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1. (WO1997019059) NOVEL SUBSTITUTED ARYL COMPOUNDS USEFUL AS MODULATORS OF ACETYLCHOLINE RECEPTORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/019059 International Application No.: PCT/US1996/018569
Publication Date: 29.05.1997 International Filing Date: 14.11.1996
Chapter 2 Demand Filed: 12.06.1997
IPC:
C07D 207/08 (2006.01) ,C07D 207/12 (2006.01) ,C07D 209/94 (2006.01) ,C07D 211/54 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
08
with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
12
Oxygen or sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56
Ring systems containing three or more rings
80
[b, c]- or [b, d]-condensed
94
containing carbocyclic rings other than six-membered
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06
having no double bonds between ring members or between ring members and non-ring members
36
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
54
Sulfur atoms
Applicants:
SIBIA NEUROSCIENCES, INC. [US/US]; 505 Coast Boulevard South La Jolla, CA 92037-4641, US (AllExceptUS)
VERNIER, Jean, Michel [FR/US]; US (UsOnly)
MCDONALD, Ian, A. [AU/US]; US (UsOnly)
Inventors:
VERNIER, Jean, Michel; US
MCDONALD, Ian, A.; US
Agent:
REITER, Stephen, E.; Pretty, Schroeder, Brueggemann & Clark Suite 2000 444 South Flower Street Los Angeles, CA 90071, US
FIENER, Josef; Postfach 12 49 Maximilianstrasse 57 D-87712 Mindelheim, DE
Priority Data:
08/559,82117.11.1995US
Title (EN) NOVEL SUBSTITUTED ARYL COMPOUNDS USEFUL AS MODULATORS OF ACETYLCHOLINE RECEPTORS
(FR) NOUVEAUX COMPOSES D'ARYLE SUBSTITUES UTILES COMME MODULATEURS DES RECEPTEURS DE L'ACETYLCHOLINE
Abstract:
(EN) In accordance with the present invention, a novel class of substituted aryl compounds (containing ether, ester, amide, ketone or thioether substitution) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect, compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of displacing one or more acetylcholine receptor ligands, e.g., 3H-nicotine, from mammalian neuronal membrane binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors. Therapeutic indications for compounds with activity at acetylcholine receptors include diseases of the central nervous system such as Alzheimer's disease and other diseases involving memory loss and/or dementia (including AIDS dementia); cognitive dysfunction (including disorders of attention, focus and concentration), disorders of extrapyramidal motor function such as Parkinson's disease, progressive supramuscular palsy, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, anxiety and psychosis; substance abuse including withdrawal symptoms and substitution therapy; neurocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders or nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma, cardiovascular dysfunction including hypertension and cardiac arrhythmias, as well as co-medication uses in surgical applications.
(FR) Selon la présente invention, il a été découvert une nouvelle classe de composés d'aryle substitués (contenant une substitution éther, ester, amide, cétone ou thioéther) qui favorisent la libération de ligands impliqués dans la neurotransmission. Dans un aspect particulier, ces composés sont capables de moduler les récepteurs de l'acétylcholine, ainsi que de déplacer un ou plusieurs ligands des récepteurs de l'acétylcholine, tels que la 3H-nicotine, des sites de liaison de la membrane des neurones chez les mammifères. Ils peuvent se comporter comme des agonistes, des agonistes partiels, des antagonistes ou des modulateurs allostériques des récepteurs de l'acétylcholine. Les indications thérapeutiques des composés ayant une activité sur les récepteurs de l'acétylcholine sont les suivantes: les maladies du système nerveux central comme la maladie d'Alzheimer et d'autres pathologies accompagnées d'une perte de mémoire et/ou d'une démence (y compris la démence du sida); les troubles cognitifs (troubles de l'attention et de la concentration), les troubles de la fonction motrice extra-pyramidale comme la maladie de Parkinson, la paralysie supramusculaire progressive, la maladie de Huntington, le syndrome de Gilles de la Tourette et la dyskinésie tardive; les troubles de l'humeur et les troubles émotionnels tels que la dépression, l'angoisse et la psychose; les toxicomanies, y compris les symptômes de manque et la thérapie de substitution; les troubles endocriniens et la dysrégulation de la prise alimentaire, y compris la boulimie et l'anorexie; les troubles de la nociception et la lutte contre la douleur; les perturbations du système nerveux autonome telles que les troubles de la motilité et du fonctionnement gastro-intestinal, notamment les maladies intestinales inflammatoires, le syndrome de l'intestin irritable, la diarrhée, la constipation, l'hypersécrétion d'acide gastrique et les ulcères; le phéochromocytome, les troubles cardio-vasculaires y compris l'hypertension et les arythmies cardiaques. Ces composés peuvent également être utilisés en tant que co-médication en chirurgie.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TR, TT, UA, UG, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, 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, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0874818US6316490JP3969741 JP2000501080CA2237752AU1997010782