Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T29130 Target Info
Target Name Signal transducer and activator of transcription 3 (STAT3)
Synonyms Acute-phase response factor; APRF
Target Type Successful Target
Gene Name STAT3
Biochemical Class Transcription factor
UniProt ID
STAT3_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014070859
Title Stat3 Dimerization Inhibitors.
Abstract 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 well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.
Applicant(s) H. Lee Moffitt Cancer Center and Research Institute
Representative Drug(s) D06RBL Drug Info IC50 = 15000 nM Click to Show More [1]
2 D08ETA Drug Info IC50 = 45000 nM [1]
Patent ID WO2013177534
Title New Salicylic Acid Derivatives, Pharmaceutically Acceptable Salt Thereof, Composition Thereof and Method of Use Thereof.
Abstract The present invention relates to novel compounds (Formula (I)), compositions containing same and methods for inhibiting STAT3 and/or STAT5 activity or for the treatment of a STAT3 or STAT5-dependent cancer using said compounds; or a pharmaceutically acceptable salt, solvate or prodrug thereof.
Applicant(s) The Governing Council of the University of Toronto
Representative Drug(s) D08EID Drug Info Kd = 300 nM Click to Show More [1]
2 D0U7LL Drug Info IC50 = 19000 nM [1]
3 D03ARS Drug Info N.A. [1]
4 D04ANB Drug Info N.A. [1]
5 D09ZCV Drug Info N.A. [1]
6 D0EX9O Drug Info N.A. [1]
7 D0V3PA Drug Info N.A. [1]
Patent ID WO2013187965
Title Pyrazole Derivatives As Inhibitors of Stat3.
Abstract Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.
Applicant(s) Mayo Foundation for Medical Education and Research
Representative Drug(s) D0DC3S Drug Info N.A. Click to Show More [1]
2 D0ET3L Drug Info N.A. [1]
3 D0M5AR Drug Info N.A. [1]
4 D0M8OV Drug Info N.A. [1]
5 D0S0UL Drug Info N.A. [1]
Patent ID WO2012142615
Title Auranofin and Auranofin Analogs Useful To Treat Proliferative Disease and Disorders.
Abstract Auranofin analogs and pharmaceutical compositions which inhibit p-STAT3 are provided together methods of synthesizing and methods of using the compounds. Also provided are methods of treating p-STAT3 diseases and disorders in a patient in need thereof by administering a therapeutically effective amount of one or more of these compounds, alone or in combination with another drug therapy. The compounds and pharmaceutical compositions disclosed are useful to treat proliferative diseases and disorders including, but not limited to, cancer.
Applicant(s) Board of Regents, the University of Texas System
Representative Drug(s) D03HEP Drug Info N.A. Click to Show More [1]
2 D0FH4G Drug Info N.A. [1]
3 D0J1US Drug Info N.A. [1]
Patent ID WO2012135736
Title Modulation of Signal Transducer and Activator of Transcription 3 (Stat3) Expression.
Abstract Disclosed herein are antisense compounds and methods for decreasing STAT3 mRNA and protein expression. Such methods, compounds, and compositions are useful to treat, prevent, or ameliorate hyperproliferative diseases.
Applicant(s) Isis Pharmaceuticals, Inc
Patent ID WO2010062681
Title Luteolin and Diosmin/Diosmetin As Novel Stat3 Inhibitors for Treating Autism.
Abstract The present invention includes methods for the treatment of autoimmune disorders such as autism, schizophrenia, and type 1 diabetes. Flavonoids, luteolin, diosmin, and diosmin's aglycone form, diosmetin, were found to inhibit activation/phosphorylation of STAT3 induced by IL-6 in cultured neuronal cells. Furthermore, mice treated with diosmin showed a significant reduction of autistic phenotype induced by IL-6 through inhibition of STAT3 activation.
