首页> 外国专利> URETHANES DERIVED FROM AZACICLOALCANOS ITS ANALOGOS UNCLEAR AND SAID ITS PREPARATION AND ITS UTILIZATION AS INHIBITORS OF 2,3-EPOXYCYSKALENO-LANOSTEROL-CICLASE

URETHANES DERIVED FROM AZACICLOALCANOS ITS ANALOGOS UNCLEAR AND SAID ITS PREPARATION AND ITS UTILIZATION AS INHIBITORS OF 2,3-EPOXYCYSKALENO-LANOSTEROL-CICLASE

机译:从杜鹃花中提取的尿素,其ANALOGOs不明确和说明,其制备及其被用作2,3-环氧环戊基诺基-胆固醇固溶酶的抑制剂

摘要

The present invention relates to urethanes derived from azacycloalkanes in addition to thio and dithio analogues of general formula (I), wherein m= 0 or 1, n=1or 2, A is a single bond, a straight-chain or branched C1-8 alkylene group, a C2-8 alkenylene or C2-8 alkylene group, whereby an unsaturated group is not directly bonded to radical Y; X and Y is an oxygen or sulphur atom, R1 and R2 are a straight-chain or branched C1-6 alkyl group, a C1-4 alkenyl group or a C1-4 alkinyl group, whereby a multiple bond is isolated from the nitrogen-carbon bond, or R1 and R2 together with the nitrogen atom represent a 5-7 membered saturated heterocyclic ring, whereby one methylene group isolated from the nitrogen atom can be replaced by an oxygen or sulphur atom or by an -NH or -N (alkyl) group, R3-R6 can be identical or different and represent hydrogen atoms or alkyl groups, R7 is a C3-7 cycloalkyl group, optionally a phenyl or naphtyl group substituted by two halogen atoms, an alkyl, alkoxy, trifluoromethyl or cyano group or a hydrogen atom, provided that A does not represent a single bond, E is an oxygen or sulphur atom, a methylene, carbonyl or sulfinyl group and R8 represents a hydrogen atom or E represents the -C(R9R10)- group, wherein R10 and adjacent group R8 represent a carbon-carbon bond. The invention also relates to enantiomers, diastereomers and salts thereof, especially physiologically acceptable acid additive salts with valuable properties such as exhibiting an inhibiting effect on cholesterol biosynthesis, in addition to medicaments containing said compounds, the use thereof and a method for the production thereof.
机译:除通式(I)的硫代和二硫代类似物外,本发明还涉及由氮杂环烷衍生得到的氨基甲酸酯,其中m = 0或1,n = 1或2,A为单键,直链或支链C1-8。亚烷基,C 2-8亚烯基或C 2-8亚烷基,其中不饱和基团不直接键合到基团Y上; X和Y为氧或硫原子,R 1和R 2为直链或支链的C 1-6烷基,C 1-4烯基或C 1-4炔基,其中多键R 1和R 2与氮原子分离,或R 1和R 2与氮原子一起代表5-7元饱和杂环,其中从氮原子分离的一个亚甲基可被氧取代或硫原子或-NH或-N(烷基)基团,R 3 -R 6可以相同或不同,并且代表氢原子或烷基,R 7是C3-7环烷基,任选地被两个卤素原子,烷基,烷氧基,三氟甲基或氰基或氢原子取代的苯基或萘基,条件是A不代表单键,E是氧或硫原子,亚甲基,羰基或亚磺酰基R 8表示氢原子,E表示-C(R 9 R 10)-基,R 10和相邻的基团R 8表示碳-碳键。本发明还涉及对映异构体,非对映异构体及其盐,尤其是生理学上可接受的酸加成盐,其除了包含所述化合物的药物外,还具有有价值的性质,例如对胆固醇生物合成具有抑制作用,其用途及其制备方法。

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