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CAPLUS COPYRIGHT 2012 ACS
||Preparation of pyrimidinyltetrahydrofuranylbenzimidazolylurea derivatives for use as gyrase and topoisomerase IV inhibitors useful in treatment of bacterial infections
||Le Tiran, Arnaud; Grillot, Anne-Laure; Charifson, Paul S.; Bennani, Youssef Laafiret; O'Dowd, Hardwin; Perola, Emanuele
||Vertex Pharmaceuticals Incorporated, USA
||PCT Int. Appl., 149pp. CODEN: PIXXD2
Title compds. I [X = H, PO(OH)2, PO(OH)O-M+, PO(O-)2-2M+, or PO(O-)2-D2+; R1 = H or F; M+ = pharmaceutically acceptable monovalent cation; D2+ = pharmaceutically acceptable divalent cation], and their pharmaceutically acceptable salts, are prepared and disclosed as gyrase and topoisomerase IV inhibitors useful in treatment of bacterial infections. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated in MIC90 assays (data given).
Please note: Titles and abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced both the abstract and title using additional information found in the patent. The original title of the PCT publication is Pyrimidine gyrase and topoisomerase IV inhibitors. For the CAplus record, this title was enhanced to read Preparation of pyrimidinyltetrahydrofuranylbenzimidazolylurea derivatives for use as gyrase and topoisomerase IV inhibitors useful in treatment of bacterial infections.
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