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1. 发明申请

US20090012119A1 FLUOROALKYLPYRROLIDINE DERIVATIVE 审中-公开
标题翻译：氟代甲基吡咯烷衍生物
公开(公告)号：US20090012119A1
公开(公告)日：2009-01-08
申请号：US11813950
申请日：2006-01-20
申请人： Hisashi Takahasi , Rie Miyauchi , Makoto Takemura
发明人： Hisashi Takahasi , Rie Miyauchi , Makoto Takemura
IPC分类号： A61K31/4709 , C07D401/02 , A61P3/04
CPC分类号： C07D401/04
摘要： This invention relates to a compound represented by the following formula (1):[F.1] its salt or a hydrate thereof. R1 represents hydrogen atom, an optionally substituted alkyl group containing 1 to 6 carbon atoms, a cycloalkyl group containing 3 to 6 carbon atoms, or a substituted carbonyl group derived from an amino acid, a dipeptide, or a tripeptide; R2 represents hydrogen atom, an optionally substituted alkyl group containing 1 to 6 carbon atoms, or a cycloalkyl group containing 3 to 6 carbon atoms; R3 represents an alkyl group containing 1 to 6 carbon atoms or a halogen-substituted alkyl group containing 1 to 6 carbon atoms; R4 represents a cycloalkyl group containing 3 to 6 carbon atoms or a halogen-substituted cycloalkyl group containing 3 to 6 carbon atoms; R5 represents hydrogen atom, phenyl group, acetoxymethyl group, pivaloyloxymethyl group, ethoxycarbonyl group, choline group, dimethylaminoethyl group, 5-indanyl group, phthalidyl group, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, 3-acetoxy-2-oxobutyl group, or a phenylalkyl group comprising an alkylene group containing 1 to 6 carbon atoms and phenyl group; X1 and X2 independently represent hydrogen atom or a halogen atom; and X represents hydrogen atom or a halogen atom. This compound exhibits broad and strong antibacterial activity to both Gram positive and Gram negative bacteria as well as high safety, and therefore, this compound is useful as a quinolone antibacterial drug, and a prophylactic and/or therapeutic drug for an infectious disease.
摘要翻译：本发明涉及由下式（1）表示的化合物：[F.1]其盐或其水合物。 R1表示氢原子，含有1-6个碳原子的任意取代的烷基，含有3-6个碳原子的环烷基或衍生自氨基酸，二肽或三肽的取代的羰基; R2表示氢原子，可以具有取代基的碳原子数为1〜6的烷基或碳原子数为3〜6的环烷基。 R3表示含有1至6个碳原子的烷基或含有1至6个碳原子的卤素取代的烷基; R 4表示碳原子数3〜6的环烷基或碳原子数3〜6的卤素取代环烷基。 R5表示氢原子，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，胆碱基，二甲基氨基乙基，5-二氢化茚基，苯酞基，5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基， 3-乙酰氧基-2-氧代丁基或含有1〜6个碳原子的亚烷基的苯基烷基和苯基; X1和X2独立地表示氢原子或卤原子; X表示氢原子或卤原子。该化合物对革兰氏阳性和革兰氏阴性细菌具有广泛和强的抗菌活性以及高安全性，因此该化合物可用作喹诺酮抗菌药物，以及用于感染性疾病的预防和/或治疗药物。

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