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1. (WO2010074587) 5-O-SUBSTITUTED 3-N-ARYL-1,3,4-OXADIAZOLONES FOR MEDICAL USE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/074587 International Application No.: PCT/PT2009/000079
Publication Date: 01.07.2010 International Filing Date: 23.12.2009
IPC:
C07D 285/13 (2006.01) ,C07D 413/12 (2006.01) ,C07D 413/14 (2006.01) ,A61K 31/4245 (2006.01) ,A61K 31/4709 (2006.01)
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
12
1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
125
with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
13
Oxygen atoms
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
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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
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
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
Applicants:
BIAL - PORTELA & CA., S.A. [PT/PT]; À Av. Da Siderurgia Nacional P-4745-457 S. Mamede do Coronado, PT (AllExceptUS)
LEARMONTH, David Alexander [GB/PT]; PT (UsOnly)
SILVA, Patrício Manuel Vieira Araújo Soares da [PT/PT]; PT (UsOnly)
Inventors:
LEARMONTH, David Alexander; PT
SILVA, Patrício Manuel Vieira Araújo Soares da; PT
Agent:
MOREIRA, Pedro Alves; Rua do Patrocínio, 94 P-1399 - 019 Lisboa, PT
Priority Data:
61/203,54923.12.2008US
Title (EN) 5-O-SUBSTITUTED 3-N-ARYL-1,3,4-OXADIAZOLONES FOR MEDICAL USE
(FR) 3-N-ARYL-1,3,4-OXADIAZOLONES 5-O-SUBSTITUÉES DESTINÉES À UNE UTILISATION MÉDICALE
Abstract:
(EN) The present invention relates to a compound of formula (I), wherein A represents an optionally substituted phenyl or a 5- or 6-membered heteroaromatic ring system containing up to 4 heteroatoms selected from O, S and N, B represents a single bond, O, S or NR1, wherein R1 is selected from hydrogen or a C1-C6-alkyl group; L represents a linker; C represents an amino moiety; n represents 0 or 1; m represents 0, 1, 2, 3, 4, 5 or 6; X represents O or S; and Y represents hydrogen or an optionally substituted carbon moiety; and to stereoisomers, pharmaceutically acceptable salts or esters, or prodrugs thereof. The compounds of the invention are potent FAAH inhibitors.
(FR) La présente invention concerne un composé de formule (I), dans laquelle A représente un groupe phényl facultativement substitué ou un système cyclique hétéroaromatique à 5 ou 6 chaînons contenant jusqu'à 4 hétéroatomes choisis parmi O, S et N, B représente une liaison simple, O, S ou NR1, R1 étant choisi parmi un atome d'hydrogène ou un groupe alkyle en C1-C6; L représente un liant; C représente une fraction amino; n représente 0 ou 1; m représente 0, 1, 2, 3, 4, 5 ou 6; X représente O ou S; et Y représente un atome d'hydrogène ou une fraction carbone facultativement substituée; et leurs stéréoisomères, leurs sels ou esters pharmaceutiquement acceptables, ou leurs promédicaments. Les composés de l'invention sont de puissants inhibiteurs de la FAAH.
front page image
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, 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, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)