发明名称 9, 10-secopregnane derivative and pharmaceutical
摘要 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.
申请公布号 US8796246(B2) 申请公布日期 2014.08.05
申请号 US200712302975 申请日期 2007.06.01
申请人 Nippon Shinyaku Co., Ltd. 发明人 Fujieda Hiroki;Otsu Hironori;Yasufuku Shoji;Shirai Masaaki
分类号 A61K31/593;C07C401/00 主分类号 A61K31/593
代理机构 McDermott Will & Emery LLP 代理人 McDermott Will & Emery LLP
主权项 1. A 9,10-secopregnane compound of formula [1]: wherein the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Z is hydroxy, Y is ethylene or ethenylene, R1 and R2 are the same or different, each is methyl, trifluoromethyl or ethyl, and R3 is methyl: Ra and Rb are both hydrogens, or Ra and Rb, taken together, form methylene; Rc and Rd are the same or different, and each represents hydrogen or methyl, or Re and Rd, taken together, form methylene: or a pharmaceutically acceptable salt thereof.
地址 Kyoto JP