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    1H-[1]benzopyrano[3,4-f]quinoline derivatives and their use as glucocorticoid-selective anti-inflammatory agents
    7.
    发明专利
    1H-[1]benzopyrano[3,4-f]quinoline derivatives and their use as glucocorticoid-selective anti-inflammatory agents 未知

    公开(公告)号：NZ506013A

    公开(公告)日：2003-03-28

    申请号：NZ50601399

    申请日：1999-02-12

    Applicant: ABBOTT LAB ,  LIGAND PHARM INC

    Inventor： COUGHLAN MICHAEL J ,  ELMORE STEVEN W ,  KORT MICHAEL E ,  YM PHILIP R ,  MOORE JIMMIE L ,  PRATT JOHN K ,  WANG ALAN X ,  DWARDS JAMES P ,  JONES TODD K

    IPC: C07D491/052 ,  A61K31/4738 ,  A61K31/519 ,  A61P29/00 ,  C07D491/04 ,  A61K31/4741 ,  A61K31/4747 ,  A61K31/527 ,  C07D491/20

    Abstract: A compound of Formula I, where: R1 is -L1-RA where L1 is selected from a covalent bond, -O-, -S(O) t-, -C(X)-, -NR7-, -NR8C(X)NR9-, -X'C(X)-, -C(X)X'-, -X'C(X)X", -NR8C(X)-, -C(X)NR8-, -NR8C(X)X'-, -X'C(X)NR8, - S02NR8-, -NR8SO2- and -NR8S02NR9-, and where RA is selected from -OH, -OG, -SH, -C02R20, alkoxylcarbonyl, -CN, halo, haloalkoxy, perfluoroalkoxy, -CHO, -NR7R7' -C(X)NR8R9, - OSO2R11, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, perfluoroalkyl, aryl, and heterocycle R2, R3, and R4 are independently hydrogen or R1; or R1 and R2 together are -X*-Y*-Z*, where X* is -O- or -CH2-, Y* is-C(O)- or -(C(R12)(R13))v-, and Z* is selected from - CH2-,-CH2S(O) t-,-CH2O-, -NR7-,-CH2NR7-, -O- L2 is selected from a covalent bond, alkylene, alkynylene, - NR7-, -C(X)-, -O-, and -S(O) t-; R5 is halo, hydrogen, -C(=NR7)OR10, or -CN, provided that when R5 is halo, hydrogen, -C(=NR7)OR10, L2 is a covalent bond, or R5 is alkyl, alkynyl, cycloalkyl, heterocycle, aryl R6 is hydrogen or alkyl; or -L2-R5 and R6 together are selected from =O, a group of formula II or a group of formula III. R16 and R16' are independently hydrogen or alkyl; or R16 and R16' together are alkenyl of two carbons; a broken line represents the optional presence of a double bond, provided that when R16 and R16' together are alkenyl of two carbons, the double bond is not present; Y is selected from carbon, nitrogen, and N+(-O-); R17 is absent or hydrogen or alkyl, provided that when the double bond is present, and Y is nitrogen or N+(-O-), R17 is absent; and R18 and R18' are independently hydrogen or alkyl; or R18 and R18' together are a cycloheteroalkyl ring or a cycloalkyl ring. Also described is a pharmaceutical composition comprising the compound of formula I. The compounds of formula I are useful for selectively modulating the activation, repression, agonism, and antagonism effects of the glucocorticoid receptor.

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