公开(公告)号：US20030105074A1

公开(公告)日：2003-06-05

申请号：US10281194

申请日：2002-10-28

Applicant: Eisai Co., Ltd.

Inventor： Nobuhisa Watanabe ,  Norio Karibe ,  Kazuki Miyazaki ,  Fumihiro Ozaki ,  Atsushi Kamada ,  Shuhei Miyazawa ,  Yoshimitsu Naoe ,  Toshihiko Kaneko ,  Itaru Tsukada ,  Tadashi Nagakura ,  Hiroki Ishihara ,  Kohtarou Kodama ,  Hideyuki Adachi

IPC: A61K031/55 ,  A61K031/502 ,  C07D43/02

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D237/28 ,  C07D237/34 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D409/14 ,  C07D411/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/06 ,  C07D471/08 ,  C07D491/04 ,  C07D491/08 ,  C07D491/10

Abstract: The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: 1 wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is a cyano group, a nitro group or a chlorine atom, R1 is a chlorine atom, R2 is a methoxy group and Y is a 5- or 6-memberred amine ring substituted with a hydroxyl group is excluded.

Abstract translation: 本发明提供作为下述式表示的勃起功能障碍治疗剂的酞嗪化合物，其药理学上可接受的盐或其水合物：其中R1和R2彼此相同或不同，表示卤素原子， 可以被卤素原子取代的C1〜C4烷基，可被卤素原子或氰基取代的C1〜C4烷氧基; X表示氰基，硝基，卤素原子，可被取代的羟基亚氨基或可被取代的杂芳基; Y表示可以被取代的杂芳基，可以被取代的芳基，可以被取代的炔基，烯基，烷基，任选取代的饱和或不饱和的4-至8-元胺环，环胺化合物是 单环化合物，双环化合物或螺环化合物; l为1〜3的整数， 条件是其中l为1或2的情况，X为氰基，硝基或氯原子，R1为氯原子，R2为甲氧基，Y为被5或6成员取代的胺环 不包括羟基。