C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/277.1, 260/2
C07D 221/10 (2006.01) C07C 43/178 (2006.01) C07C 43/205 (2006.01) C07C 49/255 (2006.01) C07D 213/30 (2006.01) C07D 215/233 (2006.01) C07D 221/12 (2006.01) C07D 295/14 (2006.01) C07D 303/22 (2006.01) C07D 491/10 (2006.01) C07F 9/54 (2006.01)
Patent
CA 1095909
ABSTRACT OF THE DISCLOSURE 1,9-Dihydroxyoctahydrobenzo[c]quinolines (I), 1-hydroxyhaxahydrobenzo[c]quinoline-9(??)-ones (II), and 1-hydroxy-tetrahydrobenzo[c]quinolines (?V) useful as CNS agents, especially as analgesics and tranquilizers, as hypo- tensives, as agents for the treatment of glaucoma and as di- uratics; intermediates therefor (III) and derivatives thereof having the formulae: Image , Image , (I) (II) Image and Image (III) (IV) wherein R is hydroxy, alkanoyloxy having from one to five carbon atoms and hydroxymethyl; R1 is hydrogen, benzyl, benzoyl, alkanoyl having from one to five carbon atoms or -CO_(CH2)p-NR2R3 wherein p is 0 or an integer from 1 to 4; each of R2 and R3 when taken individually is hydrogen or alkyl having from one to four carbon atoms; R2 and R3 when taken together with the nitrogen to which they are attached form a 5- or 6-membered hetero- cyclic ring (piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from one to four carbon atoms in the alkyl group); R4 is hydrogen, alkyl having from 1 to 6 carbon atoms and -(CH2)z-C6H5 wherein z is an integer from 1 to 4; R5 is hydrogen, methyl or ethyl; R6 is hydrogen, -(CH2)y- carbalkoxy having from 1 to 4 carbon atoms in the alkoxy group wherein y is 0 or an integer from 1 to 4; carbobenzyloxy, formyl, alkanoyl having from two to five carbon atoms, alkyl having from one to six carbon atoms; -(CH2)x-C6H5 wherein x is an integer from 1 to 4; and -CO(CH2)x-1-C6H5; Ro is oxo, methylene or alkylenedioxy having from two to four carbon atoms; R' is R or Ro; z is (a) alkylene having from one to nine carbon atoms; (b) -(alk1)m-X-(alk2)n- wherein each of (alk1) and (alk2) is alkylene having from one to nine carbon atoms, with the proviso that the summation of carbon atoms in (alk1) plus (alk2) is not greater than 9; each of m and n is 0 or 1; X is O, S, SO or SO2; and W is hydrogen, methyl, Image wherein W1 is hydrogen, chloro or fluoro; pyridyl, piperidyl, cycloalkyl having from 3 to 7 carbon atoms, or monosubstituted cyclo- alkyl wherein the substituent is Image wherein W2 is hydro- gen, chloro or fluoro; and pharmaceutically-acceptable acid addition salts of compounds of Formulae I, II and IV and the ketals of compounds of Formulae II, II and IV wherein the ketal moiety has from two to four carbon atoms.
278410
Gowling Lafleur Henderson Llp
Limited Pfizer
LandOfFree
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