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1. (WO2017040993) SMALL MOLECULE INHIBITORS OF DYRK1A AND USES THEREOF
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Pub. No.: WO/2017/040993 International Application No.: PCT/US2016/050198
Publication Date: 09.03.2017 International Filing Date: 02.09.2016
IPC:
A01N 43/00 (2006.01) ,C07D 513/04 (2006.01) ,C07D 487/04 (2006.01) ,A61K 31/43 (2006.01)
A HUMAN NECESSITIES
01
AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
N
PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
43
Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
513
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
429
condensed with heterocyclic ring systems
43
Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
Applicants:
ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA [US/US]; The University of Arizona, Tech Transfer Arizona, University Services Annex, 4th Floor, P.O. Box 210300A Tucson, Arizona 85721, US
THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE [US/US]; 445 N. 5th Street, Suite 600 Phoenix, 85004, US
Inventors:
HULME, Christopher; US
DUNCKLEY, Travis; US
SHAW, Yeng-Jeng; US
Agent:
GOETZ, Robert A.; US
Priority Data:
62/213,90403.09.2015US
Title (EN) SMALL MOLECULE INHIBITORS OF DYRK1A AND USES THEREOF
(FR) PETITES MOLÉCULES INHIBITRICES DE DYRK1A ET LEURS UTILISATIONS
Abstract:
(EN) 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.
(FR) La présente invention concerne le domaine de la chimie médicale. En particulier, l'invention concerne une nouvelle classe de petites molécules ayant une structure benzimidazole ou imidazopyridine dont la fonction est d'inhiber la protéine DYRK1A, et leur utilisation en tant qu'agents thérapeutiques pour le traitement de la maladie d'Alzheimer, de la trisomie 21, du glioblastome, des maladies auto-immunes, des troubles inflammatoires (par exemple l'inflammation des voies aériennes) et d'autres maladies.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)