Search International and National Patent Collections
Some content of this application is unavailable at the moment.
If this situation persists, please contact us atFeedback&Contact
1. (WO2010084120) N-OXIDES OF 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/084120 International Application No.: PCT/EP2010/050607
Publication Date: 29.07.2010 International Filing Date: 20.01.2010
IPC:
C07D 471/06 (2006.01) ,A61K 31/4375 (2006.01) ,A61P 5/00 (2006.01) ,A61P 25/28 (2006.01) ,A61P 25/30 (2006.01) ,A61P 29/00 (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
06
Peri-condensed 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
435
having six-membered rings with one nitrogen as the only ring hetero atom
4353
ortho- or peri-condensed with heterocyclic ring systems
4375
the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5
Drugs for disorders of the endocrine system
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
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
30
for treating abuse or dependence
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
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)
Inventors:
PETERS, Dan; DK
TIMMERMANN, Daniel, B.; DK
CHRISTOFFERSEN, Eva, Dam; DK
Common
Representative:
NEUROSEARCH A/S; Pederstrupvej 93 DK-2750 Ballerup, DK
Priority Data:
61/146,47822.01.2009US
PA 2009 0009021.01.2009DK
Title (EN) N-OXIDES OF 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
(FR) N-OXYDES DE DÉRIVÉS DE 1,4-DIAZA-BICYCLO[3.2.2]NONYLPYRIMIDINYLE UTILES EN TANT QUE LIGANDS DES RÉCEPTEURS NICOTINIQUES DE L'ACÉTYLCHOLINE
Abstract:
(EN) This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl 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. 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. Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein Ar represents an indolyl group, which indolyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, triflυoromethoxy, cyano, nitro, amino, alkyl, hydroxy and alkoxy.
(FR) L'invention concerne de nouveaux dérivés de 1,4-diaza-bicyclo[3.2.2]nonylpyrimidinyle et leur utilisation pour la fabrication de compositions pharmaceutiques. Il a été découvert que les composés de l'invention sont des ligands cholinergiques des récepteurs nicotiniques de l'acétylcholine. En raison de leur profil pharmacologique, les composés de l'invention peuvent être utiles pour le traitement de maladies ou de troubles aussi divers que ceux associés au système cholinergique du système nerveux central (SNC), du système nerveux périphérique (SNP), de maladies ou de troubles associés à la contraction de muscles lisses, de maladies ou de troubles endocriniens, de maladies ou de troubles associés à la neuro-dégénération, de maladies ou de troubles associés à l'inflammation, la douleur et les symptômes de sevrage provoqués par l'arrêt de l'abus de substances chimiques. Formule (I) un stéréoisomère ou un mélange de ses stéréoisomères, ou un de ses sels pharmaceutiquement acceptables, dans laquelle Ar représente un groupe indolyle, ledit indolyle pouvant éventuellement être substitué une ou plusieurs fois par des substituants choisis parmi halogéno, trifluorométhyle, trifluorométhoxy, cyano, nitro, amino, alkyle, hydroxy et alcoxy.
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, 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:
US20120004214