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 T92803 Target Info
Target Name Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A)
Synonyms hMNB; Protein kinase minibrain homolog; MNBH; MNB; HP86; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; Dual specificity YAK1-related kinase; DYRK
Target Type Patented-recorded Target
Gene Name DYRK1A
Biochemical Class Kinase
UniProt ID
DYR1A_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2017055530
Title New Imidazo[4,5-B]Pyridine Derivatives As Dual Dyrk1/Clk1 Inhibitors.
Abstract Formula I Compounds of formula (I) usefull for the treatment of cancer, neurodegenerative disorders and metabolic disorders.
Applicant(s) Servier Lab
Representative Drug(s) D0L2XV Drug Info IC50 = 2 to 9 nM Click to Show More [1]
2 D00OWF Drug Info IC50 = 80 nM [1]
Patent ID WO2015143380
Title 5-Substituted Indazole-3-Carboxamides and Preparation and Use Thereof.
Abstract Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, fibrotic disorders, cartilage (chondral) defects, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, and neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
Applicant(s) Samumed, Llc
Representative Drug(s) D05ZHR Drug Info IC50 = 1 nM Click to Show More [1]
2 D06TIU Drug Info IC50 = 1 nM [1]
3 D0PM1B Drug Info IC50 = 2 nM [1]
4 D0K2BT Drug Info IC50 = 3 nM [1]
Patent ID WO2015118026
Title Neurodegenerative Therapies.
Abstract The present invention provides a compound of formula (I) wherein: Y represents a C or N atom which may be substituted or form a cyclic group with R'" but may not be a quaternary C atom; R' is -OR1, -CONH2, -CF3, F, -OH, -NO2, -CN or -OCOR1 in which R1, is C1-3 alkyl and each may be in the beta or gamma position; R" is C1-3 alkyl or H; and R'" is H or a group consisting of 1-12 non-hydrogen atoms and may be linear, branched and/or incorporate one or more cyclic groups, cyclic groups may be aromatic and/or heterocyclic and 2 or more cyclic groups may be linked or fused and each may be substituted; or a salt, hydrate or solvate of a compound of formula (I) for use in the treatment or prevention of a neurodegenerative disorder by inhibiting formation of neurofibrillary (tau) tangles and/or by inhibiting Dyrk 1A. The invention further relates to non-therapeutic uses of these compounds.
Applicant(s) Lytix Biopharma As
Representative Drug(s) D0I8CT Drug Info IC50 = 400 nM Click to Show More [1]
2 D0A7CE Drug Info IC50 = 800 nM [1]
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) D0CC7E Drug Info IC50 = 18 nM Click to Show More [1]
2 D09CDR Drug Info IC50 = 25 nM [1]
3 D0GE4F Drug Info IC50 = 27 nM [1]
4 D0GV3X Drug Info IC50 = 50 nM [1]
5 D09UNF Drug Info IC50 = 5500 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 = 0.22 nM Click to Show More [1]
2 D08CUF Drug Info IC50 = 0.36 nM [1]
3 D0PJ1W Drug Info IC50 = 0.94 nM [1]
4 D0DT5I Drug Info IC50 = 0.98 nM [1]
5 D0O9BK Drug Info IC50 = 0.99 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 = 4.6 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) D00TFF Drug Info IC50 = 4.6 nM Click to Show More [1]
2 D0B8IQ Drug Info IC50 = 6 nM [1]
Patent ID WO2010010797
Title Pharmaceutical Composition Comprising Dyrk-Inhibiting Compound.
Abstract Disclosed is a pharmaceutical composition for treating or preventing a disease accompanied by the increase in an activity of at least one member selected from DYRK1A, DYRK1B and DYRK2.Specifically disclosed is a pharmaceutical composition for treating or preventing a disease accompanied by the increase in an activity of at least one member selected from DYRK1A, DYRK1B and DYRK2, which comprises a compound capable of inhibiting the protein phosphorylation activity of at least one member selected from DYRK1A, DYRK1B and DYRK2 as an active ingredient.
Applicant(s) Kinopharma Co., Ltd
Representative Drug(s) D06MBI Drug Info IC50 = 0.93 nM Click to Show More [1]
2 D0RG1T Drug Info IC50 = 240 nM [1]
Patent ID WO20110041655
Title Quinazolin-4-Amine Derivatives; and Methods of Use.
Applicant(s) Department of Health and Human Services (Nih, Bethesda, Us)
Representative Drug(s) D0JQ0Z Drug Info DYRK1A IC50 = 17 nM Click to Show More [1]
2 D05BVP Drug Info DYRK1A IC50 = 27 nM [1]
Patent ID WO2009001152
Title Flow Reversing Device and Fluid Treatment Apparatus.
