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1. 发明公开

EP0123541A1 Leukotriene antagonists 有权
标题翻译： Leukotrienantagonisten。
公开(公告)号：EP0123541A1
公开(公告)日：1984-10-31
申请号：EP84302718.6
申请日：1984-04-19
申请人： MERCK FROSST CANADA INC.
发明人： Belanger, Patrice , Guindon, Yvan , Fortin, Rejean , Yaokim, Christiane , Rokach, Joshua
IPC分类号： C07C59/90 , C07C51/347 , C07C149/40 , C07C147/107 , C07D317/14 , C07D233/78 , C07D207/44 , C07D303/02 , A61K31/19
CPC分类号： C07D285/10 , C07C45/71 , C07C49/84 , C07C49/86 , C07C59/90 , C07C255/00 , C07D257/04
摘要： Compounds of the formula:
and their pharmaceutically acceptable salts, which are novel, are antagonists of leukotrienes of C4, D4 and E., the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents and are made into pharmaceutical compositions.
In the formula, R, is a radical of formula COOR 3 , where R 3 is hydrogen or an alkyl or cycloalkyl group containing not more than six carbon atoms; CH 2 OH; CHO; CH 2 NHSO 2 R 4 , where R 4 is OH; C 1-6 alkyl, C 1-6 alkoxy phenyl, phenyl substituted by Ci-3 alkyl or Ci- 3 alkoxy, halogen, hydroxy, haloalkyl, COOH, CN, formyl, C 1-6 acyl or C 1-4 perfluoroalkyl; CN; or CON(R 5 ) 2 , where each R 5 , independently of the other, is H, OH or C 1-4 alkyl; a tetrazolyl radical, a monocyclic or bicyclic heterocyclic ring containing an acidic hydroxyl group; or a radical of formula
where each s, independently of the other, is 0,1, 2 or 3; R 7 is

(A) a monocyclic or bicyclic heterocyclic radical containing from 3 to 12 nuclear carbon atoms and 1 or 2 nuclear heteroatoms, one being N, and the other (if any) being N or S, each ring in the heterocyclic radical having 5 or 6 atoms, or
(B) a radical X-R 8 where X is O, S or NH and R 8 contains up to 21 carbon atoms and is (1) a hydrocarbon radical or (2) an acyl radical derived from an organic acyclic or monocyclic carboxylic acid containing not more than 1 heteroatom that is N, 0 or S in the ring; and each R 10 , independently of the other is H or Ci-4 alkyl;
R 6 is H or Ci-4 alkyl;
R 2 is a halogen atom; and
R 9 is a hydrogen atom or hydroxyl group.
摘要翻译：下式的化合物及其药物上可接受的盐是C4，D4和E4的白三烯拮抗剂，即过敏反应缓慢的物质。这些化合物可用作抗哮喘，抗过敏和抗炎剂并制成药物组合物。在该式中，R 1是式COOR 3的基团，其中R 3是氢或含有不超过6个碳原子的烷基或环烷基; CH2OH; CHO; CH2NHSO2R4，其中R4是OH; C 1-6烷基，C 1-6烷氧基苯基，被C 1-3烷基或C 1-3烷氧基取代的苯基，卤素，羟基，卤代烷基，COOH，CN，甲酰基，C 1-6酰基或C 1-4四氟烷基; CN; 或CON（R5）2，其中每个R5独立于H，OH或C1-4烷基; 四唑基，含有酸性@羟基的单环或双环杂环; 或式的基团，其中每个s独立于0,2,2或3; R2是（A）含有3至12个核碳原子和1或2个核杂原子的单环或双环杂环基，一个为N，另一个为N或S，杂环基中的每个环均为5 或6个原子，或（B）基团X-R8，其中X是O，S或NH和R8含有至多21个碳原子，并且是（1）烃基或（2）衍生自有机非环或在环中含有不多于1个N，O或S的杂原子的单环羧酸; 每个R 10独立地为H或C 1-4烷基; R6是H或C1-4烷基; R2是卤原子; R9为氢原子或羟基。

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