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1. (WO2018083247) 4,4A,5,7-TETRAHYDRO-3H-FURO[3,4-B]PYRIDINYL COMPOUNDS
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Pub. No.: WO/2018/083247 International Application No.: PCT/EP2017/078200
Publication Date: 11.05.2018 International Filing Date: 03.11.2017
IPC:
C07D 491/048 (2006.01) ,A61K 31/4355 (2006.01) ,A61P 25/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
044
with only one oxygen atom as ring hetero atom in the oxygen-containing ring
048
the oxygen-containing ring being five-membered
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
4353
ortho- or peri-condensed with heterocyclic ring systems
4355
the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
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: JANSSEN PHARMACEUTICA NV[BE/BE]; Turnhoutseweg 30 2340 Beerse, BE
Inventors: VAN BRANDT, Sven, Franciscus, Anna; BE
GIJSEN, Henricus, Jacobus, Maria; BE
ROMBOUTS, Frederik, Jan, Rita; BE
Agent: GARCIA PRIETO, Maria; BE
Priority Data:
16197351.604.11.2016EP
17162307.722.03.2017EP
Title (EN) 4,4A,5,7-TETRAHYDRO-3H-FURO[3,4-B]PYRIDINYL COMPOUNDS
(FR) COMPOSÉS DE 4,4 A, 5,7-TÊTRAHYDRO -3 H-FURO [3,4-B]PYRIDINYL
Abstract:
(EN) The present invention relates to 4,4a,5,7-tetrahydro-3H-furo[3,4-b]pyridinyl compound inhibitors of beta-site APP-cleaving enzyme having the structure shown in Formula (I) wherein the radicals are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-site APP- cleaving enzyme is involved, such as Alzheimer's disease (AD), mild cognitive impairment, preclinical Alzheimer's disease, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, and dementia associated with beta-amyloid.
(FR) La présente invention concerne un composé de 4,4a,5,7-têtrahydro-3H-furo[3,4-b]pyridinyl, inhibiteurs d'enzyme de clivage du site ß de l'APP ayant la structure représentée dans la formule (I), les radicaux étant tels que définis dans la description. L'invention concerne en outre des compositions pharmaceutiques comprenant lesdits composés, des procédés permettant de préparer lesdits composés et lesdites compositions, et l'utilisation desdits composés et desdites compositions pour la prévention et le traitement de troubles dans lesquels l'enzyme de clivage du site ß de l'APP est impliquée, comme la maladie d'Alzheimer (AD), le trouble cognitif léger, la maladie d'Alzheimer préclinique, la sénilité, la démence, la démence à corps de Lewy, le syndrome de Down, la démence associée à un accident vasculaire cérébral, la démence associée à la maladie de Parkinson et la démence associée à la bêta-amyloïde.
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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)