Vitamin D.sub.3 derivative and treating agent for inflammatory
respiratory disease using same
    7.
    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

    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。

    Vitamin d3 derivatives and remedies using the same
    10.
    发明申请
    Vitamin d3 derivatives and remedies using the same 审中-公开
    维生素d3衍生物及其使用方法

    公开(公告)号:US20050101575A1

    公开(公告)日:2005-05-12

    申请号:US10503388

    申请日:2003-02-19

    CPC分类号: C07D307/58

    摘要: A vitamin D3 derivative expressed by the following general formula (1) [wherein, R is a hydrogen atom or a methyl group, and A is a single bond, —CH2—, —CH═CH—, —CH2—CH═CH—, —CH═CH—CH═CH—, —C≡C— or —CH2—C≡C—; and a compound in which R is an hydrogen atom, A is —CH2—, the steric configuration at the 1-position is (S)-configuration, and the steric configuration at the 3-position is (R)-configuration is excluded] or a pharmaceutically permissible solvate thereof. The compound can be an effective ingredient of a treating agent for osteoporosis, malignant tumor, psoriasis, hyperparathyroidism, an inflammatory respiratory disease, rheumatoid arthritis, growth onset type diabetes mellitus, hypertension, alopecia, acne, dermatitis, hypercalcemia or Paget's disease of bone.

    摘要翻译: 由以下通式(1)表示的维生素D 3 N衍生物[其中,R是氢原子或甲基,A是单键,-CH 2 O / ,-CH-CH-,-CH 2 -CH-CH-,-CH-CH-CH-CH - , - C≡C-或-CH 2 >-C≡C-; 和其中R为氢原子的化合物,A为-CH 2 - ,1位的空间构型为(S)构型,3位的空间构型为 (R) - 构型]或其药学上可允许的溶剂化物。 该化合物可以是骨质疏松症,恶性肿瘤,牛皮癣,甲状旁腺功能亢进,炎性呼吸系统疾病,类风湿性关节炎,生长发病型糖尿病,高血压,脱发,痤疮,皮炎,高钙血症或佩吉特氏病的治疗剂的有效成分。