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    • 6. 发明申请
    • HETEROCYCLIC SULFONAMIDE DERIVATIVES AS INHIBITORS OF FACTOR XA
    • 作为因子XA的抑制剂的杂环磺酰胺衍生物
    • WO2007008143A1
    • 2007-01-18
    • PCT/SE2006/000837
    • 2006-07-05
    • ASTRAZENECA ABALSTERMARK, ChristerAMIN, KosratANDERSSON, KjellCHEN, YantaoFAHLANDER, UlfFOOTE, Kevin, MichaelGRANBERG, KennethHOVDAL, Daniel
    • ALSTERMARK, ChristerAMIN, KosratANDERSSON, KjellCHEN, YantaoFAHLANDER, UlfFOOTE, Kevin, MichaelGRANBERG, KennethHOVDAL, Daniel
    • C07D401/14A61K31/497A61K31/501A61P7/02C07D401/12C07D403/14C07D409/14C07D413/14
    • C07D409/14C07D401/04C07D401/14
    • The invention relates to compounds of formula (I), wherein R 1 and R 3 are independently selected from carbon and nitrogen; R 2 is oxo or thioxo; n is 0, 1 or 2; each R 10 is independently selected from hydrogen and C 1 - 3 alkyl; R 4 and R 5 are each selected from carbon and nitrogen, wherein at least one of R 4 and R 5 is nitrogen; R 6 is hydrogen or oxo; R 7 is an aliphatic, partially saturated or aromatic carbocyclic ring, said carbocyclic ring having 0, 1 or 2 hetero nitrogen; m is 0, 1 or 2; each R 11 is independently selected from hydrogen, hydroxy, oxo, C 1-5 alkyl, carboxy, hydroxyC 1-5 alkyl, carboxyC 1-5 alkyl, C 1-5 alkoxyoxoC 1-5 alkyl, carbamoyl, C 1-5 alkylcarbamoyl, di (C 1-5 alkyl)carbamoyl, carbamoylC 1-4 alkyl,C 1-5 alkylcarbamoylC 1-4 alkyl, di(C 1-5 alkyl)carbamoylC 1-4 alkyl, hydroxyC 1-5 alkylcarbamoyl, C 1-5 alkoxyC 1-5 alkylcarbamoyl, hydroxyC 1-5 alkylcarbamoylC 1-4 alkyl, C 1-5 alkoxyC 1-5 alkylcarbamoylC 1-4 alkyl, CONR 80 (CH 2 ) x S(O) p R90, CONH(CH 2 ) q NR 100 R 100 , -C 1-5 alkyl-Y 1 , -COOCHR 170 R 180 and -CON R 170 R 180 ; R 8 is a bond, C 1-4 alkylene or C 2-6 alkenylene; R 9 is an aromatic ring system having 0, 1 or 2 hetero atoms; wherein R 9 is substituted by 0 or 1 halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.
    • 本发明涉及式(I)化合物,其中R 1和R 3独立地选自碳和氮; R 2是氧代或硫代; n为0,1或2; 每个R 10独立地选自氢和C 1 -C 3 - 烷基; R 4和R 5各自选自碳和氮,其中R 4和R 5中的至少一个 >是氮; R 6是氢或氧代; R 7是脂族,部分饱和或芳族碳环,所述碳环具有0,1或2个杂氮; m为0,1或2; 每个R 11独立地选自氢,羟基,氧代,C 1-5烷基,羧基,羟基C 1-5烷基,羧基C 1-4烷基, C 1-5烷基,C 1-5烷氧基氧基C 1-5烷基,氨基甲酰基,C 1-5烷基氨基甲酰基, 二(C 1-5烷基)氨基甲酰基,氨基甲酰基C 1-4烷基,C 1-5烷基氨基甲酰基C 1-4 - 烷基,二(C 1-5烷基)氨基甲酰基C 1-4烷基,羟基C 1-5烷基氨基甲酰基,C 1 -5烷氧基C 1-5烷基氨基甲酰基,羟基C 1-5烷基氨基甲酰基C 1-4烷基,C 1-5 烷基C 1-4烷基氨基甲酰基C 1-4烷基,CONR 80(CH 2)