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    • 9. 发明申请
    • 5-(1',1'-CYCLOALKYL/ALKENYL)METHYLIDENE 1,2-DIHYDRO-5H-CHROMENO[3,4-f]QUINOLINES AS SELECTIVE PROGESTERONE RECEPTOR MODULATOR COMPOUNDS
    • 作为选择性孕激素受体调节剂化合物的5-(1',1'-环烯基/亚苄基)甲基1,2-二氢-5H-氯苯并[3,4-f]喹啉
    • WO2004033459A1
    • 2004-04-22
    • PCT/US2003/024416
    • 2003-08-04
    • LIGAND PHARMACEUTICALS INCORPORATEDZHI, LinVAN OEVEREN, Cornelis, Arjan
    • ZHI, LinVAN OEVEREN, Cornelis, Arjan
    • C07D491/04
    • C07D491/04G01N33/743
    • The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions. A compound of the formula (I), wherein R 1 is selected from the group of hydrogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C l -C 4 heteroalkyl, COR 5 , C0 2 R 5 , S0 2 R 5 , and CONR 5 R 6 ; R 2 and R 3 each independently is selected from the group of hydrogen, C 1 -C 6 alkyl, and C 1 -C 6 haloalkyl; or R 2 and R 3 taken together form a cycloalkyl ring of from three to twelve carbons; R 7 through R 9 each independently is selected from the group of hydrogen, F, Cl, Br, I, NO 2 , CN, OR 5 , NR 5 R 6 , SR 5 , COR 5 , C0 2 R 5 , CONR 5 R 6 , C 1 -C 8 alkyl, C 1 -C s heteroalkyl, C 1 -C 8 haloalkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl; Y and Z each independently is selected from the group of O, S, NR 6 and CR 14 R 15 ; n is 0, 1, 2, or 3.
    • 本发明涉及用于调节由孕酮受体介导的过程的化合物,药物组合物和方法。 还提供了制备这些化合物和药物组合物的方法。 式(I)的化合物,其中R 1选自氢,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 1 -C 4杂烷基,COR 5,CO 2 R 5,SO 2 R 5 >和CONR 5 R 6; R 2和R 3各自独立地选自氢,C 1 -C 6烷基和C 1 -C 6卤代烷基; 或R 2和R 3一起形成3至12个碳的环烷基环; R 7至R 9各自独立地选自氢,F,Cl,Br,I,NO 2,CN,OR 5,NR 5 R 6,SR 5, COR 5,CO 2 R 5,CONR 5 R 6,C 1 -C 8烷基,C 1 -C 8杂烷基,C 1 -C 8卤代烷基,C 2 -C 8烯基,C 2 -C 8炔基; Y和Z各自独立地选自O,S,NR 6和CR 14 R 15; n为0,1,2或3。