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1. (WO2018220542) 1,3-DIAZO-4-OXA-[3.3.1]-BICYCLIC DERIVATIVES, PROCESS FOR THEIR MANUFACTURE AND THEIR USE AS A MEDICAMENT, IN PARTICULAR FOR TREATING DIABETES
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Pub. No.: WO/2018/220542 International Application No.: PCT/IB2018/053834
Publication Date: 06.12.2018 International Filing Date: 30.05.2018
IPC:
C07D 498/08 (2006.01) ,A61K 31/5395 (2006.01) ,A61P 3/00 (2006.01)
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
08
Bridged systems
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
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5395
having two or more nitrogen atoms in the same ring, e.g. oxadiazines
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
Applicants:
UNIVERSITA' DI PISA [IT/IT]; Lungarno Antonio Pacinotti 43/44 56126 Pisa, IT
Inventors:
BERTI, Francesco; IT
PINESCHI, Mauro; IT
MENICHETTI, Andrea; IT
Agent:
BIGGI, Cristina; IT
ROSSETTI, Elena; IT
ERRICO, Michela; IT
Priority Data:
10201700005929231.05.2017IT
Title (EN) 1,3-DIAZO-4-OXA-[3.3.1]-BICYCLIC DERIVATIVES, PROCESS FOR THEIR MANUFACTURE AND THEIR USE AS A MEDICAMENT, IN PARTICULAR FOR TREATING DIABETES
(FR) DÉRIVÉS 1,3-DIAZO-4-OXA-[3.3.1]-BICYCLIQUES, PROCÉDÉ POUR LEUR FABRICATION ET LEUR UTILISATION EN TANT QUE MÉDICAMENT, EN PARTICULIER POUR LE TRAITEMENT DU DIABÈTE
Abstract:
(EN) The present invention relates to compounds having structural formula (I) wherein R1 and R2 are defined as set forth in the description. The invention also relates to a process for the manufacture of the above compounds of formula (I), wherein a 4a,7, 8, 8a-tetrahydropyrido[4,3-e]-1,4,2-dioxazine reacts with a hydride selected from the group consisting of: lithium triethylborohydride (LiBHEt3), sodium triethylborohydride (NaBHEt3), and lithium tetrahydroaluminate (LiAIH4), in the presence of tetrahydrofuran. Furthermore, the invention is aimed at the above compounds of formula (I), or pharmaceutically acceptable salts thereof, for use in medicine, preferably in the treatment of the diabetes and pathologies or conditions correlated thereto.
(FR) La présente invention concerne des composés ayant la formule structurale (I) dans laquelle R1 et R2 sont tels que définis dans la description. L'invention concerne également un procédé de fabrication des composés ci-dessus de formule (I), où un 4a,7,8,8a-tétrahydropyrido[4,3-e]-1,4,2-dioxazine réagit avec un hydrure choisi dans le groupe constitué par : le triéthyl-borohydrure de lithium (LiBHEt3), le triéthyl-borohydrure de sodium (NaBHEt3), et le tétrahydroaluminate de lithium (LiAIH4), en présence de tétrahydrofurane. En outre, l'invention concerne les composés ci-dessus de formule (I), ou des sels pharmaceutiquement acceptables de ceux-ci, destinés à être utilisés en médecine, de préférence dans le traitement du diabète et de pathologies ou d'états corrélés au diabète.
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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: Italian (IT)