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    Imidazole derivatives
    2.
    发明授权
    Imidazole derivatives 失效
    咪唑衍生物

    公开(公告)号：US06288061B1

    公开(公告)日：2001-09-11

    申请号：US09598216

    申请日：2000-06-21

    申请人： Hiroyuki Sueoka ,  Jouji Yasuoka ,  Akira Nishiyama ,  Masatoshi Kiuchi ,  Katsuya Yamamoto ,  Kunio Sugahara ,  Syuji Ehara ,  Kei Sakata

    发明人： Hiroyuki Sueoka ,  Jouji Yasuoka ,  Akira Nishiyama ,  Masatoshi Kiuchi ,  Katsuya Yamamoto ,  Kunio Sugahara ,  Syuji Ehara ,  Kei Sakata

    IPC分类号： A61K314178

    CPC分类号： C07D401/04 ,  C07D233/66 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14

    摘要： 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.

    摘要翻译： 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。

    Purine derivative and pharmaceutical composition
    4.
    发明授权
    Purine derivative and pharmaceutical composition 失效
    嘌呤衍生物和药物组合物

    公开(公告)号：US4728644A

    公开(公告)日：1988-03-01

    申请号：US768535

    申请日：1985-07-22

    申请人： Hiroshi Yuki ,  Hiroyuki Sueoka ,  Mitsuyoshi Yasumoto ,  Michio Terasawa ,  Tomonori Imayoshi

    发明人： Hiroshi Yuki ,  Hiroyuki Sueoka ,  Mitsuyoshi Yasumoto ,  Michio Terasawa ,  Tomonori Imayoshi

    IPC分类号： A61K31/52 ,  A61P25/04 ,  A61P29/00 ,  C07D473/34 ,  C07D473/04

    CPC分类号： C07D473/34

    摘要： Purine derivatives of the formula: ##STR1## wherein R is hydrogen, alkyl or phenyl which may be substituted by at least one halogen, lower alkyl or lower alkoxy; each of R.sup.1 and R.sup.2 is hydrogen, alkyl, cycloalkyl, hydroxyalkyl, dialkylaminoalkyl, cyclic aminoalkyl, alkenyl or aralkyl, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom form a heterocycle; and each of R.sup.3 and R.sup.4 is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof and/or hydrates, methods of preparing said compounds and pharmaceutical compositions containing said compounds. The purine compounds exhibit antiinflammatory, analgesic, antipyretic and antiallergic activity, and inhibitory activity on platelet aggregation, and are useful as drugs.

    摘要翻译： PCT No.PCT / JP84 / 00633 Sec。 371日期：1985年7月22日 102（e）日期1985年7月22日PCT提交1984年12月28日PCT公布。 第WO85 / 03077号公报 1985年7月18日。具有下式的嘌呤衍生物：其中R是氢，可被至少一个卤素，低级烷基或低级烷氧基取代的烷基或苯基; R 1和R 2各自为氢，烷基，环烷基，羟基烷基，二烷基氨基烷基，环状氨基烷基，烯基或芳烷基，或者R 1和R 2与相邻的氮原子一起形成杂环; 并且R 3和R 4各自为氢或低级烷基，及其药学上可接受的酸加成盐和/或水合物，制备所述化合物的方法和含有所述化合物的药物组合物。 嘌呤化合物具有抗炎，止痛，解热和抗过敏活性，对血小板聚集具有抑制活性，可用作药物。