Back to results
US 7,745,479 B2Granted
1,5-substituted indol-2-yl amide derivatives
AssigneeHoffmann-La Roche Inc.
InventorsMatthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Valerie Runtz-Schmitt, Sven Taylor
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds of formula I wherein R1 to R4 and G 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.
Claims22
A compound of formula I,
- wherein:
- R1 is selected from the group consisting of
- lower alkyl, lower alkenyl, lower alkynyl,
- cycloalkyl, lower cycloalkylalkyl,
- lower hydroxyalkyl,
- lower alkoxyalkyl,
- lower alkylsulfanylalkyl,
- lower dialkylaminoalkyl,
- lower dialkylcarbamoylalkyl,
- phenyl unsubstituted or substituted with one or two groups independently selected from lower alkyl, lower halogenoalkoxy and lower hydroxyalkyl,
- lower phenylalkyl wherein the phenyl ring may be unsubstituted or substituted with one or two groups independently selected from lower alkyl, halogen, 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, lower alkoxy and lower hydroxyalkyl and
- lower heterocyclylalkyl wherein the heterocyclyl ring may be unsubstituted or substituted with one or two lower alkyl groups;
- R2 is selected from the group consisting of hydrogen,
- lower alkyl, lower alkenyl, lower alkynyl,
- cycloalkyl, lower cycloalkylalkyl,
- lower hydroxyalkyl, lower alkoxyalkyl,
- lower alkylsulfanylalkyl,
- lower dialkylaminoalkyl,
- lower dialkylcarbamoylalkyl,
- phenyl unsubstituted or substituted with one or two groups independently selected from lower alkyl, lower halogenoalkoxy and lower hydroxyalkyl,
- lower phenylalkyl wherein the phenyl ring may be unsubstituted or substituted with one or two groups independently selected from lower alkyl, halogen, 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, lower alkoxy and lower hydroxyalkyl and
- lower heterocyclylalkyl wherein the heterocyclyl ring may be 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 or partly unsaturated heterocyclic ring
- being unsubstituted or substituted by one, two or three groups independently selected from lower alkyl, halogen, halogenoalkyl, hydroxy, lower hydroxyalkyl, lower alkoxy, oxo, phenyl, benzyl, pyridyl and carbamoyl, 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;
- R3 is selected from the group consisting of lower hydroxyalkyl,
- lower cyanoalkyl, lower alkoxycarbonyl,
- phenylsulfonyl wherein the phenyl ring may be unsubstituted or substituted with one or two groups independently selected from lower alkyl, halogen, cyano, lower halogenoalkyl, lower alkoxy, lower halogenoalkoxy and lower hydroxyalkyl;
- phenyl unsubstituted or substituted with one or two groups independently selected from lower alkyl, halogen, lower halogenoalkyl, cyano, lower alkoxy, lower halogenoalkoxy and lower hydroxyalkyl;
- lower phenylalkyl, wherein the phenyl ring may be unsubstituted or substituted with one or two groups independently selected from lower alkyl, halogen, lower halogenoalkyl, cyano, lower alkoxy, lower halogenoalkoxy and lower hydroxyalkyl;
- and
- heteroaryl unsubstituted or substituted with one or two groups independently selected from lower alkyl, lower alkoxy, halogen, lower halogenoalkyl, lower halogenoalkoxy, morpholino and cyano;
- R4 is hydrogen or halogen;
- G is a group selected from
- wherein
- m is 0, 1 or 2;
- R5 is selected from lower alkyl, lower halogenoalkyl, cycloalkyl, halogenocycloalkyl, lower cycloalkylalkyl and lower phenylalkyl;
- n is 0, 1 or 2;
- R6 is lower alkyl;
- p is 0, 1 or 2;
- q is 0, 1 or 2;
- A is selected from CR12R12′, O and S;
- R7, R7′, R8, R8′, R9, R9′, R12 and R12′ independently from each other are selected from the group consisting of hydrogen, lower alkyl, hydoxy, halogen and dialkylamino, or
- R8 and R12 together form a double bond;
- R10 is lower alkyl;
- R11 is C3-C6-alkyl;
- and pharmaceutically acceptable salts thereof.
48 more elements
Dependencies are inferred from the claim text.