abstract |
REFERS TO DERIVATIVES OF PROLINE AND CYCLIC AMINO ACIDS OF FORMULA I WHERE A IS ARYL, HETEROARYL; B IS NHCO-ALKYL, NH-CO-CYCLOALKYL, COR1, CYCLOALKYL, HETEROCYCLE, ARYL, HETEROARYL; C IS PHENYL, HETEROARYL OPTIONALLY SUBSTITUTED WITH HALOGEN, HYDROXY, CO2R2, COR2, CONR2R2 ', AMONG OTHERS; G IS H, HALO, ALKYL, HALO-ALKYL, HYDROXY-ALKYL, CH2O-ALKYL, AMONG OTHERS; W1 IS A HYDROCARBON CHAIN; R1 IS ALCOXY, CYCLOALKYL, HETEROCYCLOALKYL, CYCLOALKENYL, ARYL, HETEROARYL, AMONG OTHERS; R2 AND R2 'ARE H, ALKYL; R3 AND R4 ARE H, ALKYL, ARALKYL, ARYL, HETEROARYL, ALCOXYCARBONYL, ARALCOXYCARBONYL, SO2-ALKYL, AMONG OTHERS. ALSO REFERS TO COMPOUNDS OF FORMULA II; X "IS CH2, CH, NH, N; R10 AND R11 ARE H, OH, HALO, ALKYL, AMONG OTHERS. PREFERRED COMPOUNDS 2 - [(3-FLUORO-2'-SULFAMOYL-BIPHENYL-4-IL) AMIDE] OF 1 - [(4-CHLORO-PHENYL) -AMIDE] OF PYRROLIDINE-1,2-DICARBOXYL ACID; 2 - [(3-FLUORO-2'-SULFAMOY-BIPHENYL-4-IL) AMIDE] OF 1 - [( PYRROLIDINE-1,2-DICARBOXYL ACID 5-CHLORO-PYRIDIN-2-IL) -AMIDE] 2 - [(3-FLUORO-2'-SULFANOY-BIPHENYL-4-IL) AMIDE] DE 1 - [(2 , 4-DIFLUORO-PHENYL) -AMIDE] OF THE PYRROLIDINE-1,2-DICARBOXYLIC ACID, AMONG OTHERS. ALSO REFERS TO A PROCEDURE FOR THE PREPARATION. THE COMPOUNDS ARE INHIBITORS OF THE SERINE PROTEASE FACTOR Xa AND MAY BE USEFUL TREATMENT OF THROMBOTH DISORDERS, VENOUS THROMBOSIS, ARTERIAL, PULMONARY EMBOLIA, MYOCARDIAL INFARCTION, BRAIN, RESTENOSIS, ANGINA CANCER |