abstract |
REFERS TO PYRIDINE AND PYRAZINE COMPOUNDS SUBSTITUTED FOR FORMULA (I), WHERE R1 AND R2 FORM A BRIDGE WITH TWO T2 REMAINS AND A T3 REST, FORMING A BICYCLE WITH THE RING, WHERE T2 IS N, CH, 0 CG1 AND T3 ES S, O, CR4G1, C (R4) 2 OR NR3; X IS O, S, Y NR3; AND IT IS LOWER ALKYLENE, CH2-O-, CH-NH-, AMONG OTHERS; q IS FROM 0 TO 3; G3 IS A SELECTED MONO OR BIVALENT REMAINS OF LOWER RENT, NR3COR6, OR6, AMONG OTHERS; A, B, D, E, L ARE INDEPENDENTLY N OR CH, WITH THE CONDITION: a) THE TOTAL NUMBER OF N ATOMS IN THE RING THAT CONTAINS THEM IS FROM 0 TO 3; b) WHEN L IS CH, AND A G3 IS A MONOVALENT SUBSTITUTE AT LEAST ONE OF A AND D IS N; J IS ARYL, PYRIDYL, OR CYCLOALKYL; q 'IS 0 TO 5; G4 E A MONO OR BIVALENT REST OF -N (R6) 2; NR3COR6; HALOGEN, ALKYL, ETC; Z IS N O CR4. THEY ARE SELECTED: 4- (4-CHLOROPHENYLAMINE) -7- (2-METHYLAMINOCARBONYL-4-PYRIDYLMETOXY) FURO- [2,3-d] PYRIDAZINE. IT ALSO REFERS TO A PREPARATION PROCEDURE AND A PHARMACEUTICAL COMPOSITION OPTIONALLY COMBINED WITH AT LEAST ONE ELASTASE OR KINASE INHIBITOR SUCH AS GLIVEC. THESE COMPOUNDS ARE KDR INHIBITORS AND ARE USEFUL IN THE TREATMENT OF VEGF MEDIATED DOLENCIES SUCH AS PULMONARY HYPERTENSION |