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1. (WO2001002386) SELECTIVE M¿2? MUSCARINIC RECEPTOR ANTAGONISTS HAVING 5H-DIBENZ[b,f]AZEPINE STRUCTURE
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/002386 International Application No.: PCT/EP2000/006020
Publication Date: 11.01.2001 International Filing Date: 28.06.2000
IPC:
C07D 401/06 (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
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
Applicants:
TERNI, Patrizia, Maria, Luisa [IT/IT]; IT (UsOnly)
MANDELLI, Giacomina, Roberta [IT/IT]; IT (UsOnly)
MAIORANA, Stefano [IT/IT]; IT (UsOnly)
IMBIMBO, Bruno, Pietro [IT/IT]; IT (UsOnly)
MEDIOLANUM FARMACEUTICI S.P.A. [IT/IT]; Via S.G. Cottolengo, 15/31 I-20143 Milano, IT (AllExceptUS)
Inventors:
TERNI, Patrizia, Maria, Luisa; IT
MANDELLI, Giacomina, Roberta; IT
MAIORANA, Stefano; IT
IMBIMBO, Bruno, Pietro; IT
Agent:
MINOJA, Fabrizio ; Bianchetti Bracco Minoja S.r.l. Via Rossini, 8 I-20122 Milan, IT
Priority Data:
MI99A00145201.07.1999IT
Title (EN) SELECTIVE M2 MUSCARINIC RECEPTOR ANTAGONISTS HAVING 5H-DIBENZ[b,f]AZEPINE STRUCTURE
(FR) ANTAGONISTES SELECTIFS DU RECEPTEUR MUSCARINIQUE M2 PRESENTANT UNE STRUCTURE 5H-DIBENZ[b,f]AZEPINE
Abstract:
(EN) Novel 5H-dibenzo[b,f]azepine derivatives of general formula (I) wherein X-Y represents CH2-CH2, CH=CH, CH=CR3; R1 represents hydrogen or linear or branched C1-4 alkyl; R2 represents linear or branched C1-4 alkyl, phenyl, benzyl or phenethyl; R3 represents hydroxyl, linear or branched C1-4 alkoxy, phenoxyl; m and n are independently an integer 1 to 10, are disclosed. These compounds are capable of selectively blocking muscarine M2 receptors and can be used in the treatment of cardiovascular disorders, particularly bradycardias and bradyarrhythmias and in the treatment of cognitive disorders such as Alzheimer's disease.
(FR) L'invention concerne de nouveaux dérivés de la 5H-dibenzo[b,f]azépine représentés par la formule (I) dans laquelle X-Y représente CH2-CH2, CH=CH, CH=CR3; R1 représente hydrogène ou alkyle C1-4 linéaire ou ramifié; R2 représente alkyle C1-4 linéaire ou ramifié, phényle, benzyle ou phénéthyle; R3 représente hydroxyle, alcoxy C1-4 linéaire ou ramifié, phénoxyle; m et n valent indépendamment un entier compris entre 1 et 10. Ces composés sont capables de bloquer sélectivement les récepteurs muscariniques M2 et peuvent être utilisé dans le traitement de troubles cardio-vasculaires, notamment les bradycardies et les bradyarythmies, et dans le traitement de troubles cognitifs, tels que la maladie d'Alzheimer.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)