Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Recombinant or stably-transformed bacterium encoding one or...
Patent
1979-09-24
1981-05-19
Helfin, Bernard
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Recombinant or stably-transformed bacterium encoding one or...
424311, 424331, 560108, 560255, 568326, 568 31, 568 37, 568 41, A01N 3500, C07C 49788
Patent
active
042685230
ABSTRACT:
Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;
R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;
R.sub.3 is selected from hydrogen, methyl and ethyl;
R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;
Z is selected from:
(a) alkylene having from one to nine carbon atoms;
(b) -(alk.sub.1).sub.m -X-(alk.sub.2).sub.n - wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;
m and n are each 0 or 1;
X is selected from O, S, SO and SO.sub.2 ; and
W is selected from hydrogen, methyl, pyridyl, piperidyl, phenyl, monochlorophenyl, monofluorophenyl and ##STR2## wherein W.sub.1 is selected from hydrogen, phenyl, monochlorophenyl and monofluorophenyl; a is an integer from 1 to 5 and b is 0 or an integer from 1 to 4, with the proviso that the sum of a and b is not greater than 5.
Compounds I and II are useful as analgesics. Compound III is useful as an intermediate for the preparation of Compounds I and II. Intermediates for the preparation of I, II and III are disclosed. A process for the use of compounds I and II to produce analgesia is also described.
REFERENCES:
patent: 3681407 (1972-08-01), Los
patent: 3736345 (1973-05-01), Los
Boyakhchyan et al., Sin. Gilerotsikl Soedin, 1972, #9 pp. 71-73, (Chem. Abst., vol. 79, #146361w (1973).
Althuis Thomas H.
Harbert Charles A.
Johnson Michael R.
Melvin, Jr. Lawrence S.
Helfin Bernard
Pfizer Inc.
Reamer James H.
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