| abstract |
A compound represented by the general formula (I), a pharmaceutically acceptable salt, a deuteride or a stereoisomer thereof: ** Formula ** wherein X represents O or S; R1 represents H; R2, R4 and R5 each independently represent H R3 represents carboxyl or C1-3-alkyl OC (O) -, 3-8 membered monocyclic cycloalkyl-OC (O) -, carbamoyl or benzyl- OC (O) -, which is unsubstituted or substituted with 1-3 groups represented by Q1, Q1 represents halogen, hydroxy, amino, phenyl, 3-6 membered cycloalkyl, C1-3 alkyloxy, C1-3 alkylamino or di (C1-3alkyl) amino; R6 represents the following groups, which are unsubstituted or substituted with 1-3 groups represented by Q2: (1) C1-3 alkyl, 3-8 membered monocyclic cycloalkyl, aryl, the carbon atom in the cycloalkyl and the aryl may be substituted with 1-3 identical or different groups selected from N, NH, N (C 1-3 alkyl), O, S (O) m and C (O), (2) ** Formula ** and the carbon atom in the ring can be substituted with 1-3 identical or different groups selected from NH, N (C 1-3 alkyl), O, S (O) m and C (O), p represents 0, 1, 2 or 3, r represents 0 , 1 or 2, s represents 0, 1 or 2, Q2 represents halogen, hydroxy, cyano, carboxyl, amino, nitro, trifluoromethyl, C1-3 alkyl, C1-3 alkyloxy, hydroxy C1-3 alkyl, amino C1-alkyl -3, C1-3alkyloxy-C1-3alkyl, carboxyl-C1-3alkyloxy, C1-3alkylamino, di (C1-3alkyl) amino, C1-3alkyloxycarbonyl, carbamoyl, C1-3alkylaminocarbamoyl, di (C 1-3 alkyl) carbamoyl, C 1-3 alkylcarbonylamino, N 5 (C 1-3 alkyl) C 1-3 alkylcarbonyla ino, C 1-3 -alkylsulfonylamino, N- (C 1-3 alkyl) -C 1-3 alkylsulfonylamino or phenyl-C 1-3 alkylsulfomilamino; R7 represents H or C1-3 alkyl, 3-6 membered moncyclic cycloalkyl or 3-8 membered monocyclic heterocyclyl, which is unsubstituted or substituted with 1-3 groups represented by Q3; ring A represents phenyl, pyrrolyl, pyridyl, pyrimidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl; R8 represents formula (IIa) ** Formula ** in which, Ra, Rb, Rc and Rd each independently represent H, C1-3 alkyl, C1-3 alkyloxy, amino or C1-3 alkylamino, Re represents H, C1-3 alkyl, C1-3 alkyloxy, amino, C1-3 alkylamino, di (C1-3 alkyl) amino, phenylamino, N- (C1-3 alkyl) phenylamino, benzylamino, N- (C1-3 alkyl) benzylamino, phenyl or 5-7 membered monocyclic heterocyclyl, the carbon atom in the 5-7 membered monocyclic heterocyclyl can be substituted with 1-3 identical or different groups selected from S (O) to C (O), the C1- alkyl 3 and the 5-7 membered monocyclic heterocyclyl can be substituted with 1-3 groups represented by Q3, Q3 represents halogen, hydroxy, cyano, carboxyl, amino, nitro, trifluoromethyl or C1-3 alkyl; R 9 represents H, halogen, hydroxy, cyano, carboxyl, amino, nitro, C 1-3 alkyl, trifluoromethyl or C 1-3 alkyloxy; a and b each independently represent 0, 1 or 2; n represents 0, 1 or 2, when n is 2, the substituents represented by R 9 may be the same or different; n1 represents 0, 1 or 2; n2 represents 0 or 1; n3 represents 0, 1 or 2; m represents 1 or 2. |