Processing

Please wait...

Settings

Settings

Goto Application

1. WO2011033255 - (4-PHENYL-PIPERIDIN-1-YL)-[5-1H-PYRAZOL-4YL)-THIOPHEN-3-YL]-METHANONE COMPOUNDS AND THEIR USE

Publication Number WO/2011/033255
Publication Date 24.03.2011
International Application No. PCT/GB2010/001732
International Filing Date 14.09.2010
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 451/06 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 31/4439 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
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 3/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
CPC
A61P 1/00
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
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
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
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
61/242,82516.09.2009US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) (4-PHENYL-PIPERIDIN-1-YL)-[5-1H-PYRAZOL-4YL)-THIOPHEN-3-YL]-METHANONE COMPOUNDS AND THEIR USE
(FR) COMPOSÉS DE (4-PHÉNYL-PIPÉRIDIN-1-YL)-[5-1H-PYRAZOL-4-YL)-THIOPHÉN-3-YL]-MÉTHANONE ET LEUR UTILISATION
Abstract
(EN) The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)- [5-(1 H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds 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 1 1 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 d'une façon générale le domaine des composés thérapeutiques. De façon plus spécifique, la présente invention porte sur certains composés de (4-phényl-pipéridin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophén-3-yl]-méthanone qui, entre autres, inhibent la 11β-hydroxystéroïde déshydrogénase de type 1 (11β-HSD1). La présente invention porte également sur des compositions pharmaceutiques comprenant de tels composés et sur l'utilisation de tels composés et de telles compositions, aussi bien in vitro qu'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 comprend des troubles tels que le diabète de type 2 et l'obésité, et les troubles associés dont l'insulinorésistance, l'hypertension, les troubles lipidiques et les troubles cardiovasculaires tels qu'une cardiopathie (coronaire) ischémique ; pour traiter des troubles du SNC tels qu'une déficience cognitive légère et une démence précoce, dont la maladie d'Alzheimer ; etc.
Latest bibliographic data on file with the International Bureau