Aromatic carboxylic acid esters
    43.
    发明授权
    Aromatic carboxylic acid esters 失效
    芳香族羧酸酯

    公开(公告)号:US5726191A

    公开(公告)日:1998-03-10

    申请号:US735941

    申请日:1996-10-23

    摘要: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 -alkyl; R.sup.2 is C.sub.1-6 -alkyl or adamantyl; R.sup.3 is C.sub.1-6 -alkyl or hydroxy; or R.sup.2 and R.sup.3 taken together are --(CR.sup.6 R.sup.7).sub.n --; R.sup.4 is C.sub.2-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 -alkynyl, --OCH.sub.2 R.sup.5 or C.sub.2-8 -alkanoyl; and hydrogen when R.sup.3 is hydroxy; R.sup.5 is C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl; R.sup.6 and R.sup.7 are hydrogen or C.sub.1-6 -alkyl; Y is oxygen or sulphur; and n is 3, 4 or 5, and pharmaceutically usable salts of carboxylic acids of formula I act as selective ligands of retinoic acid .gamma.-receptors and are useful for the treatment of epithelial lesions.

    摘要翻译: 式Ⅰ化合物,其中R 1是氢或C 1-6 - 烷基; R2是C1-6烷基或金刚烷基; R3是C1-6烷基或羟基; 或R 2和R 3一起为 - (CR 6 R 7)n - ; R 4是C 2-8 - 烷基,C 2-8 - 烯基,C 2-8 - 炔基,-OCH 2 R 5或C 2-8 - 烷酰基; 当R3为羟基时为氢; R5是C1-6-烷基,C2-6-烯基或C2-6-炔基; R6和R7是氢或C1-6烷基; Y是氧或硫; 并且n为3,4或5,并且式I的羧酸的药学上可用的盐作为视黄酸γ-受体的选择性配体,并且可用于治疗上皮损伤。

    Stilbene derivatives
    44.
    发明授权
    Stilbene derivatives 失效
    二苯乙烯衍生物

    公开(公告)号:US5378705A

    公开(公告)日:1995-01-03

    申请号:US102609

    申请日:1993-08-05

    摘要: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.

    摘要翻译: 式Ⅰ的化合物,其中R 1和R 2各自独立地为低级烷基; 或一起是直链中具有3-5个C原子的亚烷基; 残基R3和R4之一是氢,另一个是氢或低级烷基; R6和R7是氢或低级烷基; R5和R8是氢,低级烷基,低级烷氧基或卤素; X表示-O - , - S - , - SO - , - SO 2 - 或-NR 9; R9是氢,低级烷基或酰基; Y是-S(O)m R 10或-NHet,且其中X是-NR 9 - , - S - , - SO-或-SO 2 - ,以及-N(R 11)2或-OR 12; R10为低级烷基; R 11和R 12是氢,低级烷基或酰基; -NHet是通过N-原子连接的5-8元饱和或不饱和的单环杂环; n为2,3或4,m为0,1或2。 式I的化合物可用作治疗诸如赘生物,皮肤病或皮肤老化的病症的药剂。

    Carboxamides and anilides
    45.
    发明授权
    Carboxamides and anilides 失效
    碳酰胺和抗体

    公开(公告)号:US5216148A

    公开(公告)日:1993-06-01

    申请号:US842662

    申请日:1992-02-27

    摘要: Described herein are compounds of the formula ##STR1## wherein R.sup.1 signifies hydrogen, lower-alkyl or a cation;R.sup.2 signifies hydrogen, lower-alkyl, lower-alkoxy or halogen;M signifies --CONH-- or --NHCO--;X and Y are each independently selected from the group consisting of >CR.sup.3 R.sup.4 and --CONR.sup.5 --;Z signifies >CR.sup.6 R.sup.7 ;R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are each independently selected from the group consisting of hydrogen and lower-alkyl;R.sup.5 signifies alkyl; andn signifies 0, 1 or 2;provided that at least one of X or Y is --CONR.sup.5 -- which is bonded to the phenyl ring via the N atom.These compounds are useful in the treatment and prophylaxis of neoplasms, dermatoses and aging of the skin.

    摘要翻译: 本文描述的是其中R 1表示氢,低级烷基或阳离子的式Ⅰ化合物; R2表示氢,低级烷基,低级烷氧基或卤素; M表示-CONH-或-NHCO-; X和Y各自独立地选自> CR 3 R 4和-CONR 5 - ; Z表示> CR6R7; R3,R4,R6和R7各自独立地选自氢和低级烷基; R5表示烷基; n表示0,1或2; 条件是X或Y中的至少一个是-CONR 5 - 其经由N原子键合到苯环。 这些化合物可用于治疗和预防皮肤赘生物,皮肤病和老化。