Abstract The invention relates to a multi-ports extracorporeal medical device (1) having a selector body (19) which can be linearly displaced within the housing (16) in order to create different flow paths and connection among the ports. The device can for instance be used for reversing the flow in an extracorporeal blood circuit.
Applicant(s) Gambro Lundia Ab
Representative Drug(s) D0Q3VZ Drug Info IC50 = 10 to 60 nM Click to Show More [1]
2 D0NS6I Drug Info IC50 = 600 to 950 nM [1]
3 D0B0AS Drug Info N.A. [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 WO2017055533
Title New Pyrrolo[2,3-D]Pyrimidine Derivatives As Dual Dyrk1/Clk1 Inhibitors.
Abstract Formula I Compounds of formula (I) usefull for the treatment of cancer, neurodegenerative disorders and metabolic disorders.
Applicant(s) Servier Lab
Patent ID WO2017040993
Title Small Molecule Inhibitors of Dyrk1A and Uses Thereof.
Abstract This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a benzimidazole or imidazopyridine structure which function as inhibitors of DYRK1A protein, and their use as therapeutics for the treatment of Alzheimer's disease, Down syndrome, glioblastoma, autoimmune diseases, inflammatory disorders (e.g., airway inflammation), and other diseases.
Applicant(s) Arizona Board of Regents On Behalf of the University of Arizona
Representative Drug(s) D03TFJ Drug Info 60 - 100% inhibition = 10000 nM [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 = 25.1 nM [1]
Patent ID WO2014096388
Title Novel Benzimidazole Derivatives As Kinase Inhibitors.
Abstract The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3-and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.
Applicant(s) Selvita Sa
Representative Drug(s) D02GEJ Drug Info IC50 = 410 nM [1]
Patent ID WO2014096093
Title 3,5-Diarylazaindoles As Dyrk1A Protein Inhibitors for The Treatment of Cognitive Deficiences Associated with Down'S Syndrome and with Alzheimer'S Disease.
Abstract The present invention relates to a compound of formula (I') or a pharmaceutically acceptable salt, solvate or hydrate thereof, in which: X3 is F, OH or SH, Y3 is F, OH or SH, X1, X2, X4, X5, 1, Y2, Y4 and Y5 are, independently of one another, H, F, Cl, Br, OH or SH, and 1 to 2 groups among the X1, X2, X4 and X5 radicals are other than H and/or 1 to 2 groups among the 1, Y2, Y4 and Y5 radicals are other than H. The present invention also relates to a compound of formula (I') for use as a medicament, in particular in the prevention and/or treatment of cognitive disorders associated with a dysfunction of the Dyrk1A protein.
Applicant(s) Centre National De La Recherche Scientifique
Patent ID WO2011135259
Title Pyrido[3,2-D]Pyrimidine Derivatives, Processes for Preparing Same and Therapeutic Uses Thereof.
Abstract The present invention relates to a compound of following general formula (I): (I) in which: - R1 is in particular H, a halogen atom or an aryl group, - R2 is in particular a halogen atom or an aryl group, - R3 is in particular a halogen atom or an aryl or heteroaryl group, and also the pharmaceutically acceptable salts thereof, the hydrates thereof or the polymorphic crystalline structures thereof, the racemates, diastereoisomers or enantiomers thereof, with the exception of the compound 1...2,4-diaminopyrido[3,2-d]pyrimidin-7-yl)-3,6,6-trimethyl-6,7-dihydro-1H-indol-4(5H)-one.
Applicant(s) Gui Limiter Gerald
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]
Patent ID WO2011068990
Title Compositions and Methods for Inhibiting Dyrk1A To Treat Central Nervous System Diseases and Disorders.
Abstract Compositions and methods for treating, preventing and/or delaying the onset and/or the development of diseases and disorders of the central nervous system are disclosed. The present disclosure relates to indoloquinoline compounds that are capable of inhibiting at least one protein kinase, and to methods for preparing and uses of such compounds. The compounds described herein are administered to patients to achieve a therapeutic effect.
Applicant(s) Medipropharma, Inc
Representative Drug(s) D0O9WA Drug Info N.A. [1]
Patent ID WO2015199503
Title Pharmaceutical Composition for Preventing and Treating Degenerative Brain Diseases, Containing Cx-4945 As Active Ingredient.
Abstract The present invention relates to a pharmaceutical composition for preventing and treating degenerative brain diseases, containing 5-[(3-chlorophenyl)amino]benzo [c]-2,6-naphthyridine-8-carboxylic acid.
Applicant(s) Korea Research Institute of Bioscience and Biotechnology
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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