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    • 1. 发明授权
    • Imidazole derivatives
    • 咪唑衍生物
    • US06288061B1
    • 2001-09-11
    • US09598216
    • 2000-06-21
    • Hiroyuki SueokaJouji YasuokaAkira NishiyamaMasatoshi KiuchiKatsuya YamamotoKunio SugaharaSyuji EharaKei Sakata
    • Hiroyuki SueokaJouji YasuokaAkira NishiyamaMasatoshi KiuchiKatsuya YamamotoKunio SugaharaSyuji EharaKei Sakata
    • A61K314178
    • C07D401/04C07D233/66C07D403/12C07D417/12C07D417/14
    • The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof. The compounds of the formulas (I) and (XII) and pharmaceutically acceptable salts thereof of the present invention inhibit IL-4 and IL-5 production by Th2 cells and are effective for the prophylaxis and treatment of allergic diseases such as atopic dermatitis, bronchial asthma, allergic rhinitis and the like.
    • 本发明涉及下式(I)的咪唑衍生物,其中R 1是氢,任选取代的烷基等,R 2是氢,任选取代的烷基等,R 3是任选取代的杂芳基,R 4是任选取代的环烷基,任选地 取代的苯基等,条件是当R 1为氢时,R 2和R 4相同或不同,并且各自为苯基或被卤素原子取代的苯基,低级烷基或低级烷氧基,R 3为被苯基取代的苯并噻唑基或噻唑基,咪唑 下式(Ⅻ)的衍生物,其中R 6是任选取代的苯基或任选取代的杂芳基且R 7是取代的苯基,及其药学上可接受的盐。 本发明的式(I)和(XII)化合物及其药学上可接受的盐抑制Th2细胞的IL-4和IL-5产生,对预防和治疗变应性疾病如特应性皮炎,支气管 哮喘,过敏性鼻炎等。