Macrolide antibiotic derivatives

Claim 2

A relatively acid stable macrolide antibiotic having a plurality of hydroxyl groups, in which one or more of the hydroxyl groups are replaced by a group of the formula -O-SiR'R"R'", where R', R", and R'" are hydrogen or C 1 to C 8 alkyl, substituted alkyl, cycloalkyl, alkaryl or alkenyl, provided that R', R ", and R'" are not all hydrogen; and pharmaceutically acceptable salts and esters thereof.

Claim 3

A compound of the formula or where A is =0 or =N-OR1, B is H or OR 4 , R 1 , R2' R3' R4 and R5 are independently selected from hydrogen, C 1 to C 8 alkyl and SiR'R"R'", where R', R", and R'" are hydrogen or alkyl, substituted alkyl, cycloalkyl, alkaryl or alkenyl of 1 to 8 carbon atoms, provided that at least one of R', R ", and R'" is not hydrogen; and R 6 is selected from hydrogen, methyl, and ethyl; provided that at least one of R 1 - R 5 is of the formula SiR'R"R'", and further provided that when A is =O and B is OH, at least one of R 1 to R 6 is neither hydrogen nor SiR'R"R'".

Claim 4

A compound of the formula or where A is =0 or =N-OR1, B is H or OR 4 , R 1 , R2' R3' R4 and R5 are independently selected from hydrogen, C 1 to C 8 alkyl and SiR'R"R'", where R', R", and R'" are hydrogen or alkyl, substituted alkyl, cycloalkyl, alkaryl or alkenyl of 1 to 8 carbon atoms, provided that at least one of R', R ", and R'" is not hydrogen; and R 6 is selected from hydrogen, methyl, and ethyl; provided that at least one of R 1 - R 5 is of the formula SiR'R"R'", and further provided that when A is =O and B is OH, at least one of R 1 to R 6 is neither hydrogen nor SiR'R"R'".

Claim 5

A compound according to formula (I) of Claim 2 wherein R 2 is trimethylsilyl, A is =0, R 6 is hydrogen, and B is H or OR 4 where R 4 is C 1 to C 8 alkyl.

Claim 6

A compound according to formula (II) of Claim 2 wherein A is = 0 , R 2 is trimethylsilyl, B is OH, and R 6 is methyl.

Claim 7

A compound according to Claim 4 where A= O , R2 is trimethylsilyl, B is OR 4 , R 3 -R 5 are all hydrogen, and R 6 is methyl.

Claim 8

A pharmaceutical composition in unit dosage form, comprising a compound according to Claim 1 in combination with a pharmaceutical carrier.

Claim 9

A liquid oral dosage form according to Claim 6 wherein the pharmaceutical carrier comprises water, a sweetening agent, and a flavoring agent.

Claim 10

A method of treating and preventing bacterial and other microbiological infections in humans and lower animals in need of such treatment, comprising administering to the human or lower animal a therapeutically effective amount of the composition of Claim 6.