1-Cyclopropyl-6-fluoro-7-[3-(1,2,3-triazol-1-yl) pyrrolidin-1-yl]-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid | 168959-30-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 1-Cyclopropyl-6-fluoro-7-[3-(1,2,3-triazol-1-yl) pyrrolidin-1-yl]-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid
• 英文别名: 1-Cyclopropyl-6-fluoro-8-methoxy-4-oxo-7-[3-(triazol-1-yl)pyrrolidin-1-yl]quinoline-3-carboxylic acid
• CAS: 168959-30-6
• 化学式: C₂₀H₂₀FN₅O₄
• 分子量: 413.408
• InChiKey: TVXONVWWGIXZKT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  101
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸乙酯 、 氟硼酸 、 3-(1,2,3-triazol-1-yl)pyrrolidine 以to yield the desired product, m.p. 200°-201° C的产率得到1-Cyclopropyl-6-fluoro-7-[3-(1,2,3-triazol-1-yl) pyrrolidin-1-yl]-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid
  参考文献：
  名称：

  7-substituted-6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid

  摘要：

  取代的喹啉化合物及其中间体，制备这些化合物和中间体的过程，使用这些化合物的制药组合物，使用这些化合物治疗细菌感染的方法，以及使用这些化合物进行消毒的方法。

  公开号：

  US05342846A1

文献信息

• [DE] HERBIZIDE 3-(BENZAZOL-4-YL)PYRIMIDINDION-DERIVATE<br/>[EN] HERBICIDES 3-(BENZAZOL-4-YL)PYRIMIDINE-DIONE-DERIVATIVES<br/>[FR] DERIVES DE 3-(BENZAZOL-4-YLE)DIONE DE PYRIMIDINE HERBICIDES
  申请人：BASF AKTIENGESELLSCHAFT

