CAS: 790-69-2; Loflucarban

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      专利号:US-7199128-B2
      优先权日:2005-02-02
      标题 :8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
      发明人:BRADBURY BARTON J; WILES JASON ALLAN; DESHPANDE MILIND; WANG QIUPING; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
      权利人:ACHILLION PHARMACEUTICALS INC
      摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.

      专利号:US-2009012071-A1
      优先权日:2007-04-23
      标 题 :4-substituted-1h-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2h,9h)-diones and related compounds as anti-infective agents
      发明人:BRADBURY BARTON JAMES; DESHPANDE MILIND; HASHIMOTO AKIHIRO; KIM HA YOUNG; LUCIEN EDLAINE; PAIS GODWIN; PUCCI MICHAEL JOHN; WANG QIUPING; WILES JASON ALLAN
      权利人:ACHILLION PHARMACEUTICALS INC
      摘要:The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents. The invention provides methods for treating or preventing microbial infections, preferably animals, by administering an effective amount of a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound to an organism suffering from or susceptible to microbial infection. The invention also provides methods of inhibiting microbial growth and survival by applying an effective amount of a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound.

      专利号:US-8946422-B2
      优先权日:2005-07-27
      标题:8-methoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones and related compounds as anti-infective agents
      发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG
      权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC
      摘要:The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

      专利号:US-7659399-B2
      优先权日:2005-01-05
      标 题 :1-thia-2,4a-diaza-cyclopenta[b]napththalene-3,4-diones and related compounds as anti-infective agents
      发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN
      权利人:ACHILLION PHARMACEUTICALS INC
      摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

      专利号:EP-1809639-B1
      优先权日:2004-11-11
      标 题 :8a, 9-dihydro-4a-h-isothiazolo[5,4-b] quinoline-3, 4-diones and related compounds as anti-infective agents
      发明人:BRADBURY BARTON JAMES; DESHPANDE MILIND; PUCCI MICHAEL JOHN; WANG QIUPING; WILES JASON ALLAN; SONG YONGSHENG; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
      权利人:ACHILLION PHARMACEUTICALS INC
      摘要:The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables n, m, p, RA, RB, A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.

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      主要参考文献


      1: Thuan NK, Naher K, Kubo R, Taniguchi T, Hayashidani H. Evaluation of Chromogenic Medium for Selective Isolation of Yersinia. Shokuhin Eiseigaku Zasshi. 2016;57(5):166-168. doi: 10.1016/j.plasmid.2016.10.001. Epub 2016 Oct 12. doi: 10.1007/s10661-016-5510-1. Epub 2016 Aug 9. doi: 10.1371/journal.pone.0106329. eCollection 2014.
      6: Condie LW, Buhler DR. Effect of hexachlorophene, tribromsalan, trichlorcarban and cloflucarban on hexobarbital sleeping time and hepatic drug-metabolizing enzyme activity in vitro in the rat. Biochem Pharmacol. 1979;28(3):375-80. doi: 10.1371/journal.pone.0079119. eCollection 2013. Erratum in: PLoS One. 2015;10(5):e0126198.
      8: González M, Gude MJ, Seral C, Abad MP, Algarate S, Castillo FJ. [Comparasion of two methods for recovery of Aeromonas spp. in feces from agar CIN (Cefsulodin-Irgasan-Novobiocin)]. Rev Esp Quimioter. 2010 Dec;23(4):217-8. Spanish. doi: 10.1098/rstb.2011.0060.

      合成参考文献


      参考文献:10.1007/978-3-642-57741-3_1
      摘要:Blümer-Schwinum B, Reuß W, Schenk D, Hoffmann-Schollmayer U. Indikations-und Stoffgruppenregister. 1995. In: Hagers Handbuch. : Springer Berlin Heidelberg; 1995.
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