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    • 6. 发明授权
    • Alpha-substituted pyridazino quinoline compounds
    • α-取代哒嗪喹啉化合物
    • US5837705A
    • 1998-11-17
    • US617728
    • 1996-04-01
    • Thomas Michael BareJames Roy EmpfieldJanet Marie ForstKeith John HerzogRichard Bruce Sparks
    • Thomas Michael BareJames Roy EmpfieldJanet Marie ForstKeith John HerzogRichard Bruce Sparks
    • C07D491/147A61K31/50A61P25/00A61P25/04A61P25/28A61P25/30C07D471/04C07D471/14C07D495/14C07D491/14
    • C07D471/04
    • The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: ##STR1## wherein Ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R.sup.1 is selected from a variety of substituents including halogen, (1-4C)alkyl and nitro; R.sup.2 is selected from a group of the formula R2', R2" or R2"' wherein R2' is --CHR.sup.3 (CH.sub.2).sub.n C(O)NR.sup.5 R.sup.6 ; R2" is --CHR.sup.3 (CH.sub.2).sub.n R.sup.4 and R2"' is --CHR.sup.3 (CH.sub.2).sub.n L wherein n is 0-6; R.sup.5 is aryl or substituted aryl; R.sup.6 is (1-6C)alkyl or hydrogen; R.sup.3 is (1-6C)alkyl, (0-6C)alkylCF.sub.3 or (0-6C)alkylCOOR'; R.sup.4 is (1-6C)alkyl, (2-6C)alkyl containing a double or triple bond, or (0-6C)alkylaryl; L is a variety of substituents including phenyl, heteroaryl and CO.sub.2 R'; R' is hydrogen or (1-4C)alkyl; Z is selected from oxo, --OH, H,H--, H, (1-6C)alkyl or (1-6C)alkylaryl; and R.sup.7 is hydrogen or --(CO)R.sup.8 wherein R.sup.8 is a variety of substituents including hydrogen and (1-12C) alkyl.
    • 本发明涉及式I的α-取代的哒嗪 - 喹啉化合物:其中环A选自邻近稠合芳族或杂芳族五元或六元环; R1选自多种取代基,包括卤素,(1-4C)烷基和硝基; R2选自式R2',R2“或R2”'的基团,其中R2'为-CHR3(CH2)nC(O)NR5R6; R2“是-CHR3(CH2)nR4,R2”'是-CHR3(CH2)nL,其中n是0-6; R5是芳基或取代的芳基; R6是(1-6C)烷基或氢; R3是(1-6C)烷基,(0-6C)烷基CF3或(0-6C)烷基COOR'; R4是(1-6C)烷基,含有双键或三键的(2-6C)烷基,或(0-6C)烷基芳基; L是各种取代基,包括苯基,杂芳基和CO 2 R'; R'是氢或(1-4C)烷基; Z选自氧代,-OH,H,H,H,(1-6C)烷基或(1-6C)烷基芳基; 并且R 7是氢或 - (CO)R 8,其中R 8是各种取代基,包括氢和(1-12C)烷基。