| 摘要 |
PURPOSE: The alanine derivatives having selective FXa inhibiting activity are provided, which show the improved selectivity to similar enzymes such as trypsin and thrombin, and is thus used for the prevention and treatment of thrombosis. CONSTITUTION: The alanine derivatives are represented by formula, in which D is selected from NH2, CN, aminoiminomethyl and aminomethyl; A is phenyl, hydroxyphenyl, pyridine, pyrol, furan, thiophene, oxazole, isooxazole, imidazole, 1,2-diazole, thiazole, isothiazole, pyridazine, pyrimidine, pyrazine, naphthalene, quinoline, isoquinoline, benzofuran, benzothiophene and indole; Y is selected from CO2R, CH2OR, CH2OAr, wherein Ar is phenyl, pyridine, pyrol, furan, thiophene, oxazole, isooxazole, imidazole, 1,2-diazole, thiazole, isothiazole, pyridazine, pyrimidine, pyrazine, 1,2,3-triazole, 1,2,4-triazole, tetrazol or 1,35-triazine, CH2O(C=O)R, CH2O(C=O)Ar, CONR(R1) and CON(R1)2 when X is NRCO, wherein R is hydrogen or linear, branched, ring, or partial ring lower alkyl having carbon number of 10 or less, NRSO2; P and Q are individually selected from phenyl, pyridine, pyrol, furan, thiopen, oxazole, isooxazole, imidazole, 1,2-diazole, thiazole, isothiazole, pyridazine, pyrimidine, pyrazine, 1,2,3-triazole, 1,2,4-triazole, tetrazol and 1,3,5-triazine; and G1, G2 and G3 are individually selected from H, F, Cl, Br, I, CN, R, OR, SR, NR2, CO2R, COR, CONR2, NR(=O)R, NR(C=O)Ar, N((C=O)R)2, SO2R, SO2NR2, S(=O)R, C(=NH)NH2, CF3, OCF3, SCF3 and NR(C=O)CF3.
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