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    • 9. 发明授权
    • Compounds having CRTH2 antagonist activity
    • 具有CRTH2拮抗活性的化合物
    • US07919512B2
    • 2011-04-05
    • US12828800
    • 2010-07-01
    • Richard Edward ArmerEric Roy PettipherMark WhittakerGraham Michael WynneJulia VileFrank Schroer
    • Richard Edward ArmerEric Roy PettipherMark WhittakerGraham Michael WynneJulia VileFrank Schroer
    • A61K31/44C07D401/00
    • A61K31/4439A61K31/47A61K45/06C07D401/06
    • Compounds of general formula (II) wherein W is chloro or fluoro; R1 is phenyl optionally 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, or —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; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; 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(II)的化合物,其中W是氯或氟; R 1是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或-O(CH 2)p O(CH 2)q OR 2,其中每个R 2独立地是氢,-C 1 -C 6烷基, C8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; 芳基,(CH2)mOC(= O)C1-C6烷基,((CH2)mO)nCH2CH2X,(CH2)mN(R5)2或CH ((CH 2)m O(C = O)R 6)2; m为1或2; n为1-4; X为OR 5或N(R 5)2; R5是氢或甲基; R6为C1-C18烷基; 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。