Applicant(s) University of South Florida
Representative Drug(s) D02KDA Drug Info N.A. Click to Show More [1]
2 D0EV5U Drug Info N.A. [1]
3 D0V7NH Drug Info N.A. [1]
4 D0Y3DN Drug Info N.A. [1]
5 D0Z8BD Drug Info N.A. [1]
Patent ID WO2009036059
Title Novel Stat3 Pathway Inhibitors and Cancer Stem Cell Inhibitors.
Abstract The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.
Applicant(s) Boston Biomedical, Inc
Representative Drug(s) D09BOL Drug Info N.A. Click to Show More [1]
2 D09SYX Drug Info N.A. [1]
3 D0T1GB Drug Info N.A. [1]
4 D0V7HS Drug Info N.A. [1]
5 D0WW1Z Drug Info N.A. [1]
Patent ID WO2006012625
Title Stat3 Decoy Oligonucleotides and Uses Therefor.
Abstract A composition is provided that is useful in treating cancers in which STAT3 is activated, such as squamous cell carcinomas including squamous cell carcinoma of the head and neck. The composition comprises an effective amount of a STAT3 decoy and a pharmaceutically acceptable carrier. Also provided are methods of treating such cancers and methods of modulating STAT3 transcriptional activation in a cell.
Applicant(s) University of Pittsburgh - of the Commonwealth System of Higher Education
Patent ID WO2008070697
Title Stat3 Inhibitor Having Anti-Cancer Activity and Associated Methods.
Abstract 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.
Applicant(s) University of Central Florida Research Foundation, Inc
Representative Drug(s) D0EZ6V Drug Info IC50 = 79000 nM [1]
Patent ID WO2008044667
Title Stat3/5 Activation Inhibitor.
Abstract An object of the present invention is to provide a STAT3/5 activation inhibitor. The present invention provides a STAT3/5 activation inhibitor containing an aromatic compound represented by the general formula or a salt thereof as an active ingredient: wherein X1 represents a nitrogen atom or a group -CH=, R1 represents a group -Z-R6, in which Z represents a group -CO-, a group -CH(OH)- or the like, R6 represents a 5-to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group -O-, a group -CO-, a group -CH(OH)-or a lower alkylene group, and A represents a group wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.
Applicant(s) Otsuka Pharmaceutical Co., Ltd
Representative Drug(s) D0ZQ8T Drug Info IC50 < 150 nM [1]
Patent ID WO2006071812
Title Platinum Iv Complex Inhibitor.
Abstract The invention disclosed herein provides methods for diagnosing and treating diseases and/or conditions associated with dysregulated Stat3-mediated activity.
Applicant(s) H. Lee Moffitt Cancer Center and Research Institute
Representative Drug(s) D01BVU Drug Info IC50 = 1400 nM [1]
Patent ID WO2011163424
Title Substituted 2-(9H-Purin-9-Yl) Acetic Acid Analogues As Inhibitors of Stat3.
Abstract 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.
Applicant(s) University of Central Florida Research Foundation, Inc
Representative Drug(s) D0Y2PO Drug Info N.A. [1]
Patent ID WO2000032189
Title Celecoxib Compositions.
Abstract Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.
Applicant(s) Gd Searle & Co
Representative Drug(s) D0KP0U Drug Info N.A. [1]
Patent ID WO2013063504
Title Platinum Compounds That Inhibit Constitutive Stat3 Signaling and Induce Cell Cycle Arrest and Apoptosis of Malignant Cells.
Abstract The subject invention concerns a compound and compositions having activity as an inhibitor of Stat3 protein and methods of using the compound and compositions. In one embodiment, a compound of the invention has the structure shown in formula I, formula II, or formula III. The subject invention also concerns methods of using the compounds and compositions of the invention.
Applicant(s) H. Lee Moffitt Cancer Center and Research Institute
Patent ID WO2011110359
Title Stat3 Activation Inhibitors.
