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1. WO2011135276 - 3, 3 -DISUBSTITUTED- ( 8 - AZA - BICYCLO [3.2.1] OCT- 8 - YL) -[5- (1H - PYRAZOL - 4 -YL) -THIOPHEN-3 -YL] METHANONES AS INHIBITORS OF 11 (BETA) -HSD1

Publication Number WO/2011/135276
Publication Date 03.11.2011
International Application No. PCT/GB2011/000345
International Filing Date 10.03.2011
IPC
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 451/02 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
451Heterocyclic compounds containing 8-azabicyclo octane, 9-azabicyclo nonane, or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
02containing not further condensed 8-azabicyclo octane or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane; Cyclic acetals thereof
C07D 451/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
451Heterocyclic compounds containing 8-azabicyclo octane, 9-azabicyclo nonane, or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
02containing not further condensed 8-azabicyclo octane or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane; Cyclic acetals thereof
04with hetero atoms directly attached in position 3 of the 8-azabicyclo octane or in position 7 of the 3-oxa-9-azatricyclo nonane ring system
C07D 451/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
451Heterocyclic compounds containing 8-azabicyclo octane, 9-azabicyclo nonane, or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
02containing not further condensed 8-azabicyclo octane or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane; Cyclic acetals thereof
04with hetero atoms directly attached in position 3 of the 8-azabicyclo octane or in position 7 of the 3-oxa-9-azatricyclo nonane ring system
06Oxygen atoms
A61K 31/4535 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4535containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 31/46 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
468-Azabicyclo octane; Derivatives thereof, e.g. atropine, cocaine
CPC
A61K 31/4155
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4151,2-Diazoles
4155non condensed and containing further heterocyclic rings
A61K 31/4427
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
A61P 1/04
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
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
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, J.
Priority Data
61/329,45329.04.2010US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) 3, 3 -DISUBSTITUTED- ( 8 - AZA - BICYCLO [3.2.1] OCT- 8 - YL) -[5- (1H - PYRAZOL - 4 -YL) -THIOPHEN-3 -YL] METHANONES AS INHIBITORS OF 11 (BETA) -HSD1
(FR) (8-AZA-BICYCLO[3.2.1]OCT-8-YL)-[5-(1H-PYRAZOL-4-YL]-MÉTHANONES 3,3-DISUBSTITUÉES 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 3,3-disubstituted-(8-aza- bicyclo [3.2.1]oct-8-yl)[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted- (6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4, 4-disubstituted piperidin-1 -yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula (I) that, inter alia, inhibit 11 β-hydroxysteroid dehydrogenase type 1 (11 β-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 11 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-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.
(FR) La présente invention concerne généralement le domaine de composés thérapeutiques. Plus spécifiquement, la présente invention concerne certains composés (8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophén-3-yl]-méthanone 3,3-disubstituée, (6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophén-3-yl]-méthanone 3,3-disubstituée, et (pipéridin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophén-3-yl]-méthanone 4,4-disubstituée de la formule (I) suivante qui, entre autres, inhibent la 11β-hydroxystéroïde déshydrogénase de type 1 (11β-HSD1). La présente invention concerne en outre des compositions pharmaceutiques comprenant de tels composés, et l'utilisation de tels composés et compositions, 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 11β-hydroxystéroïde déshydrogénase de type 1; pour traiter le syndrome métabolique, qui comprend des troubles tels que le diabète de type 2 et l'obésité, et des troubles associés comprenant l'insulinorésistance, l'hypertension, les troubles lipidiques et les troubles cardiovasculaires tels qu'une cardiopathie ischémique (coronarienne); pour traiter des troubles du SNC tels qu'un trouble cognitif léger et la démence précoce, comprenant la maladie d'Alzheimer; etc.
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