  公开号：WO1999031091A1

  公开（公告）日：1999-06-24

  (DE) 3-(Benzazol-4-yl)pyrimidindion-Derivate der Formel (I) und deren Salze, wobei X = O, S; R1 = H, NH2, C1-C6-Alkyl, C1-C6-Halogenalkyl; R2 = H, Halogen, C1-C6-Alkyl, C1-C6-Halogenalkyl, C1-C6-Alkylthio, C1-C6-Alkylsulfinyl, C1-C6-Alkylsulfonyl; R3 = H, Halogen, C1-C6-Alkyl; R4 = H, Halogen; R5 = CN, Halogen, C1-C6-Alkyl, C1-C6-Halogenalkyl, C1-C6-Alkoxy, C1-C6-Halogenalkoxy; =Y- = eine Gruppe =N-N(R6)-, =C(ZR7)-N(R6)-, =C(ZR7)-O-, =C(ZR7)-S-; R6 = C1-C6-Alkyl, C1-C4-Halogenalkyl, C3-C6-Cycloalkyl, C3-C6-Alkenyl, C3-C6-Alkinyl, C1-C6-Alkyl-SO2, C1-C6-Alkyl-CO, C1-C6-Halogenalkyl-CO, C1-C6-Alkyl-CS, C1-C6-Alkoxy-CO, C1-C6-Alkoxy-CS oder gegebenenfalls substituiertes C1-C6-Alkyl; Z = chemische Bindung, O, S, -S(O)-, -SO2-, -NH-, -N(R8)-; R7, R8 = C1-C6-Alkyl, C1-C6-Halogenalkyl, Hydroxy-C1-C4-alkyl, Cyano-C1-C4-alkyl, C1-C4-Alkoxy-C1-C4-alkyl, C1-C4-Halogenalkoxy-C1-C4-alkyl, C3-C4-Alkenyloxy-C1-C4-alkyl, C3-C4-Alkinyloxy-C1-C4-alkyl, C3-C8-Cycloalkoxy-C1-C4-alkyl, Amino-C1-C4-alkyl, C1-C4-Alkylamino-C1-C4-alkyl, Di(C1-C4-alkyl)amino-C1-C4-alkyl, C1-C4-Alkylthio-C1-C4-alkyl, C1-C4-Halogenalkylthio-C1-C4-alkyl, C3-C4-Alkenylthio-C1-C4-alkyl, C3-C4-Alkinylthio-C1-C4-alkyl, C1-C4-Alkylsulfinyl-C1-C4-alkyl, C1-C4-Halogenalkylsulfinyl-C1-C4-alkyl, C3-C4-Alkenylsulfinyl-C1-C4-alkyl, C3-C4-Alkinylsulfinyl-C1-C4-alkyl, C1-C4-Alkylsulfonyl-C1-C4-alkyl, C1-C4-Halogenalkylsulfonyl-C1-C4-alkyl, C3-C4-Alkenylsulfonyl-C1-C4-alkyl, C3-C4-Alkinylsulfonyl-C1-C4-alkyl, C3-C6-Alkenyl, Cyano-C3-C6-alkenyl, C3-C6-Halogenalkenyl, C3-C6-Alkinyl, Cyano-C3-C6-alkinyl, C3-C6-Halogenalkinyl, HO-CO-C1-C4-alkyl, (C1-C4-Alkoxy)CO-C1-C4-alkyl, (C1-C4-Alkyl-)CS-C1-C4-alkyl, H2N-CO-C1-C4-alkyl, C1-C4-Alkyl-NHCO-C1-C4-alkyl, Di(C1-C4-alkyl)NCO-C1-C4-alkyl, Di(C1-C4-alkyl)phosphonyl-C1-C4-alkyl, gegebenenfalls substituiertes C3-C8-Cyclo-alkyl, C3-C8-Cycloalkyl-C1-C4-alkyl, Phenyl, Phenyl-C1-C4-alkyl, 3- bis 7-gliedriges Heterocyclyl oder Heterocyclyl-C1-C4-alkyl, wobei jeder Heterocyclyl-Ring ein CO- oder CS-Ringglied enthalten kann, oder, sofern Z = chemische Bindung, R7 auch H, OH, CN, SH, NH2, Halogen, -CH(OH)-CH2-R9, -CH(Halogen)-CH2-R9, -CH2-CH(Halogen)-R9, -CH=CH-R9 oder -CH=C(Halogen)-R9, wobei R9 = COOH, (C1-C4-Alkoxy)carbonyl, (C1-C4-Alkythio)carbonyl, CONH2, C1-C4-Alkyl-NHCO oder Di(C1-C4-alkyl)NCO, oder R7 + R8 = gegebenenfalls substituierte 1,3-Propylen- ,Tetramethylen-, Pentamethylen- oder Ethylenoxyethylen-Kette.