Abstract The present invention relates to novel Stat3 activation inhibitors, especially to (poly)peptides capable to inhibit Stat3 signaling. The invention furthermore concerns nucleic acids encoding for these (poly)peptides and vectors comprising said nucleic acids. In addition, the present invention relates to respective uses of the Sta3 activation inhibitors and pharmaceutical compositions comprising same. The invention also relates to the isolated coiled-coil domain of Stat3 and screening methods for identifying compounds having affinity to this domain.
Applicant(s) Chemotherapeutisches Forschungs Institut
Patent ID WO2010077589
Title Stat3 Inhibitors and Therapeutic Methods Using The Same.
Abstract Inhibitors of STAT3 are disclosed. Methods of using the STAT3 inhibitors in the treatment of diseases and conditions wherein inhibition of STAT3 provides a benefit, like cancers, also are disclosed.
Applicant(s) The Regents of the University of Michigan
United States Patent and Trademark Office (USPTO)
Patent ID US0069420
Title Small-Molecule Inhibitors of Stat3 with Antitumour Activity.
Applicant(s) H. Lee Moffitt Cancer Center and Research Institute
Representative Drug(s) D06RBL Drug Info IC50 = 15000 nM Click to Show More [1]
2 D08ETA Drug Info IC50 = 45000 nM [1]
Patent ID US7960434
Title Small-Molecule Inhibitors of Stat3 with Antitumour Activity.
Applicant(s) H. Lee Moffitt Cancer Center and Research Institute
Representative Drug(s) D0TU0X Drug Info IC50 = 86000 nM Click to Show More [1]
2 D02ILH Drug Info N.A. [1]
3 D04GVY Drug Info N.A. [1]
Patent ID US20120053208
Title Curcumin Analogs As Dual Jak2/Stat3 Inhibitors and Methods of Making and Using The Same.
Applicant(s) The Ohio State University Research Foundation
Representative Drug(s) D0WD1Z Drug Info Kd = 172 nM Click to Show More [1]
2 D0IC8O Drug Info N.A. [1]
Patent ID US20120035114
Title Inhibitors of Stat3 and Uses Thereof. Board of Regent of The University of Texas System.
Representative Drug(s) D0QR1I Drug Info IC50 = 17 nM Click to Show More [1]
2 D03VMP Drug Info IC50 = 125 nM [1]
3 D02CJU Drug Info N.A. [1]
4 D0X6QQ Drug Info N.A. [1]
Patent ID US20100094061
Title Stat3 Phosphorylation Inhibitor and Notch Expression Inhibitor.
Applicant(s) Meiji Dairies Corporation
Representative Drug(s) D0MA8T Drug Info N.A. Click to Show More [1]
2 D0ZS8Q Drug Info N.A. [1]
Patent ID US8586749
Title Compounds That Suppress Cancer Cells and Exhibit Antitumor Activity.
Representative Drug(s) D0Y0OQ Drug Info IC50 = 35000 nM [1]
Patent ID US20110212911
Title Transcription Factor Inhibitors and Related Compositions, formulations and Methods.
Applicant(s) The Ohio University
Patent ID US20070010428
Title Inhibitors of Signal Transducer and Activator of Transcription 3.
European Patent Office (EPO)
Patent ID EP2325181
Title Stat3 Inhibitor Containing Quinolinecarboxamide Derivative As Active Ingredient.
Applicant(s) Pharma. Ip. General, Inc
Representative Drug(s) D00FUZ Drug Info N.A. Click to Show More [1]
2 D03XAK Drug Info N.A. [1]
3 D0D8RR Drug Info N.A. [1]
Patent ID EP2120958
Title Stat3 Inhibitor Having Anti-Cancer Activity and Associated Methods.
Applicant(s) University of Central Florida Research Foundation, Inc
Representative Drug(s) D0EZ6V Drug Info IC50 = 79000 nM [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN103301111
Title One Kind Stat3 Inhibitor -Egcg Application of Liver Cancer Treatment.
Representative Drug(s) D09CKU Drug Info N.A. [1]
References  Top
REF 1 A STAT inhibitor patent review: progress since 2011.Expert Opin Ther Pat. 2015;25(12):1397-421.

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