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US 2006/0040937 A1Published application
N-aroyl cyclic amines as orexin receptor antagonists
AssigneeGlaxo Group Limited
InventorsClive Branch, Steven Coulton, Amanda Johns, David Nash, Roderick Porter, Geoffrey Stemp
Life of this patent
Estimating the term…
Abstract
This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals.
Claims11
A compound of formula (I):
- wherein:
- X is O, CR7R8, NH or bond;
- R1 and R2 are both hydrogen, both optionally substituted (C1-4)alkyl, or are together with the carbon to which they are attached form a (C3-6)cycloalkyl ring or a 4- to 6-membered heterocyclyl ring.
- R3 and R4 are both hydrogen, both optionally substituted (C1-4)alkyl, or are together with the carbon to which they are attached form a (C3-6)cycloalkyl ring or a 4- to 6-membered heterocyclyl ring;
- R7 and R8 are both hydrogen, both optionally substituted (C1-4)alkyl, or are together with the carbon to which they are attached form a (C3-6)cycloalkyl ring or a 4- to 6-membered heterocyclyl ring;
- provided that one pair of R1 and R2, R3 and R4, R7 and R8 are both optionally substituted (C1-4)alkyl, or are together with the carbon to which they are attached form a (C3-6)cycloalkyl ring or a 4- to 6-membered heterocyclyl ring and the remaining groups are hydrogen;
- R5 is hydrogen, optionally substituted (C1-4) alkyl, or optionally substituted (C1-4)alkylCO;
- Ar1 is an optionally substituted aryl, an optionally substituted mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S;
- Ar2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R6 and further optional substituents;
- or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 4 heteroatoms selected from N, O and S;
- R6 represents hydrogen, optionally substituted(C1-4 )alkoxy, halo, cyano, optionally substituted(C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S;
- or a pharmaceutically acceptable salt thereof.
9 more elements
A compound of formula (I) as defined in any one of Examples 1 to 44, or a pharmaceutically acceptable salt of any one thereof.
Dependencies are inferred from the claim text.