Unsaturated derivatives at the 4-position of 6-tert-butyl-1,1-dimethylindane and their use in human and veterinary medicine and in cosmetics
    1.
    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 失效
    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

    公开(公告)号:US06642273B2

    公开(公告)日:2003-11-04

    申请号:US10214665

    申请日:2002-08-09

    IPC分类号: A61K3119

    摘要: 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).

    摘要翻译: 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)。

    Unsaturated derivatives at the 4-position of 6-tert-butyl-1, 1- dimethylindane and their use in human and veterinary medicine and in cosmetics
    2.
    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 失效
    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用途

    公开(公告)号:US06180674B2

    公开(公告)日:2001-01-30

    申请号:US09158892

    申请日:1998-09-23

    IPC分类号: A61K3119

    摘要: 6-tert-Butyl-1,1-dimethylindane derivatives which are unsaturated in the 4-position of formula: X represents: (i) either a radical of formula: and Y represents a radical of formula: (ii) or a radical of formula: and Y represents either a radical of formula (b) or a radical of formula: Z being —O—, —S— or 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, R2 represents H or lower alkyl, R3 represents H, lower alkyl or —COR7, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or —N(r′)(r″), R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue or an amino acid residue, r′ and r″ represent H, lower alkyl, —COR7, aryl, a sugar residue or an amino acid residue or r′ and r″ form a heterocycle, and the salts of the compounds of formula (I). Use in the topical and systemic treatment of dermatological conditions, as well as in cosmetics.

    摘要翻译: 在式X中4-位不饱和的6-叔丁基-1,1-二甲基茚满衍生物表示:(i)下式的基团:Y表示式(ⅱ)的基团或基团 并且Y表示式(b)的基团或式Z的基团是-O - , - S-或R 1表示-CH 3, - (CH 2)p -OR 4, - (CH 2)p -OR 5或 - S(O)t-R6,p为0,1,2或3,t为0,1或2,R2为H或低级烷基,R3为H,低级烷基或-COR7,R4为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-N(r')(r“),R 6表示H或低级烷基,R 7表示低级烷基 R8代表H,烷基,烯基,炔基,芳基,芳烷基,单或多羟基烷基,糖残基或氨基酸残基,r'和r“代表H,低级烷基,-COR7,芳基,糖残基或 氨基酸残基或r'和r“形成杂环,和式(I)化合物的盐。在局部和系统中使用 ic治疗皮肤病学条件,以及化妆品。

    Unsaturated derivatives at the 4-position of 6-tert-butyl-1,1-dimethylindane and their use in human and veterinary medicine and cosmetics
    3.
    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 cosmetics 失效
    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

    公开(公告)号:US06534545B1

    公开(公告)日:2003-03-18

    申请号:US09579441

    申请日:2000-05-26

    IPC分类号: A61K3119

    摘要: 6-tert-Butyl-1,1-dimethylindane derivatives which are unsaturated in the 4-position of formula: X represents: (i) either a radical of formula: (a)  and Y represents a radical of formula: (b) (ii) or a radical of formula: (c)  and Y represents either a radical of formula (b) or a radical of formula: Z being —O—, —S— or 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, R2 represents H or lower alkyl, R3 represents H, lower alkyl or —COR7, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or —N(r′)(r″), R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue or an amino acid residue, r′ and r″ represent H, lower alkyl, —COR7, aryl, a sugar residue or an amino acid residue or r′ and r″ form a heterocycle, and the salts of the compounds of formula (I). Use in the topical and systemic treatment of dermatological conditions, as well as in cosmetics.

    摘要翻译: 式中X表示不饱和的6-叔丁基-1,1-二甲基茚满衍生物:(i)式(a)的基团和Y表示式(b)的基团( ii)或式(c)的基团,Y表示式(b)的基团或式Z的基团是-O - , - S-或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 2表示H或低级烷基,R 3表示H,低级烷基或 - COR7,R4代表H,低级烷基,-COR7,芳基,芳烷基,单或多羟基烷基或聚醚基,R5代表H,低级烷基,-OR8或-N(r')(r“),R6代表 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,糖残基或氨基酸残基,r'和r“表示H,低级烷基, -COR 7,芳基,糖残基或氨基酸残基或r'和r“形成杂环,和式(I)化合物的盐。使用 皮肤病学的局部和全身治疗,以及化妆品。