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    • 7. 发明授权
    • Platelet aggregation inhibiting compounds
    • 血小板聚集抑制化合物
    • US6028087A
    • 2000-02-22
    • US10238
    • 1998-01-21
    • William Edward BondinellJames Francis CallahanWilliam Francis HuffmanRichard McCulloch KeenanBrian Walter MetcalfJames SamanenTobias Oregon Yellin
    • William Edward BondinellJames Francis CallahanWilliam Francis HuffmanRichard McCulloch KeenanBrian Walter MetcalfJames SamanenTobias Oregon Yellin
    • A61K38/00C07D213/56C07D213/73C07D417/12C07K5/083C07K5/09A61K31/44
    • C07D213/73C07D213/56C07D417/12C07K5/0806C07K5/0815C07K5/0817A61K38/00
    • Compounds of the formula (I):W--Z--(CR'R.sup.10).sub.r --U--(CR'.sub.2).sub.s --V--A (I)wherein:A is ##STR1## W is .sup.N ; Z is (CH.sub.2).sub.1-2 ;U and V independently are present as CO, CR'.sub.2, C(.dbd.CR'.sub.2), S(O).sub.r, O, NR', CR'OR', CR'(OR")CR'.sub.2, CR'.sub.2 CR'(OR"), C(O)CR'.sub.2, CR'.sub.2 C(O), CONR', NR'CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR', NR'C(S), S(O).sub.r NR', NR'S(O).sub.r, N.dbd.N, NR'NR', NR'CR'.sub.2, NR'CR'.sub.2, CR'.sub.2 O, OCR'.sub.2, C.tbd.C, CR'.dbd.CR', or CR'(NR'R")C(O);each r independently is 0 to 3;s is 0 to 2;each R' independently is H, C.sub.1-4 alkyl, C.sub.3-7 cycloalky-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;each R" independently is R', --C(O)R', or --C(O)OR.sup.15 ;R.sup.10 is H, C.sub.1-4 alkyl, or --NR'R';each R.sup.15 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;R.sup.2 is present once or twice as C.sub.1-4 alkyl, J--CO.sub.2 R', CONR', SR', NR'R", C .sub.1-4 alkoxy, hydroxy, CN, CF.sub.3, halo, or ##STR2## with the proviso that at least one R.sup.2 is J--CO.sub.2 R; and J is a single bond, --OCR'.sub.2 --, --NR'CR'.sub.2 --, CR'.sub.2 --CR'.sub.2 --, --CR'.sub.2 --, --CR'.dbd.CR', or --C(O)NR'CR'.sub.2 --;each R.sup.14 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, Ar-C.sub.0-4 alkyl, C(O)R', CN, NO.sub.2, SO.sub.2 R', or C(O)OR.sup.15 ;or a pharmaceutically acceptable salt thereof, are effective for inhibiting platelet aggregation.
    • 式(I)的化合物:W-Z-(CR'R10)r-U-(CR'2)s-V-A(I)其中:A是W是+ E,crc N + EE; Z是(CH 2)1-2; U和V独立地作为CO,CR'2,C(= CR'2),S(O)r,O,NR',CR'OR',CR'(OR“)CR'2,CR' (OR),C(O)CR'2,CR'2C(O),CONR',NR'CO,OC(O),C(O)O,C(O) ),C(S)NR',NR'C(S),S(O)rNR',NR'S(O)r,N = N,NR'NR',NR'CR'2,NR'CR'2, CR'2O,OCR'2,C 3BOND C,CR'= CR'或CR'(NR'R“)C(O); 每个r独立为0至3; s为0〜2; 每个R'独立地为H,C 1-4烷基,C 3-7环烷基-C 0-4烷基或Ar-C 0-4烷基; 每个R“独立地是R',-C(O)R'或-C(O)OR 15; R 10是H,C 1-4烷基或-NR'R'; 每个R 15独立地为C 1-4烷基,C 3-7环烷基-C 0-4烷基或Ar-C 0-4烷基; R 2存在一次或两次作为C 1-4烷基,J-CO 2 R',CONR',SR',NR'R“,C 1-4烷氧基,羟基,CN,CF 3,卤素,或条件是至少一个R 2 是J-CO2R; 并且J是单键,-OCR'2 - ,-NR'CR'2 - ,CR'2-CR'2,-CR'2-,-CR'= CR'或-C(O)NR 'CR'2-; 每个R 14独立地是C 1-4烷基,C 3-7环烷基-C 0-4烷基,Ar-C 0-4烷基,C(O)R',CN,NO 2,SO 2 R'或C(O)OR 15; 或其药学上可接受的盐对抑制血小板聚集是有效的。