(EN) The invention relates to 3-(benzazol-4-yl)pyrimidine-dione-derivatives of formula (I) and the salts thereof, whereby X = O, S; R1 = H, NH2, C1-C6-alkyl, C1-C6-alkyl halide; R2 = H, halogen, C1-C6-alkyl, C1-C6-alkyl halide, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl; R3 = H, halogen, C1-C6-alkyl; R4 = H, halogen; R5 = CN, halogen, C1-C6-alkyl, C1-C6-alkyl halide, C1-C6-alkoxyl, C1-C6-alkoxyl halide; =Y- = a group =N-N(R6)-, =C(ZR7)-N(R6)-, =C(ZR7)-O-, =C(ZR7)-S-; R6 = C1-C6-alkyl, C1-C4-alkyl halide, C3-C6-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, C1-C6-alkyl-SO2, C1-C6-alkyl-CO, C1-C6-alkyl halide-CO, C1-C6-alkyl-CS, C1-C6-alkoxyl-CO, C1-C6-alkoxyl-CS or optionally substituted C1-C6-alkyl; Z = chemical bond, O, S, -S(O)-, -SO2-, -NH-, -N(R8)-; R7, R8 = C1-C6-alkyl, C1-C6-alkyl halide, hydroxy-C1-C4-alkyl, cyano-C1-C4-alkyl, C1-C4-alkoxyl-C1-C4-alkyl, C1-C4-alkoxyl halide-C1-C4-alkyl, C3-C4-alkenyloxyl-C1-C4-alkyl, C3-C4-alkynyloxyl-C1-C4-alkyl, C3-C8-cycloalkoxyl-C1-C4-alkyl, amino-C1-C4-alkyl, C1-C4-alkylamino-C1-C4-alkyl, di(C1-C4-alkyl)amino-C1-C4-alkyl, C1-C4-alkylthio-C1-C4-alkyl, C1-C4-alkylthio halide-C1-C4-alkyl, C3-C4-alkenylthio-C1-C4-alkyl, C3-C4-alkynylthio-C1-C4-alkyl, C1-C4-alkylsulfinyl-C1-C4-alkyl, C1-C4-alkylsulfinyl halide-C1-C4-alkyl, C3-C4-alkenylsulfinyl-C1-C4-alkyl, C3-C4-alkynylsulfinyl-C1-C4-alkyl, C3-C6-alkenyl, cyano-C3-C6-alkenyl, C3-C6-alkenyl halide, C3-C6-alkynyl, cyano-C3-C6-alkynyl, C3-C6-alkynyl halide, HO-CO-C1-C4-alkyl, (C1-C4-alkoxyl)CO-C1-C4-alkyl, (C1-C4-alkyl)CS-C1-C4-alkyl, H2N-CO-C1-C4-alkyl, C1-C4-alkyl-NHCO-C1-C4-alkyl, di(C1-C4-alkyl)NCO-C1-C4-alkyl, di(C1-C4-alkyl)phosphonyl-C1-C4-alkyl, optionally substituted C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, phenyl, phenyl-C1-C4-alkyl, 3- to 7-linked heterocyclyl or heterocyclyl-C1-C4-alkyl, whereby each heterocyclyl ring can contain a CO-ring link or CS-ring link, or provided that Z = chemical bond, R7 also H, OH, CN, SH, NH2, halogen, -CH(OH)-CH2-R9, -CH(halogen)-CH2-R9, -CH2-CH(halogen)-R9, -CH=CH-R9 or -CH=C(halogen)-R9, whereby R9 = COOH, (C1-C4-alkoxyl)carbonyl, (C1-C4-alkylthio)carbonyl, CONH2, C1-C4-alkyl-NHCO or di(C1-C4-alkyl)NCO, or R7 + R8 = an optionally substituted 1,3-propylene-, tetramethylene-, pentamethylene- or ethylene oxyethylene-chain.