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23-IN-VITAMIN D3 DERIVATIVE
专利权人:
TEJDZIN FARMA LIMITED
发明人:
SAITO Khirosi (JP),САИТО Хироси (JP),KOMIJaMA Masato (JP),КОМИЯМА Масато (JP),OTIAI Ehjdzi (JP),ОТИАИ Эйдзи (JP),TAKAGI Kenikhiro (JP),ТАКАГИ Кенихиро (JP),TIDA Takajuki (JP),ТИДА Такаюки (JP),FUDZITA
申请号:
RU2013124033/04
公开号:
RU0002558362C2
申请日:
2011.10.24
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to novel derivative of vitamin D3, suitable as therapeutic means against osteoporosis, presented by formula (1) (2), where R1 represents hydrogen atom, alkyl group with 1-6 carbon atoms, alkylcarbonyloxyalkyl group, and each alkyl has 1-6 carbon atoms, or arylcarbonyloxyalkyl group, and aryl has 6-10 carbon atoms and alkyl has 1-6 carbon atoms or together with other R2 and carbon atom, which they are bound to, can form cyclic alkyl group with 3-6 carbon atoms; R3 represents alkyl group with 1-6 carbon atoms or together with other R3 and carbon atom, which they are bound to, can form cyclic alkyl group with 3-6 carbon atoms; X represents oxygen atom or methylene group; and n is equal to integer number 1 or 2.EFFECT: invention relates to pharmaceutical composition, possessing affinity to vitamin D receptor (VDR), which contains compound of formula (1); as well as relates to intermediate compound, represented by formula (2), in which R2, X and n are such, as given above, R4 represents R1 in formula (1), methoxymethyl group, methoxyethoxymethyl group, tetrahydrofuranyl group, tetrahydropyranyl group or benzyloxymethyl group; and R5 represents protective group for hydroxyl group, selected from the group, which includes methoxymethyl group, acyl group with 1-3 carbon atoms (mentioned number of carbon atoms includes carbonyl carbon), trimethylsilyl group, triethylsilyl group, tret-butyldimethylsilyl group and tret-butyldiphenylsilyl group.12 cl, 4 tbl, 14 exИзобретение относится к новому производному витамина D3, применимому в качестве терапевтического средства против остеопороза, которое представлено формулой (1), где R1 представляет собой атом водорода, алкильную группу с 1-6 атомами углерода, алкилкарбонилоксиалкильную группу, причем каждый алкил имеет 1-6 атомов углерода, или арилкарбонилоксиалкильную группу, причем арил имеет 6-10 атомов углерода и алкил имеет 1-6 атомов углерода; R2 представляет собой ат
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