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1. (WO2018041563) SUBSTITUTED N-[2-(4-PHENOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE AND N-[2-(4-BENZYLOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE DERIVATIVES P2X7 RECEPTOR ANTAGONISTS
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Pub. No.: WO/2018/041563 International Application No.: PCT/EP2017/070163
Publication Date: 08.03.2018 International Filing Date: 09.08.2017
Chapter 2 Demand Filed: 11.06.2018
IPC:
C07D 417/06 (2006.01) ,C07D 417/14 (2006.01) ,A61K 31/454 (2006.01) ,A61K 31/4709 (2006.01) ,A61P 1/00 (2006.01) ,A61P 13/00 (2006.01) ,A61P 21/00 (2006.01) ,A61P 25/28 (2006.01) ,A61P 27/02 (2006.01) ,A61P 29/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14
containing three or more hetero rings
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
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
454
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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
47
Quinolines; Isoquinolines
4709
Non-condensed quinolines containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13
Drugs for disorders of the urinary system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
21
Drugs for disorders of the muscular or neuromuscular system
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27
Drugs for disorders of the senses
02
Ophthalmic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
Applicants:
AXXAM S.P.A. [IT/IT]; Via Meucci, 3 20091 BRESSO (MI), IT
Inventors:
PEVARELLO, Paolo; IT
PRANDI, Adolfo; IT
Agent:
BARCHIELLI, Giovanna; IT
Priority Data:
16186655.331.08.2016EP
Title (EN) SUBSTITUTED N-[2-(4-PHENOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE AND N-[2-(4-BENZYLOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE DERIVATIVES P2X7 RECEPTOR ANTAGONISTS
(FR) N-[2-(4-PHÉNOXYPIPÉRIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ÉTHYL]BENZAMIDE SUBSTITUÉ ET DÉRIVÉS DE N-[2-(4-BENZYLOXYPIPÉRIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ÉTHYL]BENZAMIDE EN TANT QU'ANTAGONISTES DU RÉCEPTEUR P2X7
Abstract:
(EN) The present invention relates to novel substituted phenoxy- and benzyloxy-piperidine compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.
(FR) La présente invention concerne de nouveaux composés phénoxy- et benzyloxy-pipéridine substitués de formule (I) ayant des propriétés antagonistes du récepteur P2X7 (P2X7), des compositions pharmaceutiques comprenant ces composés, des procédés chimiques pour préparer ces composés et leur utilisation dans le traitement ou la prophylaxie de maladies associées à l'activité du récepteur P2X7 chez des animaux, en particulier des êtres humains.
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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)