- STAT3 DIMERIZATION INHIBITORS
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The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as wel
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Page/Page column 70
(2014/05/24)
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- Development of new N-arylbenzamides as STAT3 dimerization inhibitors
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The O-tosylsalicylamide S3I-201 (10) was used as a starting point for design and synthesis of novel STAT-3 dimerization inhibitors with improved drug-like qualities. The phosphonic acid 12d and salicylic acids 13f, 13g with a shorter amide linker lacking
- Urlam, Murali K.,Pireddu, Roberta,Ge, Yiyu,Zhang, Xiaolei,Sun, Ying,Lawrence, Harshani R.,Guida, Wayne C.,Sebti, Said M.,Lawrence, Nicholas J.
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supporting information
p. 932 - 941
(2013/07/27)
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- Synthesis and immunomodulating activity of new analogues of fingolimod
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Five new immunomodulators 1a-1e by using a trans-4-alkyl-substituted cyclohexane to replace the flexible C8 alkyl chain of Fingolimod were synthesized. For in-vitro test, the compounds were dissolved in DMSO as a stock solution and diluted to a desired co
- Feng, Xiang-Jun,Yang, Xiao-Ying,Luo, Yu,Li, Xin,Tang, Wei,Zuo, Jian-Ping,Lu, Wei
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experimental part
p. 93 - 100
(2012/04/04)
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- AZOLE COMPOUND AND MEDICINAL USE THEREOF
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The present invention relates to an azole compound represented by the formula [I] wherein W is S or O; R is -COOR7, -X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is -(CH2)m-X- (X is -N(R8)-, -C(R9)(R10)-, -CO- or -CO-N(R8)-); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is -(Y)s1-(A2)s-Z (Y is -O-, -S(O)t-, -N(R13)-, -N(R14)-CO-, -N(R14)-SO2-, -SO2-N(R14)- and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.
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