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 |
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[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 |
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[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 |
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[1] |
2
|
D0X0ZC
|
Drug Info
|
IC50 = 700 nM
|
[1] |
3
|
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 |
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[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 |
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[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 |
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[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 |
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[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 |
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[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) |
D0UY8K |
Drug Info
|
DYRK1A IC50 = 14 nM |
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[1] |
2
|
D0JQ0Z
|
Drug Info
|
DYRK1A IC50 = 17 nM
|
[1] |
3
|
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 |
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[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. |
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[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 |
Representative Drug(s) |
D0YT1S |
Drug Info
|
IC50 = 2 to 9 nM |
[1] |
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 |
Representative Drug(s) |
D0X8NN |
Drug Info
|
IC50 = 3 nM |
[1] |
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 |
Representative Drug(s) |
D0X5MW |
Drug Info
|
IC50 = 60 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] |
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] |