公开(公告)号：US6028208A

公开(公告)日：2000-02-22

申请号：US242665

申请日：1999-02-22

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

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

IPC: C07C401/00 ,  A61K31/59

CPC classification number: C07C401/00

Abstract: 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.

Abstract translation: 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。