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    • 1. 发明申请
    • 9, 10-SECOPREGNANE DERIVATIVE AND PHARMACEUTICAL
    • 9,10-SECOPREGNANE DERIVATIVE AND PHARMACEUTICAL
    • US20100016263A1
    • 2010-01-21
    • US12302975
    • 2007-06-01
    • Hiroki FujiedaHironori OtsuShoji YasufukuMasaaki Shirai
    • Hiroki FujiedaHironori OtsuShoji YasufukuMasaaki Shirai
    • A61K31/593C07C401/00A61P17/00
    • C07C401/00
    • A main object of the invention is to provide a novel useful vitamin D3 derivative, which has an excellent vitamin D3 activity and, as compared with conventional vitamin D3 derivatives, has a relatively small amount of influence on the systemic calcium metabolism. The invention includes a 9,10-secopregnane derivative of the following general formula [1] and a pharmaceutical composition containing it as active ingredient. In the general formula [1], the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Y is a single bond, an alkylene, an alkenylene or phenylene; R1 and R2 are the same or different, each represents hydrogen, an alkyl or a cycloalkyl; or R1 and R2, taken together with the adjacent carbon atom, form a cycloalkyl; R3 is hydrogen or methyl; Z is hydrogen, hydroxy or —NR11R12.
    • 本发明的主要目的是提供一种具有优异维生素D3活性的新型有用的维生素D3衍生物,与常规维生素D3衍生物相比,对全身钙代谢的影响相对较小。 本发明包括以下通式[1]的9,10-仲孕烷衍生物和含有它作为活性成分的药物组合物。 在通式[1]中,16位和17位之间的以下部分结构是指单键或双键:Y为单键,亚烷基,亚烯基或亚苯基; R1和R2相同或不同,各自表示氢,烷基或环烷基; 或R 1和R 2与相邻碳原子一起形成环烷基; R3是氢或甲基; Z是氢,羟基或-NR 11 R 12。
    • 2. 发明授权
    • 9, 10-secopregnane derivative and pharmaceutical
    • 9,10-孕代衍生物和药物
    • US08796246B2
    • 2014-08-05
    • US12302975
    • 2007-06-01
    • Hiroki FujiedaHironori OtsuShoji YasufukuMasaaki Shirai
    • Hiroki FujiedaHironori OtsuShoji YasufukuMasaaki Shirai
    • A61K31/593C07C401/00
    • C07C401/00
    • A main object of the invention is to provide a novel useful vitamin D3 derivative, which has an excellent vitamin D3 activity and, as compared with conventional vitamin D3 derivatives, has a relatively small amount of influence on the systemic calcium metabolism. The invention includes a 9,10-secopregnane derivative of the following general formula [1] and a pharmaceutical composition containing it as active ingredient. In the general formula [1], the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Y is a single bond, an alkylene, an alkenylene or phenylene; R1 and R2 are the same or different, each represents hydrogen, an alkyl or a cycloalkyl; or R1 and R2, taken together with the adjacent carbon atom, form a cycloalkyl; R3 is hydrogen or methyl; Z is hydrogen, hydroxy or —NR11R12.
    • 本发明的主要目的是提供一种具有优异维生素D3活性的新型有用的维生素D3衍生物,与常规维生素D3衍生物相比,对全身钙代谢的影响相对较小。 本发明包括以下通式[1]的9,10-仲孕烷衍生物和含有它作为活性成分的药物组合物。 在通式[1]中,16位和17位之间的以下部分结构是指单键或双键:Y为单键,亚烷基,亚烯基或亚苯基; R1和R2相同或不同,各自表示氢,烷基或环烷基; 或R 1和R 2与相邻碳原子一起形成环烷基; R3是氢或甲基; Z是氢,羟基或-NR 11 R 12。