abstract |
REFERS TO PYRIMIDONE SUBSTITUTE DERIVATIVES OF FORMULA B-G-L; WHERE L IS -U-C (T) (RL7) (RL8); T IS COOH; U ES - (CRL1RL2) a- (VL) b- (CRL3RL4) c- (WL) d- (CRL5RL6) e- (XL) f; a, c, e ARE 0-3; b, d, f ARE 0-1; RL1, RL2, RL3, RL4, RL5, RL6 ARE H, HALOGEN, HYDROXYL, C1-C6 ALKYL, - (CH2) w- (YL) y-RL9, AMONG OTHERS; w IS 0-4; and ES 0-1; YL IS CO, WITH (RY1), N (RY1) CO, AMONG OTHERS; RY1 IS H, C1-C6 ALKYL, C1-C6 ALCOXYALKYL, AMONG OTHERS; RL7, RL8 ARE H, HALOGEN, HYDROXYL, C1-C6 ALKYL, AMONG OTHERS; RL9 IS H, OH, CN, HALOGEN, AMONG OTHERS; WL IS A 4-11 MEMBER POLYCYCLIC HYDROCARBON; VL, XL ARE CO, CONRL10, NRL10CO, S, SO, AMONG OTHERS; RL10 IS H, C1-C6 ALKYL, C1-C6 ALCOXYALKYL, AMONG OTHERS; G IS AN IG GROUP; ZG ES O, S, NRG3; RG1, RG2 ARE H, CN, NO2, HALOGEN, C1-C6 ALKYL, AMONG OTHERS; RG3 IS H, OH, C1-C6 ALKYL, AMONG OTHERS. B IS AN ATOM THAT CAN FORM HYDROGEN BRIDGES. PREFERRED COMPOUNDS ARE TRIFLUOROACETATE OF 2 - [(1- {1- [2-CARBOXY-3- (2-NAPHTHYL) PROPYL] -5-METHYL-2-OXO-1,2-DIHYDROPYRIMIDIN-4-IL} -PIPERIDIN- 4-IL) AMINO] -1H-BENZYMIDAZOLE) -1IO; 2 - {[(1- {1 - [(2S) -2-CARBOXI-3-PHENYLPROPYL] -5-METHYL-2-OXO-1,2-DIHYDROPYRIMIDIN-4-IL} -PIPERIDIN-4-IL ACETATE ) METHYL] AMINO} -PYRIDINIUM, AMONG OTHERS. THE COMPOUNDS ARE LIGANDS OF THE Ovß3 INTEGRIN RECEPTOR AND MAY BE USEFUL FOR THE TREATMENT OF ATHEROSCLEROSIS, RHEUMATOID ARTHRITIS, RESTENOSIS, ANGIOPLASTY, ACUTE KIDNEY FAILURE, OSTEOPOROSIS, CANCER, TRICULAR CICATRIZATION OR HUMAN HEALING |