发明公开
EP0214732A2 (Substituted benzyl)-thio heterocyclic compounds having a leukotriene-antagonist activity
失效
（取代苄基） - 硫代杂环维生素，死亡白细胞素拮抗剂 - 维尔京。
- 专利标题： (Substituted benzyl)-thio heterocyclic compounds having a leukotriene-antagonist activity
- 专利标题（中）： （取代苄基） - 硫代杂环维生素，死亡白细胞素拮抗剂 - 维尔京。
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申请号： EP86305633.9申请日： 1986-07-22
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公开(公告)号： EP0214732A2公开(公告)日： 1987-03-18
- 发明人: Mase, Toshiyasu , Murase, Kiyoshi , Tsuzuki, Ryuji , Tomioka, Kenichi , Hara, Hiromu
- 申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
- 申请人地址： No. 3-11 Nihonbashi-Honcho, 2-chome Chuo-ku Tokyo JP
- 专利权人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
- 当前专利权人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
- 当前专利权人地址： No. 3-11 Nihonbashi-Honcho, 2-chome Chuo-ku Tokyo JP
- 代理机构： Geering, Keith Edwin
- 优先权： JP164267/85 19850722; JP224197/85 19851007; JP297097/85 19851226
- 主分类号： C07D285/12
- IPC分类号： C07D285/12 ; C07D239/56 ; C07D213/70 ; C07D249/12 ; C07D275/02 ; A61K31/41 ; A61K31/44 ; A61K31/505
摘要：
Heterocyclic compound of formula (I) and salts thereof are SRS-A antagonists:
wherein R' is a C 1 to C 8 acyl group; R 2 is a C 1 to C a alkyl group; Het- is a 5- or 6-membered heterocyclic ring which contains 1 to 3 nitrogen atoms and may additionally contain a sulfur atom or an oxygen atom; R 3 is a carboxy group, an amino group, a C 1 to C 8 alkylamino group which may be carboxy-substituted, a C, to C 8 alkanoylamino group which may be carboxy-substituted, a di-(C 1 -C 8 alkyl) amino group, a hydroxy group, a C 1 to C 8 alkoxy group which may be carboxy-substituted, a mercapto group, a C 1 -C 8 alkylthio group which may be carboxy-substituted, a group of formula:
or formula:
(wherein p is integer of 1 to 5, q is 0, 1 or 2, r is an integer of 1 to 5; R 4 is a carboxy group, a C 1 -C 8 alkoxy group which may be carboxy-substituted or a C 1 -C 8 alkyl group which may be carboxy-substituted and optionally additionally contain a sulfur atom or an oxygen atom in the carbon chain thereof); and n is 0 or an integer of to 3; provided that when the compound is substituted by a carboxy group, said carboxy group may be in the form of an ester, and when n is 2 or 3 different R 3 's is may be present.
wherein R' is a C 1 to C 8 acyl group; R 2 is a C 1 to C a alkyl group; Het- is a 5- or 6-membered heterocyclic ring which contains 1 to 3 nitrogen atoms and may additionally contain a sulfur atom or an oxygen atom; R 3 is a carboxy group, an amino group, a C 1 to C 8 alkylamino group which may be carboxy-substituted, a C, to C 8 alkanoylamino group which may be carboxy-substituted, a di-(C 1 -C 8 alkyl) amino group, a hydroxy group, a C 1 to C 8 alkoxy group which may be carboxy-substituted, a mercapto group, a C 1 -C 8 alkylthio group which may be carboxy-substituted, a group of formula:
or formula:
(wherein p is integer of 1 to 5, q is 0, 1 or 2, r is an integer of 1 to 5; R 4 is a carboxy group, a C 1 -C 8 alkoxy group which may be carboxy-substituted or a C 1 -C 8 alkyl group which may be carboxy-substituted and optionally additionally contain a sulfur atom or an oxygen atom in the carbon chain thereof); and n is 0 or an integer of to 3; provided that when the compound is substituted by a carboxy group, said carboxy group may be in the form of an ester, and when n is 2 or 3 different R 3 's is may be present.
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