CAS: 27877-51-6; Tolindate

该化合物是一种化学化合物,主要被确认为用作药物剂,被归类为非类固醇抗炎药物(NSAID),以其止痛和抗炎特性著称,该化合物一般是白色和非白晶状粉,在有机溶剂中可溶解,但在水中溶解性有限;通过抑制在长效催产物生物合成中发挥关键作用,从而减少炎痛和炎痛的环氧酶(COX)作用,该产品具有阻燃功能,在代孕剂生物合成方面起着关键作用;其药用植物动力学学学涉及口服后吸收,代谢学则可能涉及 hepic途径;该化合物具有治疗用途,与所有药物一样,在使用前还可能具有副作用,包括胃肠扰动和潜在的心血管风险;与任何制药业一样,其使用应当由保健专业人员指导,以确保安全和功效.

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      专利信息


      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:US-2014315720-A1
      优先权日:2012-10-24
      标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
      发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
      权利人:CELANESE ACETATE LLC
      摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

      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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      合成参考文献


      参考文献:10.1124/mol.119.115964
      摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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