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US 4,730,059 AGranted
6'-thiomethylsubstituted spectinomycins
AssigneeThe Upjohn Company
InventorDavid R. White
Life of this patent
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Abstract
Disclosed are 6'-thiomethylsubstituted spectinomycins (XII) which are useful in the same way as other spectinomycin pharmaceutical agents. 6'-Thiomethylsubstituted (XIV) and protected spectinomycin (XIII) intermediates useful in the production of 6'-thiomethylsubstituted spectinomycins (XII) and 6'-alkenylspectinomycins (IX) are also disclosed.
Claims9
A 6'-thiomethyl-substituted spectinomycin of the formula
- where R.sub.11 is C.sub.1 -C.sub.5 alkyl, --CH.sub.2 --(C.sub.2 -C.sub.4 alkenyl), C.sub.5 -C.sub.8 cycloalkyl, phenyl or phenyl substituted with 1 through 5 --F, --Cl, --Br, or --I and pharmaceutically acceptable salts thereof.
A 6'-thiomethyl-substituted compound of the formula ##STR2## where R.sub.1 is --COO--(t-butyl), --COO--CH.sub.2 CH.sub.2 --Si(CH.sub.3).sub.3 or --COO--CH.sub.2 CH.sub.2 Cl;
- R.sub.3 is C.sub.1 -C.sub.8 alkyl;
- R.sub.11 is C.sub.1 -C.sub.3 alkyl, C.sub.5 -C.sub.8 cycloalkyl or phenyl;
- R.sub.12 is --H or R.sub.3 --CO--;
- is a single or double bond with the proviso that
- (1) when is a double bond, R.sub.12 is R.sub.3 --CO-- and
- (2) when is a single bond, R.sub.12 is a hydrogen atom.
3 more elements
Dependencies are inferred from the claim text.