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1. (WO2010084184) N-OXIDES OF DIAZABICYCLONONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/084184 International Application No.: PCT/EP2010/050759
Publication Date: 29.07.2010 International Filing Date: 25.01.2010
IPC:
C07D 471/08 (2006.01) ,A61K 31/53 (2006.01) ,A61P 25/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
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
53
having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Applicants:
NEUROSEARCH A/S [DK/DK]; Pederstrupvej 93 DK-2750 Ballerup, DK (AllExceptUS)
PETERS, Dan [SE/DK]; DK (UsOnly)
TIMMERMANN, Daniel, B. [DK/DK]; DK (UsOnly)
CHRISTOFFERSEN, Eva, Dam [DK/DK]; DK (UsOnly)
NIELSEN, Elsebet, Østergaard [DK/DK]; DK (UsOnly)
Inventors:
PETERS, Dan; DK
TIMMERMANN, Daniel, B.; DK
CHRISTOFFERSEN, Eva, Dam; DK
NIELSEN, Elsebet, Østergaard; DK
Agent:
NeuroSearch A/S; Pederstrupvej 93 DK-2750 Ballerup, DK
Priority Data:
61/148,14529.01.2009US
PA 2009 0012026.01.2009DK
Title (EN) N-OXIDES OF DIAZABICYCLONONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE
(FR) N-OXYDES DE DÉRIVÉS DE DIAZABICYCLONONYLE PYRIMIDINE ET LEUR UTILISATION MÉDICALE
Abstract:
(EN) This invention relates to novel N-oxides of certain diazabicyclononyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
(FR) La présente invention concerne de nouveaux N-oxydes de certains dérivés diazabicyclononyle pyrimidine et leur utilisation dans la fabrication de compositions pharmaceutiques. On a découvert que les composés de l'invention sont des ligands cholinergiques sur les récepteurs nicotiniques d'acétylcholine et des modulateurs de transporteurs et de récepteurs de monoamine. En raison de leur profil pharmacologique, les composés de l'invention peuvent être utiles dans le traitement de maladies et de troubles aussi divers que ceux liés au système cholinergique du système nerveux central (SNC), le système nerveux périphérique (SNP), aux maladies ou troubles liés à la contraction des muscles mous, aux maladies ou troubles endocriniens, aux maladies ou troubles liés à la neuro-dégénérescence, aux maladies ou troubles liés à l'inflammation, à la douleur, et aux symptômes de sevrage liés à l'arrêt de l'abus de substances chimiques.
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, 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, 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)
Also published as:
EP2389380US20120004215CN102292336CA2750447