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1. (WO2007142979) USE OF GPR101 RECEPTOR IN METHODS TO IDENTIFY MODULATORS OF HYPOTHALAMIC PROOPIOMELANOCORTIN (POMC)-DERIVED BIOLOGICALLY ACTIVE PEPTIDE SECRETION USEFUL IN THE TREATMENT OF POMC-DERIVED BIOLOGICALLY ACTIVE PEPTIDE-RELATED DISORDERS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2007/142979 International Application No.: PCT/US2007/012758
Publication Date: 13.12.2007 International Filing Date: 30.05.2007
IPC:
G01N 33/557 (2006.01) ,C12Q 1/68 (2006.01) ,A61P 3/04 (2006.01) ,A61P 29/00 (2006.01)
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48
Biological material, e.g. blood, urine; Haemocytometers
50
Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53
Immunoassay; Biospecific binding assay; Materials therefor
557
using kinetic measurement, i.e. time rate of progress of an antigen-antibody interaction
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
Q
MEASURING OR TESTING PROCESSES INVOLVING ENZYMES OR MICRO-ORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1
Measuring or testing processes involving enzymes or micro-organisms; Compositions therefor; Processes of preparing such compositions
68
involving nucleic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
04
Anorexiants; Antiobesity agents
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:
BAGNOL, Didier [FR/US]; US (UsOnly)
ARENA PHARMACEUTICALS, INC. [US/US]; 6166 Nancy Ridge Drive San Diego, 5 92121-3223, US (AllExceptUS)
Inventors:
BAGNOL, Didier; US
Agent:
JAMES, S., Keddie ; Bozicevic Field & Francis LLP 1900 University Avenue, Suite 200 East Palo Alto, California 94303, US
Priority Data:
60/809,63431.05.2006US
Title (EN) USE OF GPR101 RECEPTOR IN METHODS TO IDENTIFY MODULATORS OF HYPOTHALAMIC PROOPIOMELANOCORTIN (POMC)-DERIVED BIOLOGICALLY ACTIVE PEPTIDE SECRETION USEFUL IN THE TREATMENT OF POMC-DERIVED BIOLOGICALLY ACTIVE PEPTIDE-RELATED DISORDERS
(FR) UTILISATION DU RÉCEPTEUR GPR101 DANS DES PROCÉDÉS D'IDENTIFICATION DE MODULATEURS DE LA SÉCRÉTION DE PEPTIDES ACTIFS BIOLOGIQUEMENT DÉRIVÉS DE LA PROOPIOMÉLANOCORTINE (POMC) HYPOTHALAMIQUE, UTILES DANS LE TRAITEMENT DE TROUBLES LIÉS AUX PEPTIDES ACTIFS BIOLOGIQU
Abstract:
(EN) The present invention relates to methods of using GPR101 G protein-coupled receptor (GPCR) to screen candidate compounds as modulators of hypothalamic proopiomelanocortin (POMC)-derived biologically active peptide secretion. Modulators of GPR101 receptor modulate hypothalamic POMC-derived biologically active peptide secretion and are useful in the treatment of POMC-derived biologically active peptide-related disorders. POMC-derived biologically active peptides include, but are not limited to, α-melanocyte stimulating hormone (α-MSH), β-melanocyte stimulating hormone (β-MSH) and &ggr;-melanocyte stimulating hormone (&ggr;-MSH). Agonists and partial agonists of GPR101 receptor stimulate hypothalamic α-MSH, β-MSH and &ggr;-MSH secretion and are useful, for example, in the treatment and prevention of obesity and conditions related thereto (including but not limited to Type 2 diabetes, insulin resistance, and metabolic syndrome), inflammation-associated disorders, and pyrexia. Inverse agonists and antagonists of GPR101 receptor inhibit α-MSH, β-MSH and &ggr;-MSH secretion and are useful, for example, in the treatment and prevention of disorders such as cachexia.
(FR) La présente invention concerne des procédés utilisant le récepteur couplé à la protéine G GPR101 (GPCR) pour trier des composés candidats en tant que modulateurs de la sécrétion de peptides actifs biologiquement dérivés de la proopiomélanocortine (POMC) hypothalamique. Les modulateurs du récepteur GPR101 modulent la sécrétion des peptides actifs biologiquement dérivés de la proopiomélanocortine (POMC) hypothalamique et se révèlent utiles dans le traitement de troubles liés aux peptides actifs biologiquement dérivés de la POMC. Les peptides actifs biologiquement dérivés de la POMC incluent, sans s'y limiter, l'hormone stimulant les α-mélanocytes (α-MSH), l'hormone stimulant les β-mélanocytes (β-MSH) et l'hormone stimulant les &ggr;-mélanocytes (&ggr;-MSH). Les agonistes et les agonistes partiels du récepteur GPR101 stimulent les sécrétions hypothalamiques α-MSH, β-MSH et &ggr;-MSH et se révèlent utiles, par exemple, dans le traitement et la prévention de l'obésité et des états y étant liés (incluant, sans s'y limiter, le diabète de type 2, la résistance insulinique, et le syndrome métabolique), des troubles liés à l'inflammation, et de la pyrexie. Les agonistes inverses et les antagonistes du récepteur GPR101 inhibent les sécrétions α-MSH, β-MSH et &ggr;-MSH, et se révèlent utiles, par exemple, dans le traitement et la prévention de troubles tels que la cachexie.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, 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, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, 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 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, LV, MC, MT, 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)