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US 2009/0275573 A1Published application
Imidazolidinone Derivatives as 11B-HSD1 Inhibitors
AssigneeHoffmann-La Roche Inc.
InventorsJean Ackermann, Kurt Amrein, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
Life of this patent
Estimating the term…
Abstract
Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein A and R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
Claims19
A compound according to formula (I):
- wherein:
- R1 is a) bornyl, norbornyl, bicyclo[2.2.2]octanyl, or adamantyl, wherein bornyl, norbornyl, bicyclo[2.2.2]octanyl, or adamantyl are optionally substituted with one or two substituents independently selected from hydroxy, alkoxy, halogen, alkyl, hydroxyalkyl, amino, aminocarbonyl, alkoxycarbonyl, hydroxycarbonyl, alkylcarbonylamino, alkyl-S(O)2—, alkyl-S(O)2-amino, haloalkyl-S(O)2-amino, alkoxycarbonylamino-S(O)2-amino, amino-S(O)2-amino, hydroxyalkylcarbonylamino, aminocarbonylamino, haloalkoxy, and, wherein A is CR5R6 or carbonyl;
- or
- b) phenyl, phenylalkyl, substituted phenyl or substituted phenylalkyl, wherein substituted phenyl and substituted phenylalkyl are substituted with one or two substituents independently selected from alkyl, halogen, haloalkyl, alkoxy, hydroxy and haloalkoxy;
- and, wherein A is CR5R6 and none of R9, R10, R11 and R12 is hydroxy and R13 and R14 are not hydrogen at the same time;
- R2 and R3 together with the nitrogen atom N* and the carbon atom C* to which they are attached form B, C, D, E, F or G
- R4 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, arylalkyl, arylalkoxy, arylalkoxyalkyl, hydroxyalkyl, aryl, heteroarylalkyl, heteroaryloxyalkyl, substituted aryl, substituted heteroarylalkyl or substituted heteroaryloxyalkyl, wherein substituted aryl, substituted heteroarylalkyl and substituted heteroaryloxyalkyl are substituted with one to three substituents independently selected from alkyl, cycloalkyl, cyano, halogen, haloalkyl, hydroxy and alkoxy;
- R5 is hydrogen;
- R6 is hydrogen;
- one of R7 and R8 is hydrogen or halogen and the other one is hydrogen, halogen, hydroxy, alkoxy or arylalkoxy;
- one of R9 and R10 is hydrogen or halogen and the other one is hydrogen, halogen, hydroxy, alkoxy or arylalkoxy;
- one of R11 and R12 is hydrogen or halogen and the other one is hydrogen, halogen, hydroxy, alkoxy or arylalkoxy;
- one of R13 and R14 is hydrogen or halogen and the other one is hydrogen, halogen, hydroxy, alkoxy or arylalkoxy;
- or a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.