Patent application number | Description | Published |
20090069420 | Small molecule inhibitors of STAT3 with anti-tumor activity - The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis. The invention further includes an in-vitro screening test for the presence of malignant cells in a mammalian tissue; a method of identifying inhibitors of constitutive Stat3 activation, Stat3-DNA binding, Stat5-DNA binding, and/or Stat3 dimerization; and a method of identifying anti-cancer agents. | 03-12-2009 |
20090318367 | Use of SH2 STAT3/STAT1 Peptidomimetics as Anticancer Drugs - The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention display selective inhibition of specific STAT isoform homo-dimerization. The peptidomimetic probes of STAT1 function, described herein, provide the means to preferentially inhibit STAT1 over STAT3 through the exploration of the C-terminus. | 12-24-2009 |
20100310645 | METHODS FOR INHIBITING TUMOR CELL PROLIFERATION - The subject invention concerns methods for inhibition of STAT biological functions using platinum complexes. | 12-09-2010 |
20110124602 | Stat3 Inhibitor Having Anti-Cancer Activity and Methods - A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers. | 05-26-2011 |
20110201576 | Small molecule inhibitors of stat3 with anti-tumor activity - The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis. The invention further includes an in-vitro screening test for the presence of malignant cells in a mammalian tissue; a method of identifying inhibitors of constitutive Stat3 activation, Stat3-DNA binding, Stat5-DNA binding, and/or Stat3 dimerization; and a method of identifying anti-cancer agents. | 08-18-2011 |
20110223661 | INHIBITORS OF STAT3 - Disclosed herein are compounds derived from a chemical structure according to the formula (I) wherein X comprises oxygen or sulfur, R | 09-15-2011 |
20110263525 | DRUG COMPOSITION CYTOTOXIC FOR PANCREATIC CANCER CELLS - The invention describes a cytotoxic composition containing a drug combination targeting two or more functional elements in pancreatic cancer cells, the functional elements comprising EGFR or Src and Stat3 or Jaks. Preferred drugs in the drug combination are selected from ZD and S3I-201, Das and S3I-201, ZD and AG490, Das and AG490, and combinations thereof. In a preferred embodiment of the invention, the drug combination further includes a nucleoside analog inhibitory for DNA replication, for example, Gemcitabine. Disclosed is also a method of cytotoxically affecting pancreatic cancer cells using the described drug combination. A method of making the cytotoxic composition is additionally described. | 10-27-2011 |
20120130079 | Compounds That Suppress Cancer Cells and Exhibit Antitumor Activity - The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo. | 05-24-2012 |
20120269729 | STABILIZED CHITOSAN-BASED NANOPARTICLES AND METHODS FOR MAKING THE SAME - A stabilized chitosan-based nanoparticle is provided having a chitosan polymer and a hydrophilic dispersing agent. In the stabilized nanoparticle, chains of the chitosan polymer electrostatically interact with chains of the hydrophilic dispersing agent to form an entangled network between the chitosan polymer and the hydrophilic dispersing agent. The stabilized chitosan-based nanoparticle has optimal particle integrity and stability properties under physiological conditions. | 10-25-2012 |
20130006007 | ACTIVATABLE NANOPROBES FOR INTRACELLULAR DRUG DELIVERY - An activatable nanoprobe is provided having a core component and an active agent associated with the core component via a bond configured to be cleaved upon exposure to an endogenous compound. | 01-03-2013 |
20130172340 | SUBSTITUTED 2-(9H-PURIN-9-YL) ACETIC ACID ANALOGUES AS INHIBITORS OF STAT3 - In one aspect, the invention relates to substituted purine 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. | 07-04-2013 |
20130177979 | METHODS AND COMPOSITIONS FOR CELL PERMEABLE STAT3 INHIBITOR - Disclosed herein are compositions for inhibition of Stat, particularly Stat3. Disclosed herein are compositions comprising cell permeable Stat3 inhibitors. Compositions may comprise peptides, polypeptides, antibodies, nucleic acids, vectors, and host cells for making, using, assaying, and evaluating Stat3 inhibitors. Disclosed herein are methods for making and using the disclosed compositions. | 07-11-2013 |
20130225621 | SUBSTITUTED 2-HYDROXY-4-(2-(PHENYLSULFONAMIDO)ACETAMIDO)BENZOIC ACID ANALOGS AS INHIBITORS OF STAT PROTEIN - In one aspect, the invention relates to 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. | 08-29-2013 |
20140194468 | Compounds that Suppress Cancer Cells and Exhibit Antitumor Activity - The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo. | 07-10-2014 |
20140369937 | ACTIVATABLE NANOPROBES FOR INTRACELLULAR DRUG DELIVERY - An activatable nanoprobe is provided having a core component and an active agent associated with the core component via a bond configured to be cleaved upon exposure to an endogenous compound. | 12-18-2014 |
20150038708 | SUBSTITUTED 2-HYDROXY-4-(2-(PHENYLSULFONAMIDO)ACETAMIDO)BENZOIC ACID ANALOGS AS INHIBITORS OF STAT PROTEIN - In one aspect, the invention relates to 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. | 02-05-2015 |