发明名称 Methods for treating resistant diseases using triazole containing macrolides
摘要 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.
申请公布号 US8796232(B2) 申请公布日期 2014.08.05
申请号 US200913125555 申请日期 2009.10.24
申请人 Cempra Pharmaceuticals, Inc. 发明人 Fernandes Prabhavathi B.;Pereira David E.
分类号 A61K31/70 主分类号 A61K31/70
代理机构 Barnes & Thornburg LLP 代理人 Barnes & Thornburg LLP
主权项 1. 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 formulaor 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.
地址 Chapel Hill NC US