首页> 外国专利> 17-(C(CH3) (CH2) O-3C (R4, R5) N (R6, R7))-SUBSTITUTED 19-NOR-PREGNA-1, 3, 5(10)-TRIENE DERIVATIVES AND THEIR MEDICAL USE

17-(C(CH3) (CH2) O-3C (R4, R5) N (R6, R7))-SUBSTITUTED 19-NOR-PREGNA-1, 3, 5(10)-TRIENE DERIVATIVES AND THEIR MEDICAL USE

机译:17-(C(CH3)(CH2)O-3C(R4,R5)N(R6,R7))取代的19-NOR-PREGNA-1、3、5(10)-三烯衍生物及其医疗用途

摘要

Compounds of formula (I) in which: R1 represents a hydrogen atom or an o-protecting group; R2 represents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; R3 represents a methyl group having α- or β- configuration; X represents a C¿1-3? alkylene group or a valence bond; Y represents a group of formula -C(R?4) (R5)NR6R7¿ where R?4 and R5¿, which may be the same or different, are each selected from hydrogen atoms, alkyl, alkenyl and alkynyl groups such that the total carbon content of R?4 and R5¿ does not exceed three atoms; R6 represents a hydrogen atom, an aliphatic or araliphatic organic group, or an acyl group comprising an aliphatic, araliphatic or aryl organic group linked to the nitrogen atom by way of a carbonyl group; and R7 is a hydrogen atom or a lower alkyl group; and the dotted line signifies that a double bond may optionally be present at the 16(17)-position exhibit potent cell modulating activity, including antiproliferative and antiangiogenic effects.
机译:式(I)的化合物,其中:R 1代表氢原子或o-保护基; R 2代表羟基,低级烷氧基,羧醛,低级烷-1-烯基或羟基或低级烷氧基取代的低级烷基; R3代表具有α-或β-构型的甲基; X代表C?1-3?亚烷基或价键; Y代表式-C(R 4)(R 5)NR 6 R 7的基团,其中R 4和R 5可以相同或不同,各自选自氢原子,烷基,烯基和炔基,使得R 4和R 5的总碳含量不超过三个原子; R6代表氢原子,脂族或芳脂族有机基团,或包含通过羰基与氮原子相连的脂族,芳脂族或芳基有机基团的酰基; R 7为氢原子或低级烷基。虚线表示在16(17)-位可能任选存在双键,表现出有效的细胞调节活性,包括抗增殖和抗血管生成作用。

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