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2. 发明公开

EP0518414A1 Thioxanthenone antitumor agents 失效转让
标题翻译： Thioxanthenon-Antitumormittel。
公开(公告)号：EP0518414A1
公开(公告)日：1992-12-16
申请号：EP92201587.0
申请日：1992-06-03
申请人： STERLING WINTHROP INC.
发明人： Miller, Theodore Charles , Collins, Joseph Charles , Wentland, Mark Philip , Perni, Robert Bruno , Corbett, Thomas Hughes , Mattes, Kenneth Charles, c/o Eastman Kodak Company
IPC分类号： C07D335/16 , C07F9/24 , A61K31/38
CPC分类号： C07F9/655372 , C07D335/16
摘要： 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones having the formula

wherein n is 2 or 3;
R¹ and R² are independently lower-alkyl;
Q is a residue chosen from the group consisting of CH₂NHR³, CH₂N(R⁴)SO₂R⁷, CH₂NHCHO, CH=N-Ar, C(O)NR⁵R⁶, CH₂N(R⁴)C(O)R⁷, CH₂N(C₂H₅)CHO, and CH₂N(R⁴)P(O)(O-lower-alkyl)₂;
R³ is hydrogen or lower-alkyl;
R⁴ is hydrogen or lower-alkyl;
R⁵ is hydrogen, lower-alkyl or Ar;
R⁶ is hydrogen or lower-alkyl;
R⁷ is lower-alkyl, or Ar;
R⁸ is hydrogen, lower-alkyl, lower-alkoxy, or halogen; and
Ar is phenyl or phenyl substituted with methyl, methoxyl, halogen or nitro;
or a pharmaceutically acceptable acid-addition salt or solvate thereof, are disclosed as antitumor agents. Compositions containing the thioxanthenones and the method of use of thioxanthenones for treating tumors and cancer in mammals are also disclosed.
摘要翻译： 1 - [[（二烷基氨基）烷基]氨基] -4-取代的噻吨-9-酮，其具有式CHEM，其中n为2或3; R 1和R 2独立地为低级烷基; Q是选自由CH 2 NHR 3，CH 2 N（R 4）SO 2 R 7，CH 2 NHCHO，CH = N-Ar，C（O）NR 5 R 6，CH 2 N（ R 4）C（O）R 7，CH 2 N（C 2 H 5）CHO和CH 2 N（R 4）P（O）（O-低级 - 烷基）2; R 3是氢或低级烷基; R 4是氢或低级烷基; R 5是氢，低级烷基或Ar; R 6是氢或低级烷基; R 7是低级烷基或Ar; R 8是氢，低级烷基，低级烷氧基或卤素; 并且Ar是苯基或被甲基，甲氧基，卤素或硝基取代的苯基; 或其药学上可接受的酸加成盐或其溶剂合物作为抗肿瘤剂公开。还公开了含有噻吨酮的组合物和用于治疗哺乳动物肿瘤和癌症的噻吨酮的方法。

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