(FR) L'invention concerne des dérivés 3-(benzazol-4-yle)dione de pyrimidine de la formule (I) et leurs sels. Dans cette formule, X = O, S; R1 = H, NH2, alkyle C1-C6, halogénure d'alkyle C1-C6; R2 = H, halogène, alkyle C1-C6, halogénure d'alkyle, alkylthio C1-C6, alkylsulfinyle C1-C6, alkylsulfonyle C1-C6; R3 = H, halogène, alkyle C1-C6; R4 = H, halogène; R5 = CN, halogène, alkyle C1-C6, halogénure d'alkyle C1-C6, alcoxy C1-C6, halogénure d'alcoxy C1-C6; =Y- = un groupe =N-N(R6)-, =C(ZR7)-N(R6)-, =C(ZR7)-O-, =C(ZR7)-S-; R6 = alkyle C1-C6, halogénure d'alkyle C1-C4, cycloalkyle C3-C6, alkényle C3-C6, alkinyle C3-C6, alkyle C1-C6-SO2, alkyle C1-C6-CO, halogénure d'alkyle C1-C6-CO, alkyle C1-C6-CS, alcoxy C1-C6-CO, alcoxy C1-C6-CS ou alkyle C1-C6 éventuellement substitué; Z = liaison chimique, O, S, -S(O)-, -SO2-, -NH-, -N(R8)-; R7, R8 = alkyle C1-C6, halogénure d'alkyle C1-C6, hydroxy-alkyle C1-C4, cyano-alkyle C1-C4, alcoxy C1-C4-alkyle C1-C4, halogénure d'alcoxy C1-C4-alkyle C1-C4, alkényloxy C3-C4-alkyle C1-C4, alkinyloxy C3-C4-alkyle C1-C4, cycloalkoxy C3-C8-alkyle C1-C4, amino-alkyle C1-C4, alkylamino C1-C4-alkyle C1-C4, di(alkyle C1-C4)amino-alkyle C1-C4, alkylthio C1-C4-alkyle C1-C4, halogénure d'alkylthio C1-C4, alkénylthio C3-C4-alkyle C1-C4, alkinylthio C3-C4-alkyle C1-C4, alkylsulfinyle C1-C4-alkyle C1-C4, halogénure d'alkylsulfinyle C1-C4-alkyle C1-C4-alkénylsulfinyle C3-C4-alkyle C1-C4, alkinylsulfinyle C3-C4-alkyle C1-C4, alkylsulfonyle C1-C4-alkyle C1-C4, halogénure d'alkylsulfonyle C1-C4-alkyle C1-C4, alkénylsulfonyle C3-C4-alkyle C1-C4, alkinylsulfonyle C3-C4-alkyle C1-C4, alkényle C3-C6, cyano-alkényle C3-C6, halogénure d'alkényle C3-C6, alkinyle C3-C6, cyano-alkinyle C3-C6, halogénure d'alkinyle C3-C6, HO-CO-alkyle C1-C4, (alcoxy C1-C4)CO-alkyle C1-C4, (alkyle C1-C4)CS-alkyle C1-C4, H2N-CO-alkyle C1-C4, alkyle C1-C4-NHCO-alkyle C1-C4, di(alkyle C1-C4)NCO-alkyle C1-C4, di(alkyle C1-C4)phosphonyle-alkyle C1-C4, cycloalkyle C3-C8 éventuellement substitué, cycloalkyle C3-C8-alkyle C1-C4, phényle, phényle-alkyle C1-C4, hétérocyclyle ayant entre 3 et 7 chaînons ou hétérocyclyle-alkyle C1-C4, chaque composé hétérocyclyle pouvant contenir un chaînon cyclique CS, ou si Z = liaison chimique, R7 désigne également H, OH, CN, SH, NH2, halogène, -CH(OH)-CH2-R9, -CH(halogène)-R9, R9 = COOH, (alcoxy C1-C4)carbonyle, (alkylthio C1-C4)carbonyle, CONH2, alkyle C1-C4-NHCO ou di(alkyle C1-C4)NCO, ou R7 + R8 = chaîne de 1,3-propylène-tétraméthylène, de pentaméthylène ou d'oxyéthylène d'éthylène, éventuellement substituée.

