| 摘要 |
Disclosed are benzoxazines and benzothiazines of formula (I), (I)wherein Q is O-(CHR)or S-(CHR); Rand each Ris H, optionally substituted [Calkyl, Calkaryl, Calkheterocyclyl, Cheterocyclyl, Ccycloalkyl, Calkcycloalkyl] or - (CRR)nNRRwherein R, R, R, Rare independently hydrogen, optionally substituted [Calkyl, Calkaryl, Calkheterocyclyl, Cheterocyclyl, Ccycloalkyl, etc.] or wherein Rand Rcombine to form=O, or wherein Rand Rcombine to form an optionally substituted Cheterocyclyl, and n is an integer between 1-6; each of Rand Ris H, hal, optionally substituted [Calkyl, Caryl, Calkaryl, Cheterocyclyl, Calkoxy, Cthioalkoxy, (CH2)NHC(NH)R, CH2)NHC(S)NHR, Calkheterocyclyl] or hydroxyl, wherein r2 is an integer from 0 to 2, Ris optionally substituted [Calkyl, Caryl, Calkaryl, Cheterocyclyl, Calkheterocyclyl, Cthioalkoxy, Cthioalkaryl, aryloyl, Cthioalkheterocylyl, or amino]; each Rand Ris H, hal, (CH)NHC(NH)Ror CH2)NHC(S)NH R; Yand Yare together=O or Yand Yare independently H, optionally substituted [Calkyl, Caryl, Calkaryl, Cheterocyclyl, Calkoxy, Cthioalkoxy, Calkheterocyclyl] or hydroxy; wherein only one of R, R, Rand Ris (CH)NHC(NH)Ror CH2)r2NHC(S)NH R; or a pharmaceutically acceptable salt or prodrug thereof. Said benzoxazines and benzothiazines of formula (I) inhibit nitric oxide synthase (NOS), particularly selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of formula (I), alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions. |
