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    • 5. 发明授权
    • Tri-, tetra-substituted-3-aminopyrrolidine derivative
    • 三取代的3-氨基吡咯烷衍生物
    • US07563805B2
    • 2009-07-21
    • US11413153
    • 2006-04-28
    • Hisashi TakahashiHiroaki InagakiSatoshi KomoriyaMakoto TakemuraRie Miyauchi
    • Hisashi TakahashiHiroaki InagakiSatoshi KomoriyaMakoto TakemuraRie Miyauchi
    • A01N43/42A61K31/47C07D215/00
    • C07D207/14Y02P20/55
    • A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):
    • 提供喹诺酮合成抗菌剂和用于感染的治疗剂,其对革兰氏阳性和革兰氏阴性细菌都具有广谱和强抗菌活性,并且也是高度安全的。 所提供的化合物由下式(I)表示:其中R1和R2表示氢原子等; R3表示含有1〜6个碳原子的烷基等; R4和R5独立地表示氢原子,含有1至6个碳原子的烷基等,条件是R4和R5不同时表示氢原子; 取代基R 4和R 5一起表示(a)包含由R 4和R 5共有的碳原子与吡咯烷环形成螺环结构的3至6元环状结构; R6和R7独立地表示氢原子,含有1至6个碳原子的烷基等; R8表示含有1〜6个碳原子的卤素取代的烷基等; X1表示氢原子或卤素原子; A表示氮原子或由式(II)表示的部分:
    • 7. 发明申请
    • Tri-, tetra-substituted-3-aminopyrrolidine derivative
    • 三取代的3-氨基吡咯烷衍生物
    • US20060264428A1
    • 2006-11-23
    • US11413153
    • 2006-04-28
    • Hisashi TakahashiHiroaki InagakiSatoshi KomoriyaMakoto TakemuraRie Miyauchi
    • Hisashi TakahashiHiroaki InagakiSatoshi KomoriyaMakoto TakemuraRie Miyauchi
    • A61K31/538A61K31/4745A61K31/4709C07D491/14C07D471/02C07D403/02
    • C07D207/14Y02P20/55
    • A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):
    • 提供喹诺酮合成抗菌剂和用于感染的治疗剂,其对革兰氏阳性和革兰氏阴性细菌都具有广谱和强抗菌活性,并且也是高度安全的。 所提供的化合物由下式(I)表示:其中R 1和R 2代表氢原子等; R 3表示含有1至6个碳原子的烷基等; R 4和R 5独立地表示氢原子,含有1至6个碳原子的烷基等,条件是R 4 O >和R 5不同时表示氢原子; 或取代基R 4和R 5一起表示(a)包含由R 4共享的碳原子的3至6元环结构 和R 5与吡咯烷环形成螺环结构; R 6和R 7独立地表示氢原子,含有1至6个碳原子的烷基等; R 8表示含有1至6个碳原子的卤素取代的烷基等; X 1表示氢原子或卤素原子; A表示氮原子或由式(II)表示的部分: