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    Arylpyridazinones and their use as prostaglandin endoperoxide H synthase biosynthesis inhibitors
    66.
    发明专利
    Arylpyridazinones and their use as prostaglandin endoperoxide H synthase biosynthesis inhibitors 未知

    公开(公告)号：NZ501808A

    公开(公告)日：2002-12-20

    申请号：NZ50180898

    申请日：1998-08-10

    Applicant: ABBOTT LAB

    Inventor： KORT MICHAEL E ,  BASHA ANWER ,  KOLASA TEODOZYJ ,  LIU HUAQING ,  MCCARTY CATHERINE M ,  PATEL MEENA V ,  ROHDE JEFFREY J ,  BLACK LAWRENCE A

    IPC: C07D237/14 ,  A61K31/496 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5377 ,  A61P5/00 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D237/10 ,  C07D237/16 ,  C07D237/18 ,  C07D237/20 ,  C07D237/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07F9/547 ,  C07F9/6509 ,  C07F11/00

    Abstract: A compound of formula (I); wherein: X is O, S, NR4, N-ORa, or N-NRbRc; R is H, alkyl, alkenyl, alkynyl, alkylcarbonylalkyl, alkylsulfonylalkyl, alkylsulfonylarylalkyl, alkoxy, alkoxyalkyl, carboxy, carboxyalkyl, cyanoalkyl, haloalkyl, haloalkenyl, haloalkynyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, arylalkyl, arylalkenyl, arylalkynyl, arylalkoxy, arylhaloalkyl, arylhydroxyalkyl, aryloxy, aryloxyhydroxyalkyl, aryloxyhaloalkyl, arylcarbonylalkyl, haloalkoxyhydroxyalkyl, heterocyclic, heterocyclic alkyl, heterocyclic alkoxy, heterocyclic oxy, -C(O)R5, (CH2)nC(O)R5, -R6-R7, -(CH2)nCH(OH)R5, -(CH2)nCH(ORd)R5, -(CH2)nC(NORd)R5, (CH2)nC(NRd)R5, -(CH2)nCH(NORd)R5, -(CH2)nCH(NRdRe)R5, -(CH2)nCºC-R7, (CH2)n[CH(CX'3)]m-(CH2)n-CX'3, -(CH2)n(CX'2)m-(CH2)n-CX'3, -(CH2)n[CH(CX'3)]m-(CH2)n-R8, (CH2)n(CHX'2)m-(CH2)nR8, -(CH2)n(CHX')m-(CH2)n-CX'3, -(CH2)n(CHX')m-(CH2)n-R8, and (CH2)nR20. At least one of R1, R2 and R3 is selected from formula (II) or (III), shown. The remaining two of the groups of R1 and R3, are independently H, hydroxy, hydroxyalkyl, halogen, alkyl, alkenyl, alkynyl, alkylamino, alkenyloxy, alkylthio, alkylthioalkoxy, alkoxy, alkoxyalkyl, alkoxyalkylamino, alkoxyalkoxy, amido, amidoalkyl, haloalkyl, haloalkenyloxy, haloalkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, cycloalkenylalkoxy, cycloalkylalkoxy, cycloalkylalkylamino, cycloalkylamino, cycloalkyloxy, cycloalkylidenealkyl, amino, aminocarbonyl, aminoalkoxy, aminocarbonylalkyl, alkylaminoaryloxy, dialkylamino, dialkylaminoaryloxy, arylamino, arylalkylamino, diarylamino, aryl, arylalkyl, arylalkylthio, arylalkenyl, arylalkynyl, arylalkoxy, aryloxy, heterocyclic, heterocyclic alkyl, heterocyclic(alkyl)amino, heterocyclic alkoxy, heterocyclic amino, heterocyclic oxy, heterocyclic thio, hydroxyalkylamino, hydroxyalkoxy, hydroxyalkylthio, mercaptoalkoxy, oxoalkoxy, cyano, nitro, aryloxyalkyl, alkylthioalkyl, arylthioalkyl, heterocyclic(alkyl) and Y, wherein Y is -OR14, -SR14, -C(R16)(R17)(R14), -C(O)NR21R14, -C(O)R14, -C(O)OR14, -NH(R14), -NC(O)R14,-N=CR21R14, -N-R19R14. R2 is H, hydroxy, hydroxyalkyl, halogen, alkyl, alkenyl, alkynyl, alkylamino, alkenyloxy, alkylthio, alkylthioalkoxy, alkoxy, alkoxyalkyl, alkoxyalkylamino, alkoxyalkoxy, amido, amidoalkyl, haloalkyl, haloalkenyloxy, haloalkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, cycloalkenylalkoxy, cycloalkylalkoxy, cycloalkylalkylamino, cycloalkylamino, cycloalkyloxy, cycloalkylidenealkyl, amino, aminocarbonyl, aminoalkoxy, aminocarbonylalkyl, alkylaminoaryloxy, dialkylamino, dialkylaminoaryloxy, arylamino, arylalkylamino, diarylamino, aryl, arylalkyl, arylalkylthio, arylalkenyl, arylalkynyl, arylalkoxy, aryloxy, heterocyclic, heterocyclic alkyl, heterocyclic(alkyl)amino, heterocyclic alkoxy, heterocyclic amino, heterocyclic oxy, heterocyclic thio, hydroxyalkylamino, hydroxyalkoxy, hydroxyalkylthio, mercaptoalkoxy, oxoalkoxy, cyano, nitro and Y, wherein Y is -OR14, -SR14, -C(R16)(R17)(R14), -C(O)NR21R14, -C(O)R14, -C(O)OR14, -NH(R14), -NC(O)R14,-N=CR21R14, -NR19R14. Also described is a pharmaceutical composition comprising the compound of formula (I). The compounds of formula (I) are useful for inhibiting prostaglandin biosynthesis. The compounds of formula (I) are particularly useful for treating pain, fever, inflammation, rheumatoid arthritis, osteoarthritis and adhesions.

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