公开(公告)号：US20040127705A1

公开(公告)日：2004-07-01

申请号：US10615836

申请日：2003-07-10

Applicant: DAIICHI PHARMACEUTICAL CO., LTD.

Inventor： Akira Mizuno ,  Makoto Shibata ,  Tomoe Kamei ,  Harukazu Fukami ,  Norio Inomata

IPC: C07D498/02 ,  A61K031/542 ,  A61K031/554

CPC classification number: C07D513/04 ,  C07D207/36

Abstract: A pyrrolesulfonamide derivative having the following formula (I): 1 wherein the ring P represented by 2 is a pyrrole ring having the following structure: 3 wherein R represents alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; 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 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR1, in which R1 represents H, or alkyl, aralkyl or aryl; l stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group 4 in which W represents CH, Cnull or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is Cnull; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. 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.

Abstract translation: 具有下式（I）的吡咯磺酰胺衍生物：其中由代表的环P是具有以下结构的吡咯环：其中R表示烷基，环烷基，环烷基 - 烷基或芳烷基; 虚线表示存在或不存在键; 当存在键时，Z 2不存在，Z1表示H，但当不存在键时，Z1表示H，Z2表示OH或Z1，Z2组合在一起表示O或NOR1基团，其中R1表示 H或烷基，芳烷基或芳基; l代表0或1; A表示亚烷基，亚烯基或亚炔基; Y表示W表示CH，C =或N的基团; 当W为CH或N时，m代表0或1，当W为C =时，m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基。 化合物（I）具有强的5-羟色胺-2受体拮抗作用，毒性低，副作用小，作为循环系统疾病如缺血性心脏病，脑血管障碍和周围循环障碍的治疗有用。