发明公开
- 专利标题: Piperazine derivatives as Tachykinin antagonists
- 专利标题(中): Piperazinderivate als速激肽拮抗剂。
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申请号: EP94118542.3申请日: 1994-11-25
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公开(公告)号: EP0655442A1公开(公告)日: 1995-05-31
- 发明人: Matsuo, Masaaki , Hagiwara, Daijiro , Manabe, Takashi , Nobukiyo, Konishi , Shigenaga, Shinji , Murano, Kenji , Matsuda, Hiroshi , Miyake, Hiroshi
- 申请人: FUJISAWA PHARMACEUTICAL CO., LTD.
- 申请人地址: 4-7, Doshomachi 3-chome Chuo-ku Osaka-shi Osaka 541 JP
- 专利权人: FUJISAWA PHARMACEUTICAL CO., LTD.
- 当前专利权人: FUJISAWA PHARMACEUTICAL CO., LTD.
- 当前专利权人地址: 4-7, Doshomachi 3-chome Chuo-ku Osaka-shi Osaka 541 JP
- 代理机构: Türk, Gille, Hrabal, Leifert
- 优先权: GB9324479 19931129; GB9402010 19941102; GB9412708 19940624
- 主分类号: C07D241/04
- IPC分类号: C07D241/04 ; C07D403/06 ; C07D409/06 ; C07D401/04 ; C07D401/06 ; C07D405/06 ; C07D417/06 ; C07D401/14 ; C07D401/12 ; A61K31/495
摘要:
A compound of the following general formula :
wherein
X is carbonyl or sulfonyl;
Y is bond or lower alkylene;
R¹ is halogen, lower alkyl, halo(lower)alkyl, aryloxy, nitro or amino which may have 1 or 2 and same or different substituent(s) selected from lower alkyl, acyl and lower alkanesulfonyl;
R² is aryl or an aromatic hetero(mono- or bi-)cyclic group, and each of which may have 1, 2 or 3 suitable substituent(s);
R³ is hydrogen or lower alkyl;
R⁴ is
(i) a group of the formula -SO₂-R⁵ in which R⁵ is lower alkyl or aryl optionally substituted with lower alkyl or lower alkoxy,
(ii) a group of the formula
in which R⁶ is aryl optionally substituted with lower alkyl or lower alkoxy, or
(iii) a group of the formula -A-(Z) p in which
A is bond, lower alkylene, lower alkenylene or lower alkynylene,
Z is hydrogen, halogen, hydroxy, nitrile, amino, cyclo(lower)alkyl, aryl, aryloxy, acyl, acylamino, lower alkanesulfonylamino, arylsulfonylamino or an aromatic hetero(mono- or bi-)cyclic group, and each of the cyclic group may have 1, 2 or 3 suitable substituent(s), and
p is 1, 2 or 3; and
n is 0, 1 or 2;
provided that when n or p is more than 1, these R¹ and Z may be the same or different group respectively; or its pharmaceutically acceptable salt, processes for their preparation and pharmaceutical compositions comprising them.
wherein
X is carbonyl or sulfonyl;
Y is bond or lower alkylene;
R¹ is halogen, lower alkyl, halo(lower)alkyl, aryloxy, nitro or amino which may have 1 or 2 and same or different substituent(s) selected from lower alkyl, acyl and lower alkanesulfonyl;
R² is aryl or an aromatic hetero(mono- or bi-)cyclic group, and each of which may have 1, 2 or 3 suitable substituent(s);
R³ is hydrogen or lower alkyl;
R⁴ is
(i) a group of the formula -SO₂-R⁵ in which R⁵ is lower alkyl or aryl optionally substituted with lower alkyl or lower alkoxy,
(ii) a group of the formula
in which R⁶ is aryl optionally substituted with lower alkyl or lower alkoxy, or
(iii) a group of the formula -A-(Z) p in which
A is bond, lower alkylene, lower alkenylene or lower alkynylene,
Z is hydrogen, halogen, hydroxy, nitrile, amino, cyclo(lower)alkyl, aryl, aryloxy, acyl, acylamino, lower alkanesulfonylamino, arylsulfonylamino or an aromatic hetero(mono- or bi-)cyclic group, and each of the cyclic group may have 1, 2 or 3 suitable substituent(s), and
p is 1, 2 or 3; and
n is 0, 1 or 2;
provided that when n or p is more than 1, these R¹ and Z may be the same or different group respectively; or its pharmaceutically acceptable salt, processes for their preparation and pharmaceutical compositions comprising them.
公开/授权文献
- EP0655442B1 Piperazine derivatives as Tachykinin antagonists 公开/授权日:2001-05-23
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