申请人:Schering Aktiengesellschaft
公开号:US04207316A1
公开(公告)日:1980-06-10
Corticoids of the formula ##STR1## wherein represents a single bond or a double bond; X is hydrogen, fluorine, chlorine or methyl; Y is hydrogen and Z is hydrogen, fluorine or chlorine, or Y and Z together are a carbon-to-carbon bond; V is .beta.-hydroxymethylene, .beta.-chloromethylene or carbonyl; W is methylene, ethylidene or vinylidene; Q is oxygen or sulfur; R.sub.1 is alkyl of 1-8 carbon atoms, alkyl of 2-8 carbon atoms with an oxygen atom between two of the carbon atoms or benzyl, and R.sub.2 is hydrogen or alkyl of 1-4 carbon atoms, or R.sub.1 and R.sub.2 collectively are trimethylene or tetramethylene; and R.sub.3 is hydrogen, fluorine, chlorine, hydroxy, or hydroxy esterified by a C.sub.1-16 hydrocarbon carboxylic acid have valuable pharmacological properties, e.g., anti-inflammatory activity.
该公式中的皮质类固醇具有有价值的药理特性,例如抗炎活性。其中表示单键或双键;X为氢、氟、氯或甲基;Y为氢,Z为氢、氟或氯,或者Y和Z共同构成碳-碳键;V为β-羟甲基、β-氯甲基或羰基;W为亚甲基、乙烯基或乙烯基;Q为氧或硫;R.sub.1为1-8个碳原子的烷基、2-8个碳原子之间有一个氧原子的烷基或苄基,R.sub.2为氢或1-4个碳原子的烷基,或者R.sub.1和R.sub.2共同构成三亚甲基或四亚甲基;R.sub.3为氢、氟、氯、羟基或通过C.sub.1-16碳氢化合物羧酸酯化的羟基。