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Substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs as inhibitors of STAT proteins

A technology of hydroxyl and haloalkoxy, which is applied in the preparation of organic compounds, drug combinations, active ingredients of amides, etc.

Inactive Publication Date: 2014-02-26
UNIV OF CENT FLORIDA RES FOUND INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010]Despite advances in drug discovery related to the identification of inhibitors of STAT protein activity, there is still a lack of potent, potent and selective activators of STAT3 and STAT5 as well as therapeutic Compounds for cancer and other diseases associated with abnormal function of STAT3, STAT5 or both proteins and diseases involving either or both STAT3 and STAT5

Method used

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  • Substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs as inhibitors of STAT proteins
  • Substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs as inhibitors of STAT proteins
  • Substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs as inhibitors of STAT proteins

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preparation example Construction

[0645] In one aspect, the invention relates to a method for the manufacture of a medicament for uncontrolled cell proliferative activity in a mammal comprising combining a therapeutically effective amount of a disclosed compound or product of the disclosed method with a pharmaceutically acceptable carrier or diluent agent.

[0646] 3. The use of the compound

[0647] In one aspect, the invention relates to the use of a compound having a structure represented by Formula I, II, III, IV, V or VI, or a pharmaceutically acceptable salt, hydrate, solvate or polymorph thereof.

[0648] In a further aspect, the compound is a disclosed compound described by Formula I, II, III, IV, V or VI or the product of a disclosed method.

[0649] In a further aspect, the use involves inhibiting STAT protein activity. In a further aspect, the use involves inhibition of STAT3 protein activity. In yet a further aspect, the use relates to preventing STAT3 protein dimerization. In yet a further asp...

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Abstract

In one aspect, the invention relates to substituted substituted 2-hydroxy-4-(2- (phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Description

[0001] Related applications [0002] This application claims the benefit of US Application Nos. 61 / 369,796, filed August 2, 2010, and 61 / 422,046, filed December 10, 2010, both of which are incorporated by reference in their entirety. [0003] Statement Regarding Government Sponsored Research [0004] This invention was made with government support under Grant Nos. CA106439 and CA128865 awarded by the National Cancer Institute, National Institutes of Health. The U.S. Government has certain rights to the invention. Background technique [0005] STAT proteins were initially discovered as potential cytoplasmic transcription factors mediating cytokine and growth factor responses (Darnell, J.E., Jr. (1996) Recent Prog. Norm. Res. 51, 391-403; Darnell. J. E. (2005) Nat. Med. 11, 595- 596). Multiple members of the family, STAT1, STAT2, STAT3, STAT4, STAT5a, and STAT5b, and STAT6 mediate a variety of physiological effects, including growth and differentiation, survival, development,...

Claims

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Application Information

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IPC IPC(8): A61K31/18
CPCA61K31/18C07C311/29C07C323/49C07C311/46C07C2101/14C07D233/84C07D215/36C07D401/04C07D213/42C07D211/26C07C311/19C07C311/42C07D211/96C07D207/48A61P9/12A61P11/00A61P17/06A61P35/00A61P43/00C07D211/34C07D211/60C07C2601/14C07C311/05
Inventor J·塔克森P·冈宁
Owner UNIV OF CENT FLORIDA RES FOUND INC