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Pyrrolidine derivatives used as cathepsin inhibitors
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
BANNER, DAVID,GRETHER, UWE,HAAP, WOLFGANG,KUEHNE, HOLGER,MAUSER, HARALD,PLANCHER, JEAN-MARC
申请号:
ES11776459
公开号:
ES2512445T3
申请日:
2011.11.02
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of formula (I) ** Formula ** wherein: R1 is hydrogen, alkyl, morpholinyl, haloalkylamino, alkyloxadiazolyl, hydroxyl, halopyrrolidinyl, azetidinyl, alkylamino, amino, cyanoalkylamino, halophenylalkylamino or cyanocycloalkylamino; R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkyloxy, halogen, hydroxyl, cyanopyrazinyloxy, pyrazolyl, alkylpyrazolyl, imidazolyl, benzoimidazolyl, 6-oxo-6H-pyridazinyl, alkyl 6-oxo-6H-pyridazinyl, piperazinyl, N-alkylpiperazinyl, piperidinyl, difluoropyrrolidinyl, phenylimidazolyl, oxo-pyrrolidinyl, oxo-oxazolidinyl, morpholinyl, oxo-morpholinyl, oxo-pyridinyl, 2-oxo-2Hpirazinilo, difluoropiperidinyl, haloalquilpiperidinilo, piperidinylalkoxy, oxethanyloxy, alkylpyrazolyl, halopyridinyl, alkylpyridinyl, cycloalkyl, cycloalkylalkyl, halophenyl, alkylcarbonylaminocycloalkylalkyl, haloalkylpiperazinyl, alkylamino, alkoxyalkylpiperazin-1,2-cycloalkylpiperazinyl, hexahydropyrrolo] [4,3-a] pyrazin-7-yl, alkylimidazolyl, azetidinyl, cycloalkylpiperazinyl, alkylimidazolyl, alkoxyalkoxy, imidazo [4,5-c] pyridinyl, alkylpiperazini lo, hexahydropyrrolo [1,2-a] pyrazinyl, haloazetidinyl, pyrimidinyl, and alkenyloxy; A1 is -CH2-, carbonyl, -C (O) O- or absent; A2 is nitrogen or CR7; A3 is nitrogen or CR8; A4 is nitrogen or CR9; R7 is hydrogen, alkyl, haloalkyl, halogen, hydroxyl, haloalkylaminocarbonyl; halophenyl alkylaminocarbonyl, phenylcycloalkylaminocarbonyl, haloalkylphenylakylaminocarbonyl, halophenylcycloalkylaminocarbonyl or halophenylcycloalkylakylaminocarbonyl; R8 is hydrogen, alkyl, haloalkyl, halogen, or hydroxyl; or R7 and R8 together with the carbon atom to which they are attached form a cycloalkyl or substituted pyrrolidinyl, said substituted pyrrolidinyl is haloalkyl or formyl N-substituted pyrrolidinyl; R9 is hydrogen, alkyl, haloalkyl, halogen, or nitro; or R8 and R9 together with the carbon atom to which they are attached form a cycloalkyl; or a pharmaceutica
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