  （DE）本发明涉及具有式（I）的3-(苯并杂环-4-基)嘧啶二酮衍生物及其盐，其中X=O，S；R₁=H，NH₂，C₁-C₆烷基，C₁-C₆卤代烷基；R₂=H，卤素，C₁-C₆烷基，C₁-C₆卤代烷基，C₁-C₆烷硫基，C₁-C₆亚磺酰基，C₁-C₆磺酰基；R₃=H，卤素，C₁-C₆烷基；R₄=H，卤素；R₅=CN，卤素，C₁-C₆烷基，C₁-C₆卤代烷基，C₁-C₆烷氧基，C₁-C₆卤代烷氧基；=Y-为=N-N(R₆)-，=C(ZR₇)-N(R₆)-，=C(ZR₇)-O-，=C(ZR₇)-S-；R₆=C₁-C₆烷基，C₁-C₄卤代烷基，C₃-C₆环烷基，C₃-C₆烯基，C₃-C₆炔基，C₁-C₆烷基-SO₂，C₁-C₆烷基-CO，C₁-C₆卤代烷基-CO，C₁-C₆烷基-CS，C₁-C₆烷氧基-CO，C₁-C₆烷氧基-CS或C₁-C₆烷基（任选取代）；Z=化学键，O，S，-S(O)-，-SO₂-，-NH-，-N(R₈)-；R₇，R₈=C₁-C₆烷基，C₁-C₆卤代烷基，羟基-C₁-C₄烷基，氰基-C₁-C₄烷基，C₁-C₄烷氧基-C₁-C₄烷基，C₁-C₄卤代烷氧基-C₁-C₄烷基，C₃-C₄烯氧基-C₁-C₄烷基，C₃-C₄炔氧基-C₁-C₄烷基，C₃-C₈环烷氧基-C₁-C₄烷基，氨基-C₁-C₄烷基，C₁-C₄烷氨基-C₁-C₄烷基，二(C₁-C₄烷基)氨基-C₁-C₄烷基，C₁-C₄烷硫基-C₁-C₄烷基，C₁-C₄卤代烷硫基-C₁-C₄烷基，C₃-C₄烯硫基-C₁-C₄烷基，C₃-C₄炔硫基-C₄烷基，C₁-C₄烷亚磺基-C₁-C₄烷基，C₁-C₄卤代烷亚磺基-C₁-C₄烷基，C₃-C₄烯亚磺基-C₁-C₄烷基，C₃-C₄炔亚磺基-C₁-C₄烷基，C₁-C₄烷磺基-C₁-C₄烷基，C₁-C₄卤代烷磺基-C₁-C₄烷基，C₃-C₄烯磺基-C₁-C₄烷基，C₃-C₄炔磺基-C₁-C₄烷基，C₃-C₆烯基，氰基-C₃-C₆烯基，C₃-C₆卤代烯基，C₃-C₆炔基，氰基-C₃-C₆炔基，C₃-C₆卤代炔基，HO-CO-C₁-C₄烷基，(C₁-C₄烷氧基)CO-C₁-C₄烷基，(C₁-C₄烷基)CS-C₁-C₄烷基，H₂N-CO-C₁-C₄烷基，C₁-十一烷基-NHCO-C₁-C₄烷基，二(C₁-C₄烷基)NCO-C₁-C₄烷基，二(C₁-C₄烷基)磷酸基-C₁-C₄烷基，C₃-C₈环烷基（任选取代），C₃-C₈环烷基-C₁-C₄烷基，苯基，苯基-C₁-C₄烷基，3-至7-员杂环基或杂环基-C₁-C₄烷基，其中每个杂环基环可含一个CO-环键或CS-环键；或者，若Z=化学键，R₇还可为H，OH，CN，SH，NH₂，卤素，-CH(OH)-CH₂-R₉，-CH(卤素)-CH₂-R₉，-CH₂-CH(卤素)-R₉，-CH=CH-R₉或-CH=C(卤素)-R₉，其中R₉=COOH，(C₁-C₄烷氧基)羰基，(C₁-C₄烷硫基)羰基，CONH₂，C₁-C₄烷基-NHCO，或二(C₁-C₄烷基)NCO；或R₇+R₈=任选取代的1,3-丙二烯基，四亚甲基，五亚甲基或氧二亚甲基链。 （EN）发明涉及式(I)的3-(苯并杂环-4-基)嘧啶二酮衍生物及其盐，其中X=O，S；R₁=H，NH₂，C₁-C₆烷基，C₁-C₆卤代烷基；R₂=H，卤素，C₁-C₆烷基，C₁-C₆卤代烷基，C₁-C₆烷硫基，C₁-C₆亚磺酰基，C₁-C₆磺酰基；R₃=H，卤素，C₁-C₆烷基；R₄=H，卤素；R₅=CN，卤素，C₁-C₆烷基，C₁-C₆卤代烷基，C₁-C₆烷氧基，C₁-C₆卤代烷氧基；=Y-为=N-N(R₆)-，=C(ZR₇)-N(R₆)-，=C(ZR₇)-O-，=C(ZR₇)-S-；R₆=C₁-C₆烷基，C₁-C₄卤代烷基，C₃-C₆环烷基，C₃-C₆烯基，C₃-C₆炔基，C₁-C₆烷基-SO₂，C₁-C₆烷基-CO，C₁-C₆卤代烷基-CO，C₁-C₆烷基-CS，C₁-C₆烷氧基-CO，C₁-C₆烷氧基-CS或C₁-C₆烷基（任选取代）；Z=化学键，O，S，-S(O)-，-SO₂-，-NH-，-N(R₈)-；R₇，R₈=C₁-C₆烷基，C₁-C₆卤代烷基，羟基-C₁-C₄烷基，氰基-C₁-C₄烷基，C₁-C₄烷氧基-C₁-C₄烷基，C₁-C₄卤代烷氧基-C₁-C₄烷基，C₃-C₄烯氧基-C₁-C₄烷基，C₃-C₄炔氧基-C₁-C₄烷基，C₃-C₈环烷氧基-C₁-C₄烷基，氨基-C₁-C₄烷基，C₁-C₄烷氨基-C₁-C₄烷基，二(C₁-C₄烷基)氨基-C₁-C₄烷基，C₁-C₄烷硫基-C₁-C⁻烷基，C₁-C₄卤代烷硫基-C₁-C₄烷基，C₃-C₄烯硫基-C₁-C₄烷基，C₃-C₄炔硫基-C₁-C₄烷基，C₁-C₄烷亚磺基-C₁-C₄烷基，C₁-C₄卤代烷亚磺基-C₁-C₄烷基，C₃-C₄烯亚磺基-C₁-C₄烷基，C₃-C₄炔亚磺基-C₁-C₄烷基，C₁-C₄烷磺基-C₁-C₄烷基，C₁-C₄卤代烷磺基-C₁-C₄烷基，C₃-C₄烯磺基-C₁-C₄烷基，C₃-C₄炔磺基-C₁-C₄烷基，C₃-C₆烯基，氰基-C₃-C₆烯基，C₃-C₆卤代烯基，C₃-C₆炔基，氰基-C₃-C₆炔基，C₃-C₆卤代炔基，HO-CO-C₁-C₄烷基，(C₁-C₄烷氧基)CO-C₁-C₄烷基，(C₁-C₄烷基)CS-C₁-C₄烷基，H₂N-CO-C₁-C₄烷基，C₁-C₄烷基-NHCO-C₁-C₄烷基，二(C₁-C₄烷基)NCO-C₁-C₄烷基，二(C₁-C₄烷基)磷酸基-C₁-C₄烷基，C₃-C₈环烷基（任选取代），C₃-C₈环烷基-C₁-C₄烷基，苯基，苯基-C₁-C₄烷基，3-至7-员杂环基或杂环基-C₁-C₄烷基，其中每个杂环基环可含一个CO-环键或CS-环键；或者，若Z=化学键，R₇还可为H，OH，CN，SH，NH₂，卤素，-CH(OH)-CH₂-R₉，-CH(卤素)-CH₂-R₉，-CH₂-CH(卤素)-R₉，-CH=CH-R₉或-CH=C(卤素)-R₉，其中R₉=COOH，(C₁-C₄烷氧基)羰基，(C₁-C₄烷硫基)羰基，CONH₂，C₁-C₄烷基-NHCO，或二(C₁-C₄烷基)NCO；或R₇+R₈=任选取代的1,3-丙二烯基，四亚甲基，五亚甲基或氧二亚甲基链。 （FR）发明涉及式(I)的3-(苯并杂环-4-基)嘧啶二酮衍生物及其盐，其中X=O，S；R₁=H，NH₂，C₁-C₆烷基，C₁-C₆卤代烷基；R₂=H，卤素，C₁-C₆烷基，C₁-C₆卤代烷基，C₁-C₆烷硫基，C₁-C₆亚磺酰基，C₁-C₆磺酰基；R₃=H，卤素，C₁-C₆烷基；R₄=H，卤素；R₅=CN，卤素，C₁-C₆烷基，C₁-C₆卤代烷基，C₁-C₆烷氧基，C₁-C₆卤代烷氧基；=Y-为=N-N(R₆)-，=C(ZR₇)-N(R₆)-，=C(ZR₇)-O-，=C(ZR₇)-S-；R₆=C₁-C₆烷基，C₁-C₄卤代烷基，C₃-C₆环烷基，C₃-C₆烯基，C₃-C₆炔基，C₁-C₆烷基-SO₂，C₁-C₆烷基-CO，C₁-C₆卤代烷基-CO，C₁-C₆烷基-CS，C₁-C₆烷氧基-CO，C₁-C₆烷氧基-CS或C₁-C₆烷基（任选取代）；Z=化学键，O，S，-S(O)-，-SO₂-，-NH-，-N(R₈)-；R₇，R₈=C₁-C₆烷基，C₁-C₆卤代烷基，羟基-C₁-C₄烷基，氰基-C₁-C₄烷基，C₁-C₄烷氧基-C₁-C₄烷基，C₁-C₄卤代烷氧基-C₁-C₄烷基，C₃-C₄烯氧基-C₁-C₄烷基，C₃-C₄炔氧基-C₁-C₄烷基，C₃-C₈环烷氧基-C₁-C₄烷基，氨基-C₁-C₄烷基，C₁-C₄烷氨基-C₁-C₄烷基，二(C₁-C₄烷基)氨基-C₁-C₄烷基，C₁-C₄烷硫基-C₁-C₄烷基，C₁-C₄卤代烷硫基-C₁-C₄烷基，C₃-C₄烯硫基-C₁-C₄烷基，C₃-C₄炔硫基-C₁-C₄烷基，C₁-C₄烷亚磺基-C₁-C₄烷基，C₁-C₄卤代烷亚磺基-C₁-C₄烷基，C₃-C₄烯亚磺基-C₁-C₄烷基，C₃-C₄炔亚磺基-C₁-C₄烷基，C₁-C₄烷磺基-C₁-C₄烷基，C₁-C₄卤代烷磺基-C₁-C₄烷基，C₃-C₄烯磺基-C₁-C₄烷基，C₃-C₄炔磺基-C₁-C₄烷基，C₃-C₆烯基，氰基-C₃-C₆烯基，C₃-C₆卤代烯基，C₃-C₆炔基，氰基-C₃-C₆炔基，C₃-C₆卤代炔基，HO-CO-C₁-C₄烷基，(C₁-C₄烷氧基)CO-C₁-C₄烷基，(C₁-C₄烷基)CS-C₁-C₄烷基，H₂N-CO-C₁-C₄烷基，C₁-C₄烷基-NHCO-C₁-C₄烷基，二(C₁-C₄烷基)NCO-C₁-C₄烷基，二(C₁-C₄烷基)磷酸基-C₁-C₄烷基，C₃-C₈环烷基（任选取代），C₃-C₈环烷基-C₁-C₄烷基，苯基，苯基-C₁-C₄烷基，3-至7-员杂环基或杂环基-C₁-C₄烷基，其中每个杂环基环可含一个CO-环键或CS-环键；或者，若Z=化学键，R₇还可为H，OH，CN，SH，NH₂，卤素，-CH(OH)-CH₂-R₉，-CH(卤素)-CH₂-R₉，-CH₂-CH(卤素)-R₉，-CH=CH-R₉或-CH=C(卤素)-R₉，其中R₉=COOH，(C₁-C₄烷氧基)羰基，(C₁-C₄烷硫基)羰基，CONH₂，C₁-C₄烷基-NHCO，或二(C₁-C₄烷基)NCO；或R₇+R₈=任选取代的1,3-丙二烯基，四亚甲基，五亚甲基或氧二亚甲基链。
• 7-SUBSTITUTED-6-FLUORO-1,4-DIHYDRO-4-OXO-QUINOLINE-3-CARBOXYLIC ACID COMPOUNDS USEFUL AS ANTIBACTERIAL AGENTS
  申请人：NAEJA Pharmaceutical Inc.

