| 摘要 |
Disclosed is the use of BUBR1 as a biomarker for predicting the response to a compound, wherein the compound is a compound of general formula I (see abstract drawing) wherein - R represents phenyl, thienyl or pyridinyl - wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; - and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; - X represents a group C=Y, wherein Y stands for oxygen or nitrogen substituted by hydroxy or lower alkoxy; - R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; - R2, R3 and R6 represent hydrogen; - R4 and R5, independently of each other, represent hydrogen, lower alkyl or lower alkoxy; - or R4 and R5 together represent methylenedioxy; - and pharmaceutically acceptable salts, solvates, polymorphs, prodrugs and salts of prodrugs thereof; - or wherein - R represents phenyl or pyridinyl - wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, formyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; - and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; - X represents oxygen; - R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; - R2, R3 and R6 represent hydrogen; - R4 and R5, independently of each other, represent hydrogen, lower alkyl or lower alkoxy; - or R4 and R5 together represent methylenedioxy; - and pharmaceutically acceptable salts, solvates, polymorphs, prodrugs and salts of prodrugs thereof, - and wherein the prefix lower denotes a radical having up to and including a maximum of 7 carbon atoms, and wherein the response is of a disease in a subject and the biomarker BUBR1 is measured ex vivo in a sample or samples taken from the human or animal body. |
