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US 2009/0156583 A1Published application
Tricyclic Amide Derivatives
AssigneeHoffmann-La Roche Inc.
InventorsMatthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
Life of this patent
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Abstract
The present invention relates to compounds of formula I wherein A, G, r and R1 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Claims23
A compound of formula I:
- wherein:
- A is C or N;
- r is 1 or 2;
- R1 is selected from the group consisting of hydrogen,
- lower alkyl,
- lower hydroxyalkyl, lower alkoxyalkyl,
- lower halogenalkyl, lower hydroxyhalogenalkyl,
- lower alkanoyl,
- lower alkylsulfonyl, lower phenylsulfonyl,
- lower cycloalkylalkyl,
- lower phenylalkyl, wherein the phenyl ring may be unsubstituted or substituted with one or two groups independently selected from lower alkyl, cyano, halogen, lower halogenalkyl, lower alkoxy and lower hydroxyalkyl,
- lower heteroarylalkyl, wherein the heteroaryl ring may be unsubstituted or substituted with one or two groups independently selected from lower alkyl, halogen, phenyl, lower alkoxy and lower hydroxyalkyl,
- lower heterocyclylalkyl, wherein the heterocyclyl ring may be unsubstituted or substituted with one or two groups independently selected from lower alkyl, halogen, phenyl, lower alkoxy and lower hydroxyalkyl, and
- —CH2—CO—NR14R15, wherein
- R14 and R15 independently from each other are selected from the group hydrogen, lower alkyl and phenyl unsubstituted or substituted with one or two groups independently selected from lower alkyl, halogen, lower halogenoalkoxy and lower hydroxyalkyl,
- or R14 and R15 together with the nitrogen atom to which they are attached form a 4-, 5-, 6- or 7-membered heterocyclic ring optionally containing a further heteroatom selected from nitrogen, oxygen or sulfur, a sulfinyl group or a sulfonyl group,
- said heterocyclic ring being unsubstituted or substituted by one, two or three groups independently selected from lower alkyl, halogen, halogenalkyl, hydroxy, lower hydroxyalkyl, lower alkoxy, oxo, phenyl, benzyl, pyridyl and carbamoyl;
- R2, R2′, R3 and R3′ independently from each other are selected from the group consisting of hydrogen, lower alkyl, lower hydroxyalkyl and lower alkoxyalkyl;
- R4 is selected from the group consisting of hydrogen and halogen;
- R5 is hydrogen or halogen;
- G is a group selected from
- wherein
- m is 0, 1 or 2;
- R6 is selected from lower alkyl, cycloalkyl, lower cycloalkylalkyl and lower phenylalkyl;
- n is 0, 1 or 2;
- R7 is lower alkyl;
- B is selected from CR13R13, O and S;
- R8, R8′, R9, R9′, R10, R10′, R13 and R13′ independently from each other are selected from the group consisting of hydrogen, lower alkyl, hydroxy, halogen and dialkylamino, or
- R9 and R13 together form a double bond;
- p is 0, 1 or 2;
- q is 0, 1 or 2;
- R11 is lower alkyl;
- R12 is lower alkyl;
- and pharmaceutically acceptable salts thereof.
31 more elements
Dependencies are inferred from the claim text.