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1. WO2009074789 - AMIDO-THIOPHENE COMPOUNDS AND THEIR USE AS 11-BETA-HSD1 INHIBITORS

Publication Number WO/2009/074789
Publication Date 18.06.2009
International Application No. PCT/GB2008/004068
International Filing Date 11.12.2008
IPC
C07D 333/38 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
333Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02not condensed with other rings
04not substituted on the ring sulfur atom
26with 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
38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 409/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14containing three or more hetero rings
C07D 413/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
C07D 453/02 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
453Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
02containing not further condensed quinuclidine ring systems
C07D 471/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
CPC
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 1/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
18for pancreatic disorders, e.g. pancreatic enzymes
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 25/22
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
22Anxiolytics
A61P 25/24
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
24Antidepressants
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for 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
Applicants
  • THE UNIVERSITY OF EDINBURGH [GB]/[GB] (AllExceptUS)
  • WEBSTER, Scott, Peter [GB]/[GB] (UsOnly)
  • SECKL, Jonathan, Robert [GB]/[GB] (UsOnly)
  • WALKER, Brian, Robert [GB]/[GB] (UsOnly)
  • WARD, Peter [GB]/[GB] (UsOnly)
  • PALLIN, Thomas, David [GB]/[GB] (UsOnly)
  • DYKE, Hazel, Joan [GB]/[GB] (UsOnly)
  • PERRIOR, Trevor, Robert [GB]/[GB] (UsOnly)
Inventors
  • WEBSTER, Scott, Peter
  • SECKL, Jonathan, Robert
  • WALKER, Brian, Robert
  • WARD, Peter
  • PALLIN, Thomas, David
  • DYKE, Hazel, Joan
  • PERRIOR, Trevor, Robert
Agents
  • WYTENBURG, Wilhelmus
Priority Data
0724251.412.12.2007GB
61/013,04212.12.2007US
Publication Language English (en)
Filing Language English (EN)
Designated States
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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