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1. (WO2019002571) HETEROCYCLYLMETHYLIDENE DERIVATIVES AND THEIR USE AS MODULATORS OF mGluR5 RECEPTORS
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Pub. No.: WO/2019/002571 International Application No.: PCT/EP2018/067628
Publication Date: 03.01.2019 International Filing Date: 29.06.2018
IPC:
C07D 401/14 (2006.01) ,C07D 401/06 (2006.01) ,C07D 401/10 (2006.01) ,C07D 401/12 (2006.01) ,C07D 403/06 (2006.01) ,C07D 405/06 (2006.01) ,C07D 407/10 (2006.01) ,C07D 413/12 (2006.01) ,C07D 487/04 (2006.01) ,C07D 207/20 (2006.01) ,C07D 498/04 (2006.01) ,C07D 211/70 (2006.01) ,C07D 295/195 (2006.01) ,A61P 13/02 (2006.01) ,A61K 31/4545 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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
407
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/183
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18
having one double bond between ring members or between a ring member and a non-ring member
20
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
68
having one double bond between ring members or between a ring member and a non-ring member
70
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
295
Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16
acylated on ring nitrogen atoms
18
by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
195
Radicals derived from nitrogen analogues of carboxylic acids
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
02
of urine or of the urinary tract, e.g. urine acidifiers
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
4545
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
Applicants:
RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA SPA [IT/IT]; Via Matteo Civitali 1 20148 Milano, IT
Inventors:
RIVA, Carlo; IT
GRAZIANI, Davide; IT
LONGHI, Matteo; IT
CALLEGARI, Elisa; IT
FRIGERIO, Fabio; IT
ANGELICO, Patrizia; IT
Agent:
PATENT OUTSOURCING LIMITED; 1 King Street Bakewell Derbyshire DE45 1DZ, GB
Priority Data:
62/526,76229.06.2017US
Title (EN) HETEROCYCLYLMETHYLIDENE DERIVATIVES AND THEIR USE AS MODULATORS OF mGluR5 RECEPTORS
(FR) DÉRIVÉS D'HÉTÉROCYCLYLMÉTHYLIDÈNE ET LEUR UTILISATION EN TANT QUE MODULATEURS DES RÉCEPTEURS MGLUR5
Abstract:
(EN) This invention relates to compounds of formula (I) and their use as allosteric modulators of mGluR5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction, such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related directly or indirectly to glutamate dysfunction.
(FR) La présente invention concerne des composés de formule (I) et leur utilisation en tant que modulateurs allostériques de l'activité du récepteur mGluR5, des compositions pharmaceutiques les contenant, et des procédés d'utilisation de ceux-ci en tant qu'agents dans le traitement et/ou la prévention de troubles neurologiques et psychiatriques associés à un dysfonctionnement du glutamate, tels que la schizophrénie ou un déclin cognitif, la démence ou un déficit cognitif, ou d'autres pathologies qui peuvent être associées directement ou indirectement à un dysfonctionnement du glutamate.
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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)