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    • 4. 发明公开
    • USE OF VITAMIN D-DERIVATIVES IN THE TREATMENT OF OSTEOPOROSIS AND RELATED BONE DISORDERS, AS WELL AS NOVEL VITAMIN D3-DERIVATIVES
    • 维生素D衍生物在骨质疏松症和相关的骨疾病的治疗,随着新的维生素D3衍生物
    • EP1255732A1
    • 2002-11-13
    • EP01948978.0
    • 2001-01-31
    • Leo Pharma A/S
    • GRUE-SORENSEN, GunnarPEDERSEN, HenrikBINDERUP, Ernst, TorndalTRANHOLM, Mikael
    • C07C401/00A61K31/593A61P19/10
    • A61K31/593A61K31/59C07C401/00C07C2601/14C07C2602/24
    • Compounds of the formula (I) wherein X represents hydrogen or hydroxy; Y represents oxygen or sulphur or oxidized sulphur selected from the groups S(O) and S(O2); R?1 and R2¿, which may be the same or different, represent hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated, C¿1?-C6-hydrocarbon; or R?1 and R2, together with the carbon atom to which they are attached (marked with an asterisk in formula (I)), bearing the group X, form a C3-C8 carbocyclic ring; Q represents a diradical residue after removal of 2 hydrogen atoms from a straight, branched or cyclic, saturated or unsaturated C1-C8-hydrocarbon; R?3¿ represents hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated C¿1?-C6-hydrocarbon; R?1, R2¿ and/or Q is optionally substituted with one or more deuterium or fluorine atoms; and n is 0 or 1; and derivatives of the compounds of formula (I) in which one or more hydroxy groups have been transformed into -O-acyl or -O-glycosyl groups, or a phosphate ester, such masked groups being hydrolyzable in vivo; may be used for the preparation of a medicament for the treatment and/or prophylaxis of osteoporosis and related bone disorders.
    • 式I worin X darstellt氢或羟基的化合物; ÿdarstellt氧或硫或者选自基团S(O)和S(O 2 )选择氧化的硫; [R 1 和R 2 ,其可以是相同或不同,代表氢或选自直链,支链或环状,饱和或不饱和除去一个氢原子后的残基 ,C 1 -C 6 - 烃; 或R 1 和R 2 ,连同它们所连接的碳原子(标有上式中星号I)带有基团X,形成C < SUB> 3 -C 8 碳环; Q darstellt双基残基,从直链,支链或环状,饱和或不饱和的C 除去2个氢原子后1 -C 8 - 烃; 且R 3 darstellt氢或选自直链,支链或环状,饱和或不饱和的C 1 -C 6 - 烃; 可用于制备用于治疗和/或预防骨质疏松症和相关骨疾病的药物的制备。