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1. (WO2010073011) HETEROCYCLIC COMPOUNDS AND THEIR USE AS AMPK ACTIVATORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/073011 International Application No.: PCT/GB2009/002945
Publication Date: 01.07.2010 International Filing Date: 22.12.2009
IPC:
C07D 285/135 (2006.01) ,A61K 31/433 (2006.01) ,A61P 35/00 (2006.01) ,A61P 3/00 (2006.01) ,A61P 11/00 (2006.01) ,A61P 9/00 (2006.01) ,A61P 17/00 (2006.01) ,A61P 25/00 (2006.01) ,A61P 15/00 (2006.01) ,A61P 19/00 (2006.01) ,A61P 29/00 (2006.01) ,A61P 27/00 (2006.01) ,C07D 417/06 (2006.01) ,C07D 417/12 (2006.01) ,C07D 285/125 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
01
Five-membered rings
02
Thiadiazoles; Hydrogenated thiadiazoles
04
not condensed with other rings
12
1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
125
with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
135
Nitrogen atoms
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
433
Thiadiazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
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)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27
Drugs for disorders of the senses
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
01
Five-membered rings
02
Thiadiazoles; Hydrogenated thiadiazoles
04
not condensed with other rings
12
1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
125
with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
Applicants:
BETAGENON AB [SE/SE]; Box 2339 S-103 18 Stockholm, SE (AllExceptUS)
WESTMAN, Jacob [SE/SE]; SE (UsOnly)
Inventors:
WESTMAN, Jacob; SE
Agent:
McNEENEY, Stephen; Potter Clarkson LLP Park View House 58 The Ropewalk Nottingham NG1 5DD, GB
Priority Data:
61/193,77423.12.2008US
61/202,08427.01.2009US
61/202,87915.04.2009US
61/241,46311.09.2009US
Title (EN) HETEROCYCLIC COMPOUNDS AND THEIR USE AS AMPK ACTIVATORS
(FR) COMPOSÉS UTILES COMME MÉDICAMENTS
Abstract:
(EN) There is provided a compound of formula (I), wherein the dotted lines, X, T, G, Y, A1 to A5 and D1 to D5 have meanings given in the description, which compounds are useful in the treatment of conditions or disorders ameliorated by the activation of AMPK, for example skin diseases, lung disease, obesity, dry-type age-related macular degeneration, cardioprotection or, preferably, hyperinsulinemia, diabetes, cancer, fibrosis, neurodegenerative diseases, sexual dysfunction, heart failure, inflammation and osteoporosis.
(FR) La présente invention concerne des composés de formule I dans laquelle les lignes pointillées, X, T, G, N, Y, A1 à A5 et D1 à D5 prennent les significations données dans la description. Ces composés sont utiles dans le traitement d'états ou de troubles améliorés par l'activation de l'AMPK, par exemple les maladies de la peau, les maladies pulmonaires, l'obésité, la dégénérescence maculaire liée à l'âge de type sec, la cardioprotection ou, de préférence, l'hyperinsulinémie, le diabète, le cancer, la fibrose, les maladies neurodégénératives, les dysfonctionnements sexuels, l'insuffisance cardiaque, l'inflammation et l'ostéoporose.
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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, 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)