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1. (WO2009074789) AMIDO-THIOPHENE COMPOUNDS AND THEIR USE AS 11-BETA-HSD1 INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2009/074789 International Application No.: PCT/GB2008/004068
Publication Date: 18.06.2009 International Filing Date: 11.12.2008
IPC:
C07D 333/38 (2006.01) ,C07D 409/06 (2006.01) ,C07D 409/14 (2006.01) ,C07D 413/14 (2006.01) ,C07D 453/02 (2006.01) ,C07D 471/04 (2006.01) ,A61K 31/381 (2006.01) ,A61P 3/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02
not condensed with other rings
04
not substituted on the ring sulfur atom
26
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
38
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
453
Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
02
containing not further condensed quinuclidine ring systems
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
04
Ortho-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
38
having sulfur as a ring hetero atom
381
having five-membered rings
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
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
Applicants:
WEBSTER, Scott, Peter [GB/GB]; GB (UsOnly)
SECKL, Jonathan, Robert [GB/GB]; GB (UsOnly)
WALKER, Brian, Robert [GB/GB]; GB (UsOnly)
WARD, Peter [GB/GB]; GB (UsOnly)
PALLIN, Thomas, David [GB/GB]; GB (UsOnly)
DYKE, Hazel, Joan [GB/GB]; GB (UsOnly)
PERRIOR, Trevor, Robert [GB/GB]; GB (UsOnly)
THE UNIVERSITY OF EDINBURGH [GB/GB]; Old College South Bridge Edinburgh Lothian EH8 9YL, GB (AllExceptUS)
Inventors:
WEBSTER, Scott, Peter; GB
SECKL, Jonathan, Robert; GB
WALKER, Brian, Robert; GB
WARD, Peter; GB
PALLIN, Thomas, David; GB
DYKE, Hazel, Joan; GB
PERRIOR, Trevor, Robert; GB
Agent:
WYTENBURG, Wilhelmus ; Mewburn Ellis LLP 33 Gutter Lane London Greater London EC2V 8AS, GB
Priority Data:
0724251.412.12.2007GB
61/013,04212.12.2007US
Title (EN) AMIDO-THIOPHENE COMPOUNDS AND THEIR USE AS 11-BETA-HSD1 INHIBITORS
(FR) COMPOSÉS AMIDO-THIOPHÈNE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE 11-BÊTA-HSD1
Abstract:
(EN) The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc. Formula (I).
(FR) La présente invention concerne de manière générale le domaine des composés thérapeutiques. La présente invention concerne plus spécifiquement certains composés amido-thiophène qui, entre autres, inhibent la 11β-hydroxystéroïde déshydrogénase de type 1 (11β-HSD1). La présente invention concerne également des compositions pharmaceutiques qui comprennent de tels composés et l'utilisation de tels composés et de telles compositions, à la fois in vitro et in vivo, pour inhiber la 11β-hydroxystéroïde déshydrogénase de type 1; pour traiter des troubles qui sont améliorés par l'inhibition de la 11β-hydroxystéroïde déshydrogénase de type 1; pour traiter le syndrome métabolique, qui inclut des troubles tels que le diabète de type 2 et l'obésité et les troubles associés, notamment la résistance à l'insuline, l'hypertension, les troubles lipidiques, et les troubles cardiovasculaires tels que la coronaropathie ischémique; pour traiter des troubles du SNC tels que la déficience cognitive légère et la démence précoce, notamment la maladie d'Alzheimer, etc.
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Designated States: AE, AG, AL, AM, AO, 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, 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 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, HR, HU, IE, IS, IT, LT, LU, LV, MC, MT, NL, NO, 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)