| 摘要 |
Disclosed are 1-phenyl-pyrrolo[3,4-b]pyrrole derivatives as represented by the general formula (I), wherein R1 is alkyl, cycloalkyl, or (cycloalkyl)methyl; R2a-R2f each are independently hydrogen, methyl, or fluoromethyl; R3a-R3d are each independently hydrogen, alkyl, fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile; L1 is a bond, oxygen, sulfur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, or NR4; L2 is a bond, oxygen, sulphur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR5, -C(=O)NR5-, or -NR5C(=O)-; Cy1 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; Cy2 is aryl, cycloalkyl, cycloalkenyl, heteroaryl or heterocycle, wherein the heteroaryl or heterocycle moiety has 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur, provided that at least one heteroatom is nitrogen; and wherein the other substituents are as defined herein. Of particular importance are the compounds 2-{ 4'-[(3aR,6aR)-5- methylhexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl]-1,1'-biphenyl-4-yl} pyridazin-3(2H)-one, 2-(5-{ 4-[(3aR,6aR)-5-methylhexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl]phenyl} pyridin-2-yl)pyridazin-3(2H)-one and 2-(6-{ 4-[(3aR,6aR)-5-methylhexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl]phenyl} pyridin-3-yl)pyridazin-3(2H)-one. Further disclosed is a harmaceutical composition which comprises a compound as defined above and a pharmaceutically acceptable carrier.
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