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1. (WO2019063414) INHIBITORS OF GLUTAMINYL CYCLASE
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Pub. No.: WO/2019/063414 International Application No.: PCT/EP2018/075494
Publication Date: 04.04.2019 International Filing Date: 20.09.2018
IPC:
C07D 403/04 (2006.01) ,C07D 471/04 (2006.01) ,A61K 31/4184 (2006.01) ,A61P 25/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
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
4164
1,3-Diazoles
4184
condensed with carbocyclic rings, e.g. benzimidazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Applicants:
PROBIODRUG AG [DE/DE]; Weinbergweg 22 Halle (Saale), 06120, DE
Inventors:
HEISER, Ulrich; DE
SOMMER, Robert; DE
Agent:
MAIKOWSKI & NINNEMANN PATENTANWÄLTE PARTNERSCHAFT MBB; Postfach 15 09 20 10671 Berlin, DE
Priority Data:
17194164.429.09.2017EP
Title (EN) INHIBITORS OF GLUTAMINYL CYCLASE
(FR) INHIBITEURS DE GLUTAMINYLE CYCLASE
Abstract:
(EN) The invention relates to a compound of formula (I): Formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein A is heteraryl selected from 1 H-benzimidazolyl and imidazo[1,2-a]pyridine, and R1, R2, R3, R4 and R5 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5) and its isoenzyme glutaminyl-peptide cyclotransferase-like protein (QPCTL). QC and QPCTL catalyze the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
(FR) L'invention concerne un composé de formule (I) : formule (I) ou un sel, un solvate ou un polymorphe pharmaceutiquement acceptables de celui-ci, y compris tous les tautomères et stéréoisomères de celui-ci, dans la formule, A est un hétéroaryle choisi parmi 1 H-benzimidazolyle et imidazo[1,2-a]pyridine, et R1, R2, R3, R4 et R5 sont tels que définis dans la description, le composé selon l'invention est utilisé en tant qu'inhibiteurs de la glutaminyle cyclase (QC, EC 2.3.2.5) et de sa protéine de type isoenzyme glutaminyl-peptide cyclotransférase (QPCTL). Selon l'invention, QC et QPCTL catalysent la cyclisation intramoléculaire de résidus glutamine N-terminaux en acide pyroglutamique (5-oxo-prolyle, pGlu*) avec libération d'ammoniac, et la cyclisation intramoléculaire de résidus glutamate N-terminaux en acide pyroglutamique avec libération d'eau.
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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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, 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)