Tylosin derivatives, their preparation and pharmaceutical compos

Details Tylosin derivatives, their preparation and pharmaceutical compos Tylosin derivatives, their preparation and pharmaceutical compos

1982-07-06

1984-10-16

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, 536 174, 536 187, 536122, 536124, A61K 3171, C07H 1708

Patent

active

044774435

ABSTRACT:
Tylosin compounds of the formula ##STR1## wherein R.sub.1 represents a hydroxyl group; a halogen atom; ##STR2## group (wherein R.sub.5 is a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group and R.sub.6 is a hydrogen atom, a lower alkyl group which may be substituted by a hydroxyl group, an aryl group, an aralkyl group, a cycloalkyl group having 3-10 carbon atoms, --CO(O).sub.m --R.sub.7 group (wherein m is 0 or 1 and R.sub.7 is a lower alkyl group, an aryl group, an aralkyl group, a furanyl group, or a pyridyl group), or --CH.sub.2 --R.sub.13 group (wherein R.sub.13 is a mono-, di-, or trifluoromethyl group)); --N(CH.sub.2).sub.n group (wherein n is an integer of 2-15) which may be substituted by an oxo group, a hydroxyl group, a lower alkyl group, or a hydroxy lower alkyl group; an imidazolyl group, a morpholino group, or a piperazino group each may be substituted by a lower alkyl group; or --OOCCH.sub.2 --R.sub.8 group (wherein R.sub.8 is ##STR3## group (wherein R.sub.9 and R.sub.10, which may be the same or different, each is a hydrogen atom or a lower alkyl group; said R.sub.9 and R.sub.10 may be combined with each other to form an alkylene group having 3-7 carbon atoms) or --S--R.sub.11 group (wherein R.sub.11 is a furanyl group or a pyridyl group)); R.sub.2 represents a hydrogen atom or a lower alkanoyl group; R.sub.3 represents a methyl group or --CH.sub.2 CHO group; R.sub.4 represents a hydrogen atom or a hydroxyl group; A represents 0.dbd., ##STR4## line represents a single bond or a double bond; and line ---- represents a single bond, a double bond, or ; however, when said R.sub.1 is a hydroxyl group, said R.sub.3 is a methyl group and R.sub.4 is a hydrogen atom, or said line ---- is ; or when said R.sub.1 is a halogen atom, said R.sub.3 is a methyl group of said line ---- is .
The foregoing compounds of this invention are useful as antibiotics.

REFERENCES:
patent: 2060850 (1936-11-01), Calcott et al.
patent: 2684961 (1954-07-01), Barham
patent: 4110530 (1978-08-01), Sciavolino
patent: 4304856 (1981-12-01), Baltz et al.
patent: 4373095 (1983-02-01), Ganguly et al.
patent: 4401660 (1983-08-01), Kirst
Houber Weyl, 1957, pp. 985-988.

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