主权项 |
1. A compound of Formula Ia: in which:
L is selected from —NR5a(CH2)2-3, —NR5a(CH2)2NR5b—, —NR5a(CH2)2S—, —NR5aCH2CH(OH)— and —NR5aCH(CH3)CH2—; wherein R5a and R5b are independently selected from hydrogen and C1-4alkyl;R1 is selected from thiophenyl, 1H-benzoimidazolyl, isoquinolinyl, 1H-imidazopyridinyl, benzothiophenyl, pyrimidinyl, pyridinyl, pyrazinyl, pyridazinyl, and thiazolyl; wherein
said thiophenyl, 1H-benzoimidazolyl, isoquinolinyl, 1H-imidazopyridinyl, benzothiophenyl, pyrimidinyl, pyridinyl, pyrazinyl, pyridazinyl, or thiazolyl of R1 can be optionally substituted by 1 to 3 radicals independently selected from cyano, hydroxy, C1-4alkyl, C1-4alkoxy, halo, halo-substituted-C1-4alkyl, halo-substituted-C1-4alkoxy, amino, —C(O)R8a, —S(O)0-2R8a, —C(O)OR8a and —C(O)NR8aR8b; wherein R8a and R8b are independently selected from hydrogen and C1-4alkyl;R2 is selected from —S(O)2NR6aR6b, —NR6aC(O)R6b—, —NR6aC(O)NR6bR6c, phenyl, 1H-pyrrolopyridin-3-yl, 1H-pyrrolopyridin-5-yl, 1H-indolyl thiophenyl, pyridinyl, 1H-1,2,4-triazolyl, 2-oxoimidazolidinyl, 1H-pyrazolyl, 2-oxo-2,3-dihydro-1H-benzoimidazolyl and 1H-indazolyl; wherein
R6a, R6b and R6c are independently selected from hydrogen and C1-4alkyl; andsaid phenyl, 1H-pyrrolopyridin-3-yl, 1H-pyrrolo[2,3-b]pyridin-5-yl, 1H-indolyl, thiophenyl, pyridinyl, 1H-1,2,4-triazolyl, 2-oxoimidazolidinyl, 1H-pyrazolyl, 2-oxo-2,3-dihydro-1H-benzoimidazolyl or 1H-indazolyl of R2 is optionally substituted with 1 to 3 radicals independently selected from hydroxy, halo, methyl, methoxy, amino, —O(CH2)2NR7aR7b, —S(O)2NR7aR7b, —OS(O)2NR7aR7b and —NR7aS(O)2R7b; wherein R7a and R7b are independently selected from hydrogen and C1-4alkyl;R3 is selected from hydrogen, C1-4alkyl and biphenyl; andR4 is selected from C1-10alkyl, prop-1-en-2-yl, cyclohexyl, cyclopropyl, 2-(2-oxopyrrolidin-1-yl)ethyl, oxetan-2-yl, oxetan-3-yl, benzhydryl, tetrahydro-2H-pyran-2-yl, tetrahydro-2H-pyran-3-yl, phenyl, tetrahydrofuran-3-yl, and benzyl, (4-pentylphenyl)(phenyl)methyl and 1-(1-(2-oxo-6,9,12-trioxa-3-azatetradecan-14-yl)-1H-1,2,3-triazol-4-yl)ethyl wherein
said alkyl, cyclopropyl, cyclohexyl, 2-(2-oxopyrrolidin-1-yl)ethyl, oxetan-3-yl, oxetan-2-yl, benzhydryl, tetrahydro-2H-pyran-2-yl, tetrahydro-2H-pyran-3-yl, phenyl, tetrahydrofuran-3-yl, benzyl, (4-pentylphenyl)(phenyl)methyl or 1-(1-(2-oxo-6,9,12-trioxa-3-azatetradecan-14-yl)-1H-1,2,3-triazol-4-yl)ethyl can be optionally substituted with 1 to 3 radicals independently selected from hydroxy, C1-4alkyl and halo-substituted-C1-4alkyl; or a salt thereof. |