Novel vitamin D. analogues
本发明涉及式(I)化合物,其中X为氢或羟基或保护羟基;R#+[1]和R#+[2]代表氢,甲基或乙基,或者,R#+[1]和R#+[2]可以与带有基团X的碳原子形成C#-[3]-C#-[5]碳环;Q为C#-[3]-C#-[6]亚烃基,亚烃基表示从直链或支链,饱和或不饱和烃基上移去两个氢原子后得到的基团,其中任何一个CH#-[2]基团可以任意地被氧原子或羰基基团所取代,因此与C-20碳原子直接相连的碳原子(C-22)为sp#+[2]或sp#+[3]杂化的碳原子,即与2或3个其它原子相连;并且其中另一个CH#-[2]基团可以被亚苯基取代,其中Q可以任意地被一或多个羟基或C#-[1]-C#-[4]烷氧基...
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Zusammenfassung: | 本发明涉及式(I)化合物,其中X为氢或羟基或保护羟基;R#+[1]和R#+[2]代表氢,甲基或乙基,或者,R#+[1]和R#+[2]可以与带有基团X的碳原子形成C#-[3]-C#-[5]碳环;Q为C#-[3]-C#-[6]亚烃基,亚烃基表示从直链或支链,饱和或不饱和烃基上移去两个氢原子后得到的基团,其中任何一个CH#-[2]基团可以任意地被氧原子或羰基基团所取代,因此与C-20碳原子直接相连的碳原子(C-22)为sp#+[2]或sp#+[3]杂化的碳原子,即与2或3个其它原子相连;并且其中另一个CH#-[2]基团可以被亚苯基取代,其中Q可以任意地被一或多个羟基或C#-[1]-C#-[4]烷氧基团取代。已发现这些化合物具有异常高的免疫抑制活性及很高的肿瘤细胞增殖抑制活性。∴
The present invention relates to compounds of formula (I), in which formula X is hydrogen or hydroxy or protected hydroxy; R1 an R2 stand for hydrogen, methyl or ethyl, or, when taken together with the carbon atom bearing the group X, R1 and R2 can form a C3-C5 carbocyclic ring; Q is a C3-C6 hydrocarbylene, hydrocarbylene indicating the diradical obtained after removal of 2 hydrogen atoms for a straight or banched, saturated or unsaturated hydrocarbon, in which one of any CH2 groups may optionally be replaced by an oxygen atom or a carbonyl group, such that the carbon atom (C-22) directly bonded to C-20 is an sp2 or sp3 hybridized carbon atom, i.e. bonded to 2 or 3 other atoms; and in which another of the CH2 groups may be replaced by phenylene, and where Q may optionally be substituted with one or more hydroxy or C1-C4-alkoxy groups. These compounds have been discovered to possess exceptionally high immunosuppressive activites together with high tumour cell proliferation inhibiting activities. |
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