首页> 外国专利> 10 BETA, 11 BETA-CROSSLINKED STEROID, INTERMEDIATE, PRODUCTION THEREOF AND ANTI- GESTAGEN AND ANTI-GLUCOCORTICOIDE ATING DRUG CONTAINING THE SAME

10 BETA, 11 BETA-CROSSLINKED STEROID, INTERMEDIATE, PRODUCTION THEREOF AND ANTI- GESTAGEN AND ANTI-GLUCOCORTICOIDE ATING DRUG CONTAINING THE SAME

机译:10 BETA,11 BETA交联的甾体,中间体,其生产及其所含的抗雌激素和抗糖皮质激素老药

摘要

10 beta ,11 beta -bridged steroids of Formula I IMAGE (I) wherein R1 is H or methyl; R2 is H, a cyanide residue, a heteroaryl residue, a straight-chain or branched aliphatic, e.g., alkyl group of up to 20 carbon atoms, optionally exhibiting double or triple bonds and, if desired, being substituted by one or several oxo groups, a C4-7 cycloalkyl or C4-7 cycloalkenyl group, an OR3-, SR3-, -OSO2-R11- group wherein R11 means a perfluroinated C1-C4-alkyl group or an NR3R4-group wherein R3 means an H atom or C1-C8-alkyl residue, R4 means R3, a cyanide or a C1-C10-acyl residue, or R3 and R4 jointly with the inclusion of N means of 5- or 6-membered heterocyclic ring wherein the ring can additionally contain a further hetero atom N, O, or S, or a 4-cyano-, 4-methoxy- or 4-dimethylamino-substituted phenyl group, A and B either mean jointly a further bond between C4 and C5, or A is an alpha -hydroxy group and B is H, X is a keto or oxime group, and Z is a pentagonal or hexagonal ring residue which is optionally substituted and optionally unsaturated, or pharmaceutically compatible acid additional salts thereof which possess antigestagen and antiglucocorticoid properties.
机译:10个式I (I)的β,11β-桥接的类固醇,其中R 1为H或甲基; R 2是H,氰化物残基,杂芳基残基,直链或支链脂族基,例如至多20个碳原子的烷基,任选地表现出双键或三键,并且如果需要,被一个或多个氧代基团取代,C4-7环烷基或C4-7环烯基,OR3-,SR3-,-OSO2-R11-基团,其中R11表示全氟化的C1-C4-烷基或NR3R4-基团,其中R3表示H原子或C1 -C 8烷基残基,R 4表示R 3,氰化物或C 1 -C 10酰基残基,或R 3和R 4结合N表示5或6元杂环,其中该环可以另外包含另外的杂原子原子N,O或S或4-氰基,4-甲氧基或4-二甲基氨基取代的苯基,A和B共同表示C4和C5之间的另一个键,或者A为α-羟基并且B是H,X是酮基或肟基,并且Z是五角或六环残基,其任选地被取代并且任选地是不饱和的,或者是药学上相容的酸具有抗孕激素和抗糖皮质激素性质的其另外的盐。

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