发明名称 Prodrugs of vitamine K
摘要 The invention relates to prodrugs of vitamin K2, in particular prodrugs of MK-7 in which the diketone is converted to a monosubstituted or disubstituted ester type derivative. These compounds are shown to give MK-7 in plasma.
申请公布号 US9512153(B2) 申请公布日期 2016.12.06
申请号 US201314382225 申请日期 2013.03.04
申请人 KAPPA BIOSCIENCE AS 发明人 Moller Mona;Sandberg Marcel;Aukrust Inger Reidun
分类号 C07C69/16;C07C69/28;C07C69/40;C07C69/76;C07C69/78;C07F9/12;C07F9/09;C07C69/017;C07C69/34;C07C271/22 主分类号 C07C69/16
代理机构 Banner & Witcoff, Ltd. 代理人 Banner & Witcoff, Ltd.
主权项 1. A compound of formula (I) wherein one R is —SO2R4, —COOH, —COOC1-6alkyl, —CON(R2)2, COAr, —COC1-6 alkyl group; —CO(CH2)pCOOR3, CO(CH2)pCON(R2)2 or —CO(CHR6)pN(R5)2, wherein both R groups are not simultaneously COCH3;each R2 group is independently hydrogen or C1-6-alkyl;R3 is H, C1-6-alkyl, Ar, (CH2)pAr;R4 is OH, C1-6 alkyl, Ph, CF3, or tolyl;each R5 is H, an amino protecting group or C1-6 alkyl;each R6 is H or C1-6 alkyl;any C1-6-alkyl group is optionally substituted by one or more groups selected from —OR2, N(R2)2 or COOR2; each Ar is an optionally substituted phenyl or naphthyl group, said substitutent being a C1-6 alkyl CHalH2, CHal2H, CHal3, OH, OC1-6Alkyl, or COOR6;each p is 1 to 4; wherein the other R is a —COC2-6 alkyl group or COAr group where Ar is an optionally substituted phenyl or naphthyl group, said substitutent being a C1-6 alkyl CHalH2 , CHal2H, CHal3, OH, OC1-6-alkyl, or COOR6; and R6 is H or C1-6 alkyl; and n is 3 to 8; or a salt or solvate thereof.
地址 Oslo NO