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US 2019/0054059 A1Published application
Parenteral formulations of macrolide antibiotics
AssigneeCempra Pharmaceuticals, Inc.
InventorsDavid Eugene PEREIRA, Prabhavathi FERNANDES
Life of this patent
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Abstract
Described herein are pharmaceutical compositions adapted for the parenteral administration of macrolide antibiotics, such as triazole-containing and fluoroketolide antibiotics. Also described herein are methods for their use in the treatment of bacterial, protozoal, and other infections.
Claims20
A pharmaceutical composition adapted for parenteral administration comprising one or more antibacterial compounds of the formula
- or a pharmaceutically acceptable salt thereof, and combinations thereof, wherein:
- R10 is hydrogen or acyl;
- X is H;
- and Y is OR7;
- where R7 is a monosaccharide or disaccharide, alkyl, aryl, heteroaryl, acyl, or C(O)NR8R9, where R8 and R9 are each independently selected from the group consisting of hydrogen, hydroxy, alkyl, aralkyl, alkylaryl, heteroalkyl, aryl, heteroaryl, alkoxy, dimethylaminoalkyl, acyl, sulfonyl, ureido, and carbamoyl;
- or X and Y are taken together with the attached carbon to form carbonyl;
- V is C(O), C(═NR11), CH(NR12, R13), or —N(R14)CH2, where N(R14) is attached to the C-10 carbon of the compound;
- wherein R11 is hydroxy or alkoxy, R12 and R13 are each independently selected from the group consisting of hydrogen, hydroxy, alkyl, aralkyl, alkylaryl, alkoxy, heteroalkyl, aryl, heteroaryl, dimethylaminoalkyl, acyl, sulfonyl, ureido, and carbamoyl;
- R14 is hydrogen, hydroxy, alkyl, aralkyl, alkylaryl, alkoxy, heteroalkyl, aryl, heteroaryl, dimethylaminoalkyl, acyl, sulfonyl, ureido, or carbamoyl;
- W is H, F, Cl, Br, I, or OH;
- A is CH2, C(O), C(O)O, C(O)NH, S(O)2, S(O)2NH, C(O)NHS(O)2;
- B is (CH2)n where n is an integer ranging from 0-10, or B is an unsaturated carbon chain of 2-10 carbons;
- and
- C is hydrogen, hydroxy, alkyl, aralkyl, alkylaryl, alkoxy, heteroalkyl, aryl, heteroaryl, aminoaryl, alkylaminoaryl, acyl, acyloxy, sulfonyl, ureido, or carbamoyl;
- and
- a tartaric acid or a salt thereof.
13 more elements
2-76. (canceled)
Dependencies are inferred from the claim text.