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new pregn - 4 - a derivatives, process for preparation thereof and pharmaceutical preparations which contain these deriva - in.

机译:新的pregn-4-衍生物,其制备方法和含有这些衍生物的药物制剂。

摘要

Novel DELTA 4-pregnenes of the formula IMAGE I wherein X1 is selected from the group consisting of =O and IMAGE Y is selected from the group consisting of hydrogen and halogen, R1 is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, X2 is selected from the group consisting of hydrogen and -OH, R in the 16 alpha - or beta -position is selected from the group consisting of hydrogen, -OH and methyl, Z is selected from the group consisting of (1) -OH, (2) alkoxy of 1 to 12 carbon atoms, (3) cycloalkoxy of 3 to 12 carbon atoms, (4) acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms, (5) IMAGE wherein W is a hydrocarbon of 1 to 12 carbon atoms, (6) IMAGE wherein R2 is hydrogen or alkyl of 1 to 12 carbon atoms, (7) IMAGE wherein R3 is a hydrocarbon of 1 to 12 carbon atoms and (8) IMAGE the dotted line in the A ring indicates the optional presence of a double bond in the 1(2)-position and A and B are both hydrogen or A is methyl, chlorine or fluorine while B is hydrogen or A and B may form a double bond in the 6(7)-position with the proviso that if the A ring has a 1(2) double bond, A is hydrogen or fluorine, B is hydrogen, Y is hydrogen or fluorine, X2 is hydrogen or -OH, R is methyl and Z is not -OH having a very marked antiallergic activity with a reduced anti-inflammatory activity and a process for their preparation.
机译: I的新型DELTA 4-孕烯,其中X1选自= O, Y选自氢和卤素,R1选自氢和酰基在1至18个碳原子的有机羧酸中,X 2选自由氢和-OH组成的组,在16个α-或β-位置的R选自由氢,-OH和甲基组成的组,Z选自(1)-OH,(2)具有1至12个碳原子的烷氧基,(3)具有3至12个碳原子的环烷氧基,(4)具有1至18个碳原子的有机羧酸的酰氧基,(5),其中W是1至12个碳原子的烃,(6),其中R2是氢或1至12个碳原子的烷基,(7),其中R3是1至12个碳原子和A环中的(8)虚线表示在1(2)-位和A和B均为氢或A为甲基,氯或氟,而B为氢或A和B可以在6(7)位形成双键,条件是如果A环具有1(2)双键,A为氢或氟,B为氢,Y为氢或氟,X 2为氢或-OH,R为甲基且Z不是-OH,具有非常显着的抗过敏活性,且抗炎活性降低,其方法为他们的准备。

著录项

  • 公开/公告号NL7804840A

    专利类型

  • 公开/公告日1978-11-08

    原文格式PDF

  • 申请/专利权人 ROUSSEL-UCLAF S.A. TE PARIJS.;

    申请/专利号NL19780004840

  • 发明设计人

    申请日1978-05-05

  • 分类号C07J7/00;

  • 国家 NL

  • 入库时间 2022-08-22 22:45:35

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