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1. (WO2018202694) HETEROCYCLIC P2X7 ANTAGONISTS
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Pub. No.: WO/2018/202694 International Application No.: PCT/EP2018/061180
Publication Date: 08.11.2018 International Filing Date: 02.05.2018
IPC:
C07D 271/07 (2006.01) ,C07D 285/08 (2006.01) ,C07D 413/06 (2006.01) ,C07D 417/06 (2006.01) ,A61K 31/4245 (2006.01) ,A61K 31/433 (2006.01) ,A61P 1/00 (2006.01) ,A61P 11/00 (2006.01) ,A61P 13/00 (2006.01) ,A61P 25/00 (2006.01) ,A61P 27/02 (2006.01) ,A61P 29/00 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
271
Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
06
1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
07
with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
01
Five-membered rings
02
Thiadiazoles; Hydrogenated thiadiazoles
04
not condensed with other rings
08
1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
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
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
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
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
4245
Oxadiazoles
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
433
Thiadiazoles
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
11
Drugs for disorders of the respiratory 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
25
Drugs for disorders of the nervous system
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)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
AXXAM S.P.A. [IT/IT]; Via Meucci, 3 20091 BRESSO (MI), IT
Inventors:
PEVARELLO, Paolo; IT
SODANO, Mariangela; IT
SEVERI, Elda; IT
VITALONE, Rocco; IT
THOMAS, Russell; IT
CUSANO, Valentina; IT
Agent:
BARCHIELLI, Giovanna; IT
Priority Data:
17169277.503.05.2017EP
Title (EN) HETEROCYCLIC P2X7 ANTAGONISTS
(FR) ANTAGONISTES HÉTÉROCYCLIQUES DE P2X7
Abstract:
(EN) The present invention refers to compounds of the following formula (I) or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions containing them and to a process for the preparation of said compounds: Formula (I), wherein: R1 is independently selected from hydrogen atom, amine group, monocyclic or bicyclic aliphatic, aromatic, heteroaliphatic or heteroaromatic ring, optionally substituted by one or more substituents selected from C1-C4 alkyl optionally substituted by one or more halogen atom(s), halogen, C1-C4 alkoxy or phenyl group, optionally substituted by C1-C4 alkyl; R2 is independently selected from monocyclic or bicylic aliphatic, heteroaliphatic, aromatic or heteroaromatic ring, C1-C6 alkyl, alkenyl or alkynyl chain, optionally substituted by one or more substituents selected from C1-C4 alkyl optionally substituted by one or more halogen atom(s), halogen, C1-C4 alkoxy, cyano, C1-C4 alkylthio, SO-C1-C4 alkyl, SO2-C1-C4 alkyl, N(C1-C4 alkyl)2; n is 1 or 2; preferably n is 1; m is 0, 1 or 2; preferably m is 0; R3 and R4 can be, independently, -H, -F, C1-C4 alkyl, -OH, -OC1-C4 alkyl; preferably they are both -H; X is O or S; R5 is -H or -CH3 optionally substituted by one or more fluorine atoms; preferably R5 is hydrogen. The compounds of the invention can be used in the treatment of conditions or diseases mediated by P2X7 receptor.
(FR) La présente invention concerne des composés de formule (I) suivante ou un sel pharmaceutiquement acceptable de ceux-ci, des compositions pharmaceutiques les contenant et un procédé de préparation desdits composés : formule (I), dans laquelle : R1 est indépendamment choisi parmi un atome d'hydrogène, un groupe amine, un cycle aliphatique, aromatique, hétéroaliphatique ou hétéroaromatique, monocyclique ou bicyclique, éventuellement substitué par un ou plusieurs substituants choisis parmi un alkyle en C1-C4 éventuellement substitué par un ou plusieurs atomes d'halogène, halogène, groupe alcoxy en C1-C4 ou groupe phényle, éventuellement substitué par un alkyle en C1-C4 ; R2 est indépendamment choisi parmi un cycle aliphatique, hétéroaliphatique, aromatique ou hétéroaromatique, monocyclique ou bicyclique, alkyle en C1-C6, chaîne alcényle ou chaîne alcynyle, éventuellement substitué par un ou plusieurs substituants choisis parmi alkyle en C1-C4 éventuellement substitué par un ou plusieurs atomes d'halogène, halogène, alcoxy en C1-C4, cyano, alkylthio en C1-C4, alkyle en SO-C1-C4, alkyle en SO2-C1-C4, N(alkyle en C1-C4)2 ; n vaut 1 ou 2 ; de préférence n vaut 1 ; m vaut 0, 1 ou 2 ; de préférence m vaut 0 ; R3 et R4 peuvent être, indépendamment, -H, -F, alkyle en C1-C4, -OH, alkyle en -OC1-C4 ; de préférence, sont ensemble -H ; X représente O ou S ; R5 représente -H ou -CH3 éventuellement substitué par un ou plusieurs atomes de fluor ; de préférence R5 représente l'hydrogène. Les composés de l'invention peuvent être utilisés dans le traitement d'états pathologiques ou de maladies à médiation par le récepteur P2X7.
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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)