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    Vitamin D.sub.3 derivative and treating agent for inflammatory respiratory disease using same
    1.
    发明授权
    Vitamin D.sub.3 derivative and treating agent for inflammatory respiratory disease using same 失效
    维生素D3衍生物和用于炎性呼吸系统疾病的治疗剂

    公开(公告)号：US6028208A

    公开(公告)日：2000-02-22

    申请号：US242665

    申请日：1999-02-22

    申请人： Qingzhi Gao ,  Kenji Manabe ,  Minoru Furuya ,  Manabu Chokki ,  Hiroaki Mitsuhashi ,  Seiichi Ishizuka ,  Tadashi Kishimoto ,  Masayasu Tabe ,  Yasuji Sakuma ,  Atsuo Hazato ,  Hiroko Tanaka

    发明人： Qingzhi Gao ,  Kenji Manabe ,  Minoru Furuya ,  Manabu Chokki ,  Hiroaki Mitsuhashi ,  Seiichi Ishizuka ,  Tadashi Kishimoto ,  Masayasu Tabe ,  Yasuji Sakuma ,  Atsuo Hazato ,  Hiroko Tanaka

    IPC分类号： C07C401/00 ,  A61K31/59

    CPC分类号： C07C401/00

    摘要： Provided are vitamin D.sub.3 derivatives expressed by the following general formula [1] ##STR1## [wherein, R.sub.1 and R.sub.2 are each a hydrogen atom, a trialkylsilyl group, an acetyl group, a methoxymethyl group, or a tetrahydropyranyl group; R.sub.3 and R.sub.4 are each a hydrogen atom, a hydroxyl group, an acyloxy group, an alkyloxy group, an alkylthio group or an alkyl group which is optionally substituted; R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each a hydrogen atom, a hydroxyl group, an alkyl group or an acyloxy group; R.sub.9 is a hydrogen atom, a hydroxyl group, an alkyl group or an alkylthio group; R.sub.10 is a hydrogen atom, an alkyl group or an alkyloxy group; A and B are each a hydrogen atom, a hydroxyl group, or together express a single bond; X and Y express a carbonyl oxygen, or one of them is a hydrogen atom and the other is a hydroxyl group or an acyloxy group; n is an integer of 0 to 2; m is an integer of 0 to 2], and a method for manufacturing the derivatives.The compounds can be sued as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension, alopecia, acne, psoriasis and dermatitis.

    摘要翻译： PCT No.PCT / JP98 / 02813 Sec。 一九九九年二月二十二日 102（e）1999年2月22日PCT提交1998年6月24日PCT公布。 公开号WO98 / 58909 日期：1998年12月30日提供由以下通式[1]表示的维生素D3衍生物[其中，R1和R2各自为氢原子，三烷基甲硅烷基，乙酰基，甲氧基甲基或四氢吡喃基; R3和R4各自为氢原子，羟基，酰氧基，烷氧基，烷硫基或任选取代的烷基; R5，R6，R7和R8分别是氢原子，羟基，烷基或酰氧基; R9为氢原子，羟基，烷基或烷硫基; R 10是氢原子，烷基或烷氧基; A和B各自为氢原子，羟基，或一起表示单键; X和Y表示羰基氧，或者其中一个是氢原子，另一个是羟基或酰氧基; n为0〜2的整数， m为0〜2的整数]，以及该衍生物的制造方法。 这些化合物可以作为炎性呼吸系统疾病，恶性肿瘤，类风湿性关节炎，骨质疏松症，糖尿病，高血压，脱发，痤疮，牛皮癣和皮炎的治疗剂的活性成分。

    Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient
    2.
    发明授权
    Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient 失效
    熔融嘧啶衍生物，其制备方法和包含与活性成分相同的药物制剂

    公开(公告)号：US5378700A

    公开(公告)日：1995-01-03

    申请号：US839769

    申请日：1992-06-09

    申请人： Yasuji Sakuma ,  Masaichi Hasegawa ,  Kenichiro Kataoka ,  Kenji Hoshina ,  Noboru Yamazaki ,  Takashi Kadota ,  Hisao Yamaguchi

    发明人： Yasuji Sakuma ,  Masaichi Hasegawa ,  Kenichiro Kataoka ,  Kenji Hoshina ,  Noboru Yamazaki ,  Takashi Kadota ,  Hisao Yamaguchi

    IPC分类号： A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Disclosed is a fused pyrimidine of the formula [I] ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined in the specification, Y represents a linking group of the formula ##STR2## wherein n is an integer of from 4 to 6, ##STR3## wherein A is a hydrogen atom or alkyl group; and Z represents a hydrogen atom, or other substituents; or Y and Z together represent an unsubstituted or substituted alkyl, alkenyl or arylalkyl group; or a 5- to 7-member heterocyclic ring which has a nitrogen atom, and further, an oxygen or sulfur atom as a hetero atom other than the nitrogen atom, being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I), a 5- to 7-member unsaturated heterocyclic ring which has 1 to 3 nitrogen atoms being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I), or a fused biheterocyclic ring constructed with 5- or 6-membered aromatic or non-aromatic rings, which has 1 to 3 nitrogen atoms in any position, being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I); andm is an integer of from 1 to 3;and a pharmaceutically acceptable acid addition salt thereof, as well as a process for producing same and a pharmaceutical preparation useful for a treatment of hypoxemia associated with respiratory diseases.

    摘要翻译： PCT No.PCT / JP90 / 01313 Sec。 371日期：1992年6月9日 102（e）日期1992年6月9日PCT提交1990年10月11日PCT公布。 出版物WO91 / 05784 日期：1991年5月2日。公开是式[I]的融合嘧啶其中R 1，R 2和R 3如说明书中所定义，Y表示式的连接基团，其中n 是4至6的整数，其中A是氢原子或烷基; O（S） Z表示氢原子或其它取代基; 或Y和Z一起表示未取代或取代的烷基，烯基或芳基烷基; 或具有氮原子的5-至7-元杂环，以及作为氮原子以外的杂原子的氧或硫原子通过氮原子键合到嘧啶环的4-位上 式（I）的通式（I）中的氮原子数为1〜3的5〜7元不饱和杂环与式（I）的嘧啶环的4-位连接， 在其中具有1至3个氮原子的5-或6-元芳族或非芳族环经由其中的氮原子键合到式（I）的嘧啶环的4-位上构成的双杂环， ; m为1〜3的整数， 和其药学上可接受的酸加成盐，以及其制备方法和用于治疗与呼吸系统疾病相关的低氧血症的药物制剂。