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    • 26. 发明申请
    • Compounds Having CRTH2 Antagonist Activity
    • 具有CRTH2拮抗作用的化合物
    • US20100022613A1
    • 2010-01-28
    • US12357792
    • 2009-01-22
    • Richard Edward ArmerGraham Michael Wynne
    • Richard Edward ArmerGraham Michael Wynne
    • A61K31/405C07D209/04
    • C07D209/10
    • Compounds of general formula (I) W is chloro or fluoro; Z is a —SO2YR1 group wherein R1 is C3-C8 heterocyclyl, aryl or heteroaryl any of which may optionally be substituted with one or more substituents selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, and —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; Y is a straight or branched C1-C4 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。