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    • 5. 发明申请
    • COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY
    • 具有CRTH2拮抗剂活性的化合物
    • WO2009093026A1
    • 2009-07-30
    • PCT/GB2009/000171
    • 2009-01-22
    • OXAGEN LIMITEDARMER, Richard, EdwardWYNNE, Graham, Michael
    • ARMER, Richard, EdwardWYNNE, Graham, Michael
    • C07D209/10A61K31/404A61P11/06A61P17/06
    • C07D209/10
    • Compounds of general formula (I) W is chloro or fluoro; Z is a -SO 2 YR 1 group wherein R 1 is C 3 -C 8 heterocyclyl, aryl or heteroaryl any of which may optionally be substituted with one or more substituents selected from halo, -CN, -C 1 -C 6 alkyl, -SOR 3 , -SO 2 R 3 , -SO 2 N(R 2 ) 2 , -N(R 2 ) 2 , -NR 2 C(O)R 3 , -CO 2 R 2 , -CONR 2 R 3 , -NO 2 , -OR 2 , -SR 2 , -O(CH 2 ) P OR 2 , and -O(CH 2 ) p O(CH 2 ) q OR 2 wherein each R 2 is independently hydrogen, -C 1 -C 6 alkyl, -C 3 -C 8 cycloalkyl, aryl or heteroaryl; each R 3 is independently, -C 1 -C 6 alkyl, -C 3 -C 8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; Y is a straight or branched C 1 -C 4 alkylene chain; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    • 通式(I)的化合物W是氯或氟; Z是-SO 2 YR1基团,其中R 1是C 3 -C 8杂环基,芳基或杂芳基,其中任何一个可以任选被一个或多个选自卤素,-CN,-C 1 -C 6烷基,-SOR 3,-SO 2 R 3,-SO 2 N (R 2)2,-N(R 2)2,-NR 2 C(O)R 3,-CO 2 R 2,-CONR 2 R 3,-NO 2,-OR 2,-SR 2,-O(CH 2)POR 2和-O(CH 2) )qOR 2,其中每个R 2独立地是氢,-C 1 -C 6烷基,-C 3 -C 8环烷基,芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基,-C 3 -C 8环烷基,芳基或杂芳基; p和q各自独立地为1至3的整数; Y是直链或支链C 1 -C 4亚烷基链; 其药学上可接受的盐,水合物,溶剂合物,复合物或前药可用于口服给药的组合物中,用于治疗过敏性疾病如哮喘,过敏性鼻炎和特应性皮炎。