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1. (WO2005108402) 3,6-DIAZABICYCLOS[3.1.1]HEPTANE DERIVATIVES WITH ANALGESIC ACTIVITY
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2005/108402 International Application No.: PCT/EP2005/004994
Publication Date: 17.11.2005 International Filing Date: 09.05.2005
IPC:
A61K 31/4995 (2006.01) ,C07D 487/08 (2006.01)
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4995
Pyrazines or piperazines forming part of bridged ring systems
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
08
Bridged systems
Applicants:
PINNA, Gérard, Aimé [IT/IT]; IT (UsOnly)
LORIGA, Giovanni [IT/IT]; IT (UsOnly)
CIGNARELLA, Giorgio [IT/IT]; IT (UsOnly)
UNIVERSITA' DEGLI STUDI DI MILANO [IT/IT]; Via Festa del Perdono, 7 I-20122 Milan, IT (AllExceptUS)
UNIVERSITA' DEGLI STUDI DI SASSARI [IT/IT]; Piazza Università, 21 I-07100 Sassari, IT (AllExceptUS)
Inventors:
PINNA, Gérard, Aimé; IT
LORIGA, Giovanni; IT
CIGNARELLA, Giorgio; IT
Agent:
BIANCHETTI, Giuseppe ; Bianchetti Bracco Minoja S.r.l. Via Plinio, 63 I-20129 Milano, IT
Priority Data:
MI2004A00095412.05.2004IT
Title (EN) 3,6-DIAZABICYCLOS[3.1.1]HEPTANE DERIVATIVES WITH ANALGESIC ACTIVITY
(FR) DERIVES DE 3,6-DIAZABICYCLO[3.1.1]HEPTANE PRESENTANT UNE ACTIVITE ANALGESIQUE
Abstract:
(EN) The invention relates to compounds of general formula (I), wherein R and R1, different from one another, are: a C2-C8 straight or branched acyl group; and a group of formula (II), wherein B and R2 are as defined in the description. The compounds (I) have higher central analgesic activity than morphine and are substantially free from the side effects of morphine or other central analgesics. The invention further relates to a process for the preparation of the compounds (I).
(FR) L'invention concerne des composés représentés par la formule générale (I). Dans cette formule R et R1 sont différents et désignent un groupe acyle droit ou ramifié en C2-C8 et un groupe représenté par la formule générale (II) dans laquelle B et R2 désignent des éléments indiqués dans la description. Ces composés (I) présentent une activité analgésique centrale supérieure à celle de la morphine et n'entraînent aucun des effets secondaires de la morphine ou d'autres analgésiques centraux. L'invention concerne également un procédé destiné à la préparation de ces composés (I).
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, 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 Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, MC, NL, PL, PT, RO, SE, SI, SK, 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)