公开(公告)号：EP1200396A1

公开(公告)日：2002-05-02

申请号：EP00952351.5

申请日：2000-07-28

申请人： TELIK, INC.

发明人： SPEVAK, Wayne, R. ,  SONGYUAN, Shi ,  PRASAD, V., V., S., V., Manchem ,  KOZLOWSKI, Michael, R. ,  SCHOW, Steven, R. ,  LUM, Robert, T. ,  ROBINSON, Louise ,  PARK, Jeong, Weong

IPC分类号： C07C309/51 ,  C07C309/59 ,  C07D213/81 ,  C07D213/82 ,  C07D307/85 ,  C07C311/21 ,  C07C311/29 ,  C07C311/13 ,  C07C237/42 ,  A61K31/16 ,  A61K31/18 ,  A61K31/33

CPC分类号： C07D241/44 ,  C07C237/42 ,  C07C309/51 ,  C07C309/59 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D307/68 ,  C07D307/85

摘要： Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds are provided. Compounds of formula (1) where: R?1 and R2¿ are, independently, hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, R3 is a substituent on the B ring; and is -SO¿2OR?6, -C(O)OR6, -SO2NR62-C(O)NR62 or tetrazolyl; the linker -WY- between the naphthyl and phenyl intersects the A ring of the naphthyl and is, independently, -C(O)NR?7-, -NR7¿C(O)-, -C(O)O-, -OC(O)-, -CH=CH-, -NR7CH2-, -CH2NR?7-, -NR7C(O)NR7- -NR7¿C(O)O-, -OC(O)NR?7-, -NR7SO¿2O-, -OSO2NR7-, -OC(O)O-, -SO¿2?NR?7-, -NR7SO¿2-, -OSO2-, or -SO2O-; each R?6 and R7¿ is, independently, hydrogen or lower alkyl; optionally in the form of single stereoisomers or mixtures of stereoisomers, or the pharmaceutically acceptable salts thereof; are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.