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US 2014/0194436 A1Published application
Heteroarylmethyl amides
AssigneeHoffmann-La Roche Inc.
InventorsPaul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
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Abstract
The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
Claims11
A compound of formula I,
- wherein:
- A1 is N;
- A2 and A3 are CH;
- R1 is selected from the group consisting of:
- lower alkyl,
- cycloalkyl,
- lower cycloalkylalkyl,
- lower hydroxyalkyl,
- lower alkoxyalkyl,
- lower halogenalkyl,
- lower carbamoylalkyl,
- lower alkylcarbonylaminoalkyl,
- lower phenylalkyl,
- lower heterocyclylalkyl wherein the heterocyclyl group is unsubstituted or substituted by oxo,
- lower heteroarylalkyl wherein the heteroaryl group is unsubstituted or mono- or di-substituted by lower alkyl, and
- phenyl which is unsubstituted or mono- or di-substituted by halogen;
- R2 and R6 independently from each other are hydrogen or halogen;
- R3 and R5 independently from each other are selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, halogen, lower halogenalkyl, lower halogenalkoxy and cyano;
- R4 is selected from the group consisting of hydrogen, lower alkoxy, halogen, lower halogenalkyl, lower halogenalkoxy and cyano;
- or R4 and R5 together with the C atoms they are attached to form a five- or six-membered carbocycle or a five- or six-membered heterocycle containing one, two or three heteroatoms selected from the group consisting of N, O and S, said carbocycle or heterocycle being unsubstituted or substituted by one or two substituents independently selected from the group consisting of lower alkyl, lower alkoxy, halogen, lower halogenalkyl, lower halogenalkoxy and cyano;
- R7 and R7′ independently from each other are hydrogen or lower alkyl;
- and
- R8 is a five- or six-membered heteroaryl group containing one, two or three heteroatoms selected from the group consisting of N, O and S, said heteroaryl group being unsubstituted or substituted by one or two substituents independently selected from the group consisting of lower alkyl, lower alkoxy, halogen, lower halogenalkyl and cycloalkyl;
- or a pharmaceutically acceptable salt thereof.
21 more elements
Dependencies are inferred from the claim text.