  公开号：EP0561850B1

  公开（公告）日：2000-07-12
• HERBIZIDE 3-(BENZAZOL-4-YL)PYRIMIDINDION-DERIVATE
  申请人：BASF AKTIENGESELLSCHAFT

  公开号：EP1047693A1

  公开（公告）日：2000-11-02
• US5342846A
  申请人：——

  公开号：US5342846A

  公开（公告）日：1994-08-30
• [EN] 7-SUBSTITUTED-6-FLUORO-1,4-DIHYDRO-4-OXO-QUINOLINE-3-CARBOXYLIC ACID COMPOUNDS AND RELATED COMPOUNDS AS ANTIBACTERIAL AGENTS<br/>[FR] COMPOSES D'ACIDE 7-SUBSTITUE-6-FLUORO-1,4-DIHYDRO-4-OXO-QUINOLINE-3-CARBOXYLIQUE ET COMPOSES CORRESPONDANTS EN TANT QU'AGENTS ANTIBACTERIENS
  申请人：SYNPHAR LABORATORIES, INC.

  公开号：WO1993024481A1

  公开（公告）日：1993-12-09

  (EN) Quinoline compounds of formula (I) wherein (A) R is hydrogen or C1-C4 alkyl group; R1 is (i) a C3-C6 cycloalkyl group which may be substituted with one or two halogen atoms, (ii) a phenyl group which may be substituted with one or two halogen atoms, or (iii) a C1-C4 alkyl group which may be substituted with one or two halogen atoms; R2 is hydrogen, a halogen atom, a C1-C4 alkyl group, a hydroxy group or an amino group; R3 is hydrogen, a hydroxy or an amino group; R4 is a 1,2,3-triazol-1-yl group, a 1,2,4-triazol-1-yl group, a 1,2,3,4-tetrazol-1-yl group or a 1,2,3,4-tetrazol-2-yl group, each of which may have 1 to 2 substituents selected from the group consisting of C1-C4 alkyl, COOH, CH2NH2, amino and phenyl groups; and X is N, CH, C-F or C-OCH3; m is 1 or 2; n is 0, 1 or 2; or (B) R1, R2, R3, R4, m and n are as defined above and X and R1 are such that (a) in formula (I) is (b), pharmaceutical compositions using those compounds, methods for treating bacterial infections using those compounds, and methods for disinfecting using those compounds.(FR) Composés quinoline selon la formule (I) dans laquelle (A) R représente l'hydrogène ou un groupe alkyle C1-C4; R1 représente (i) un groupe cycloalkyle C3-C6 qui peut être substitué avec un ou deux atomes d'un halogène, (ii) un groupe phényle qui peut être substitué avec un ou deux atomes d'un halogène, ou (iii) un groupe alkyle C1-C4 qui peut être substitué avec un ou deux atomes d'un halogène; R2 représente l'hydrogène, un atome d'un halogène, un groupe alkyle C1-C4, un groupe hydroxy ou un groupe amino; R3 représente l'hydrogène, un groupe hydroxy ou amino; R4 représente un groupe 1,2,3-triazol-1-yle, un groupe 1,2,4-triazol-1-yle, un groupe 1,2,3,4-tétrazol-1-yle ou un groupe 1,2,3,4-tétrazol-2-yle, chacun de ces groupes pouvant avoir 1 à 2 substituants sélectionnés dans le groupe composé d'alkyle C1-C4, COOH, CH2NH2, de groupes amino et phényle; et X représente N, CH, C-F ou C-OCH3; m vaut 1 ou 2; n vaut 0, 1 ou 2; ou (B) R1, R2, R3, R4, m et n sont définis tels que ci-dessus et X et R1 sont tels que (a) dans la formule (I) est (b). L'invention décrit les compositions pharmaceutiques utilisant ces composés, les procédés de traitement des infections bactériennes utilisant ces composés et les procédés de désinfection utilisant ces composés.