发明名称 Combination therapy to treat <i>Mycobacterium </i>diseases
摘要 The present invention relates to a compound of formula (I); or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.
申请公布号 US9572809(B2) 申请公布日期 2017.02.21
申请号 US201313942342 申请日期 2013.07.15
申请人 SPERO TRINEM, INC. 发明人 Locher Christopher Phillip;Bennani Youssef Laafiret;Grillot Anne-Laure;O'Dowd Hardwin;Perola Emanuele;Le Tiran Arnaud;Charifson Paul S.
分类号 A61K31/34;A61K31/4168;A61K31/506;A61K45/06;A61K31/132;A61K31/454;A61K31/47;A61K31/496;A61K31/4965;A61K31/498;A61K31/5377;A61K31/4709;A61K31/675 主分类号 A61K31/34
代理机构 Cantor Colburn LLP 代理人 Cantor Colburn LLP
主权项 1. A method of controlling, treating or reducing the advancement, severity or effects of a mycobacterium disease comprising administering to a patient in need thereof a therapeutically effective amount of: (a) a compound of formulawherein R is hydrogen or fluorine; X is hydrogen, —PO(OH)2, —PO(OH)O−M+, —PO(O−)2.2M+, or —PO(O−)2.D2+; M+ is a pharmaceutically acceptable monovalent cation; and D2+ is a pharmaceutically acceptable divalent cation; or a pharmaceutically acceptable salt thereof; in combination with: (b) one or more antibiotic compounds comprising a diarylquinolone, rifapentine, rifalazil, a nitroimidazole, a benzothiazinone, capreomycin, clofazimine, cycloserine, dapsone, a thiocarbamide, ethambutol, DC-159a, a nitrobenzthiazole, sutezolid (PNU-100480), AZD-5847, posizolid (AZD-2563), para-aminosalicylic acid, SQ-109, SQ-609, a capuramycin, a caprazene nucleoside, an isothiazoloquinolone, thioridazine, thiacetazone, dirithromycin, roxithromycin, telithromycin, azithromycin, clarithromycin, erythromycin, amikacin, kanamycin, streptomycin, levofloxacin, moxifloxacin, gatifloxacin, linezolid, rifalazil, meropenem, clavulanate, PA 824, pyrazinamide, TMC-207, oxazolidinine, nitroimidazole, or isoniazid, with the proviso that when the one or more antibiotic compounds is thioridazine, azithromycin, clarithromycin, erythromycin, amikacin, kanamycin, streptomycin, levofloxacin, moxifloxacin, gatifloxacin, linezolid, rifalazil, meropenem, clavulanate, or isoniazid, then an additional antibiotic is also present in the combination.
地址 Cambridge MA US
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