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US 8,796,232 B2Granted
Methods for treating resistant diseases using triazole containing macrolides
AssigneeCempra Pharmaceuticals, Inc.
InventorsPrabhavathi B. Fernandes, David E. Pereira
Life of this patent
Estimating the term…
Abstract
Triazole-containing macrolide and ketolide antibiotics, therapeutic compositions containing them and methods of use for treating diseases caused by one or more resistant organisms are described.
Claims30
A method for inhibiting the growth of bacteria in a host animal, having the bacteria that is resistant to one or more penicillins, cephalosporins, quinolones, macrolides, vancomycin, or a combination thereof, the method comprising the step of administering to the host animal an effective amount of a compound of the formula
- or pharmaceutically acceptable salt thereof, wherein:
- R10 is hydrogen or acyl;
- X is H;
- and Y is OR7;
- where R7 is monosaccharide, disaccharide, alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted, or acyl or C(O)NR8R9;
- where R8 and R9 are each independently selected from the group consisting of hydrogen, hydroxy, alkyl, heteroalkyl, alkoxy, aryl, arylalkyl, heteroaryl, and heteroarylalkyl, each of which is optionally substituted, and 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;
- where R11 is hydroxy or alkoxy;
- R12 and R13 are each independently selected from the group consisting of hydrogen, hydroxy, alkyl, alkoxy, heteroalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl, each of which is optionally substituted, and dimethylaminoalkyl, acyl, sulfonyl, ureido, and carbamoyl;
- R14 is hydrogen, hydroxy, alkyl, alkoxy, heteroalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, each of which is optionally substituted, or 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, or C(O)NHS(O)2;
- B is (CH2)n where n is an integer from 0 to 10;
- or an unsaturated carbon chain of 2 to 10 carbons;
- and
- C is hydrogen, hydroxy, alkyl, alkoxy, heteroalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, each of which is optionally substituted, or acyl, acyloxy, sulfonyl, ureido, or carbamoyl, where C is other than 2-pyridinyl;
- or an antibacterial composition thereof further comprising one or more pharmaceutically acceptable carriers, excipients, or diluents therefor, or a combination thereof.
16 more elements
Dependencies are inferred from the claim text.