Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...
Patent
1981-12-14
1983-08-30
Brown, Johnnie R.
Drug, bio-affecting and body treating compositions
Conjugate or complex of monoclonal or polyclonal antibody,...
Conjugated via claimed linking group, bond, chelating agent,...
536 71, A61K 3171, C07H 1708
Patent
active
044016603
ABSTRACT:
Ester derivatives of 5-O-mycaminosyl tylonolide (OMT) of the formula ##STR1## wherein R and R.sup.1 are selected from hydrogen, optionally substituted C.sub.1 -C.sub.5 -alkanoyl or optionally substituted benzoyl, phenylacetyl, or phenylpropionyl; R.sup.2 is hydrogen or an acyl group selected from: ##STR2## p is 0 or 1; m and n are integers from 0 to 4; R.sup.3 is hydrogen, halo, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, phenyl, C.sub.5 -C.sub.8 -cycloalkenyl, naphthyl, indenyl, tetralinyl, decalinyl, adamantyl, cinnoxacinyl, a monocyclic heterocyclic ring system comprising 3 to 8 atoms in the ring or a bicyclic heterocylic ring system comprising 6 to 11 atoms, provided that at least 1 atom of the ring system is carbon and at least 1 atom of the ring system is a heteroatom selected from O, N, and S; and wherein R.sup.3 and the connecting alkyl groups--(CH.sub.2).sub.m -- and --(CH.sub.2).sub.n -- are optionally substituted by one or two halo, methyl, ethyl, methoxy, amino, N-protected-amino, methylamino, dimethylamino, nitro, acetoxy, acetamido, azido, carbomethoxy, carboxamido, cyano, or hydroxyl groups, provided that, if the substituent is other than halo or alkyl, there can be no more than one substituent on any connecting --CH.sub.2 -- group; X is O, S, --NH--, --N(CH.sub.3)--, --C.tbd.C--, --CH.dbd.CH--, --C(CH.sub.3).dbd.CH--, --CH.dbd.C(CH.sub.3)-- or --C(CH.sub.3).dbd.C (CH.sub.3)--; R.sup.4 and R.sup.5 are C.sub.1 -C.sub.5 -alkyl or optionally substituted phenyl or benzyl; provided that at least one of R, R.sup.1 and R.sup.2 must be other than hydrogen and that, when R.sup.1 is other than hydrogen, R must also be other than hydrogen; and salts thereof; which are useful antibiotics or intermediates to antibiotics, are provided.
REFERENCES:
patent: 3459853 (1969-08-01), Gorman et al.
patent: 4092473 (1978-05-01), Okamoto et al.
patent: 4299953 (1981-11-01), Hamill et al.
patent: 4321361 (1982-03-01), Baltz et al.
A. Tanaka et al. "Synthesis of Recyclized Macrolide Antibiotics and Related Derivatives from Mycaminosyl Tylonolide", Bull. Soc. Chem. Soc. Japan 54, 3837-3845 (1981).
A. Tanaka et al. "Synthesis of 4'-Deoxymycaminosyl Tylonolide", J. Antibiotics 34, 1374-1376 (1981).
A. Tanaka et al. "Syntheses of Derivatives of 4'-Deoxymycaminosyl Tylonolide and Mycaminosyl Tylonolide Modified at C-23", J. Antibiotics 34, 1377-1380 (1981).
S. Omura, Derwent Abstract 82541D/45 of Japanese Kokai J56122-397, Sep. 25, 1981.
Brown Johnnie R.
Eli Lilly and Company
Harrison Nancy J.
Whale Arthur R.
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