New tri:cyclic pyridazino:pyridine derivs. - used as excitatory aminoacid antagonists for treating neurological disorders, e.g stroke or epilepsy.

摘要

(4,5-b)quinoline-1,10-dione derivs. and tricyclic hetero-fused pyridazino-pyridine analogues of formula (I) and their salts and tautomers are new, including B-ring tautomers or reduced derivs. of formula (I'):Z = O, S or NH; Z1 = H, OH, SH or NH2; ring A = ortho-fused phenyl, pyridyl, furyl,etc.; R4 = halo, Q, NO2, CN, 1-3C perfluoroalkyl, OH,etc.;R1 = H or -(CH2)nL; L = M or W; M = e.g. (i) phenyl (or benzo deriv.), opt. substd. by 1-4 of OQ, 2-4C alkenyloxy, 2-4C alkynyloxy,-OCOQ'-phenyl,etc.;(ii) 5-7 membered heterocyclyl contg. 1-3 of O, N and S as heteroatoms,etc.;or (iii) heteroaryl (or benzy deriv.) including pyridyl, thienyl, furyl, gps. contg. 2 heteroatoms selected from N, O and S (e.g. pyrazole, imidazol etc.);W = OH, ORa, OCORa, S(O)mRa, S(O)mNRaRb,etc.;W may also be CORa, NRaCORb,etc., if n is other than zero; n = 0-6;R2 = H or (CH2)nL'; L' = M' or W; M' = e.g. (i) phenyl (or benzo deriv.), opt. substd. by 1-3 of 1-3 of OQ, OH, halo, NO2,etc.; R = H or Q; Ra,Rb = H, Q, 2-4C alkenyl, 2-4C alkynyl,etc.; m = 0-2; Q = 1-4C alkyl (or alkylene if appropriate); Q' = 1-6C alkyl (or alkylene if appropriate); provided that R1 and R2 are not both H.