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US 7,608,617 B2Granted
Naphthaline derivatives as H3 inverse agonists
AssigneeHoffmann-La Roche Inc.
InventorsSilvia Gatti McArthur, Cornelia Hertel, Matthias Heinrich Nettekoven, Jean-Marc Plancher, Susanne Raab, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Franz Schuler
Life of this patent
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Abstract
The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Claims27
A compound of the formula I:
- wherein:
- R1 is selected from the group consisting of hydrogen,
- lower alkyl,
- phenyl unsubstituted or substituted with one or two groups independently selected from the group consisting of lower alkyl, lower halogenalkoxy and lower hydroxyalkyl,
- lower phenylalkyl, wherein the phenyl ring is unsubstituted or substituted with one or two groups independently selected from the group consisting of lower alkyl, halogen, lower alkoxy and lower hydroxyalkyl, and
- lower alkoxyalkyl;
- R2 is selected from the group consisting of hydrogen,
- lower alkyl,
- cycloalkyl,
- lower cycloalkylalkyl,
- lower hydroxyalkyl,
- lower alkoxyalkyl,
- lower alkylsulfanylalkyl,
- lower dialkylaminoalkyl,
- phenyl unsubstituted or substituted with one or two groups independently selected from the group consisting of lower alkyl, halogen, lower alkoxy and lower hydroxyalkyl,
- lower phenylalkyl, wherein the phenyl ring is unsubstituted or substituted with one or two groups independently selected from the group consisting of lower alkyl, halogen, lower alkoxy and lower hydroxyalkyl,
- pyrrolidinyl unsubstituted or substituted with a group selected lower alkyl or halogen,
- lower heteroarylalkyl, wherein the heteroaryl ring is unsubstituted or substituted with one or two lower alkyl groups, and
- lower heterocyclylalkyl, wherein the heterocyclyl ring is unsubstituted or substituted with one or two lower alkyl groups;
- or
- R1 and R2 together with the nitrogen atom to which they are attached form a 4-, 5-, 6- or 7-membered saturated or partly unsaturated heterocyclic ring optionally containing a further heteroatom selected from nitrogen, oxygen or sulfur,
- said saturated heterocyclic ring
- being unsubstituted or substituted by one, two or three groups independently selected from the group consisting of lower alkyl, halogen, halogenalkyl, hydroxy, lower hydroxyalkyl, lower alkoxy, oxo, phenyl, benzyl, pyridyl, dialkylamino, carbamoyl, lower alkylsulfonyl, and lower halogenalkylcarbonylamino, or
- being condensed with a phenyl ring, said phenyl ring being unsubstituted or substituted by one, two or three groups independently selected from lower alkyl, lower alkoxy and halogen;
- A is
- wherein:
- m is 0, 1 or 2;
- n is 0, 1 or 2;
- R3 is hydrogen or lower alkyl;
- R9 and R10 are independently from each other selected from hydrogen or lower alkyl;
- t is 1 or 2;
- R4 is hydrogen or lower alkyl;
- X is O, S or N—R8;
- with R8 being hydrogen or lower alkyl;
- p is 0, 1 or 2;
- R5 is lower alkyl or cycloalkyl;
- q is 0, 1 or 2;
- R6 is lower alkyl;
- s is 0, 1 or 2;
- R7 is lower alkyl;
- and pharmaceutically acceptable salts thereof,
- wherein if A is A1, then R1 and R2 together with the nitrogen atom to which they are attached do not form a 4-, 5-, 6-, or 7-membered saturated or partly unsaturated heterocyclic ring.
39 more elements
Dependencies are inferred from the claim text.