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 T82720 Target Info
Target Name Dual-specificity tyrosine-phosphorylation regulated kinase 1B (DYRK1B)
Synonyms Minibrain-related kinase; MIRK; Dual specificity tyrosine-phosphorylation-regulated kinase 1B
Target Type Patented-recorded Target
Gene Name DYRK1B
Biochemical Class Kinase
UniProt ID
DYR1B_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014115071
Title Kinase Inhibitors.
Abstract The invention relates to derivatives of indole, benzothiophene or benzofuran of formula (I), a compound having formula (Ia), in which: Y1 is selected from an NH group, a sulphur atom or an oxygen atom; Y2 is selected from a CH group or a nitrogen atom; X1, X2, X3 and X4 represent a CH group, a carbon atom or a nitrogen atom; R4 represents a -CN group, a -CONH2 group, a -CH2NR5R6 group, a -CH2NHCOCH3 group, an (AA) group or a (BB) group; Z represents a CH group or a nitrogen atom; Ar represents an aryl group; n represents an integer between 1 and 4, as well as the pharmaceutically-acceptable salts thereof, for use in the treatment of neurodegenerative diseases, depression, schizophrenia or viral infections. Some of these compounds can also be used in cancer treatment. The invention also relates to some corresponding novel compounds and to the associated production method.
Applicant(s) Center National De La Recherche Scientifique
Representative Drug(s) D09CDR Drug Info IC50 = 23 nM Click to Show More [1]
2 D0CC7E Drug Info IC50 = 23 nM [1]
3 D0GE4F Drug Info IC50 = 41 nM [1]
Patent ID WO2013026806
Title Dyrk1 Inhibitors and Uses Thereof.
Abstract The present invention relates to novel thiazolo[5,4-]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.
Applicant(s) Diaxonhit Leblond, et al
Representative Drug(s) D08DIJ Drug Info IC50 = 0.28 nM Click to Show More [1]
2 D08CUF Drug Info IC50 = 0.59 nM [1]
3 D0PJ1W Drug Info IC50 = 1.07 nM [1]
4 D0O9BK Drug Info DYRK1B IC50 = 1.63 nM [1]
5 D0DT5I Drug Info IC50 = 2.83 nM [1]
Patent ID WO2012098066
Title 1,6- and 1,8-Naphthyridines Useful As Dyrk1 Inhibitors.
Abstract Compounds of formula I, and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0C0BP Drug Info IC50 < 4.6 nM Click to Show More [1]
2 D0SB1W Drug Info IC50 = 13.8 nM [1]
Patent ID WO2012098065
Title Pyrido Pyrimidines for Use As Dyrk1 Inhibitors.
Abstract Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0B8IQ Drug Info IC50 = 8.2 nM Click to Show More [1]
2 D00TFF Drug Info IC50 = 10.5 nM [1]
Patent ID WO2012098070
Title Quinoline Dyrk1 Inhibitors.
Abstract Compounds of Formula (I) and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D05CLL Drug Info N.A. Click to Show More [1]
2 D0BP6J Drug Info N.A. [1]
Patent ID WO2015083750
Title Compound Pertaining To Neuropoiesis and Drug Composition.
Abstract Provided is a composition for activating neuropoiesis or neuron proliferation. In one or more embodiments, the composition contains, as the active ingredient, a compound having a DYRK inhibiting abili.
Applicant(s) Kyoto University
Representative Drug(s) D04SYJ Drug Info IC50 = 36 nM [1]
Patent ID WO2012098068
Title Pyrazolo Pyrimidines As Dyrk1A and Dyrk1B Inhibitors.
Abstract Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0P7QO Drug Info N.A. [1]
Patent ID WO2011133795
Title Beta-Carbolines As Inhibitors of Haspin and Dyrk Kinases.
Abstract The present disclosure is directed to compounds of Formula ( I ) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.
Applicant(s) The Brigham and Women'S Hospital, Inc
Representative Drug(s) D02DBH Drug Info N.A. [1]
Patent ID WO2011127406
Title Acridines As Inhibitors of Haspin and Dyrk Kinases.
Abstract The present disclosure is directed to compounds of Formula I: which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.
Applicant(s) The Brigham and Women'S Hospital, Inc
Representative Drug(s) D07BWC Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20120184508
Title Preparation of Pyrazolopyrimidines As Inhibitors of Dyrk1A and Dyrk1B.
Representative Drug(s) D0P7QO Drug Info N.A. [1]
References  Top
REF 1 Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors: a survey of recent patent literature.Expert Opin Ther Pat. 2017 Nov;27(11):1183-1199.

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