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    • 49. 发明授权
    • Unsaturated derivatives at the 4-position of 6-tert-butyl-1,1-dimethylindane and their use in human and veterinary medicine and in cosmetics
    • 6-叔丁基-1,1-二甲基茚满的4-位不饱和衍生物及其在人兽药和化妆品中的应用
    • US06642273B2
    • 2003-11-04
    • US10214665
    • 2002-08-09
    • Angel De LeraBeatriz Dominguez
    • Angel De LeraBeatriz Dominguez
    • A61K3119
    • C07D333/38A61K8/31A61K8/362A61K8/37A61K8/4926A61K8/4973A61K8/4986A61Q7/00A61Q19/00A61Q19/004C07C57/50C07C63/66C07C69/618C07C69/76Y10S977/801Y10S977/905Y10S977/906Y10S977/915
    • An unsaturated derivative at the 4-position of 6-tert-butyl-1,1-dimethylindane corresponding to the following formula: in which: X represents: a divalent radical of formula: and Y represents a divalent radical of following formula: R1 represents —CH3, —(CH2)p—OR4, —(CH2)p—COR5 or —S(O)t—R6, p being 0, 1, 2 or 3, t being 0, 1 or 2, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue selected from the group consisting of residues deriving from glucose, galactose, mannose and glucuronic acid or an amino acid residue deriving from lysine, glycine and aspartic acid, r′ and r″, which are identical or different, represent H, lower alkyl, —COR7, aryl, a sugar residue selected from the group consisting of residues deriving from glucose, galactose, mannose and glucuronic acid or an amino acid residue deriving from lysine, glycine and aspartic acid, or r′ and r″, taken together form a heterocycle selected from the group consisting of piperidino, morpholino, pyrrolidino and piperazino radical, the latter optionally being substituted in the 4-position by a C1-C6 alkyl radical or a mono- or polyhydroxyalkyl, and the salts of the compounds of formula (I), when R1 represents a carboxylic acid functional group, and the geometrical and optical isomers of the compounds of formula (I).
    • 对应于下式的6-叔丁基-1,1-二甲基茚的4-位的不饱和衍生物:其中:X表示:式的二价基团,Y表示下式的二价基团:R 1表示 -CH 3, - (CH 2)p -OR 4, - (CH 2)p-COR 5或-S(O)t -R 6,p为0,1,2或3,t为0,1或2,R 4表示H, 低级烷基,-COR 7,芳基,芳烷基,单 - 或多羟基烷基或聚醚基,R 5表示H,低级烷基,-OR 8或R 6表示H或低级烷基,R 7表示低级烷基,R 8表示H,烷基,烯基,炔基 芳基,芳烷基,单或多羟基烷基,选自葡萄糖,半乳糖,甘露糖和葡糖醛酸的残基或衍生自赖氨酸,甘氨酸和天冬氨酸的氨基酸残基的糖残基,r'和r“ ,其相同或不同,表示H,低级烷基,-COR 7,芳基,选自葡萄糖,半乳糖,甘露糖和葡萄糖的残基的糖残基 衍生自赖氨酸,甘氨酸和天冬氨酸或r'和r“的氨基酸残基一起形成选自哌啶子基,吗啉代,吡咯烷子基和哌嗪基的杂环,后者任选被取代在 当R1表示羧酸官能团时,通过C 1 -C 6烷基或单 - 或多羟基烷基的4-位和式(I)化合物的盐,以及式(I)化合物的几何和旋光异构体 (一世)。