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US 7,064,134 B2Granted
Quinoline derivatives
AssigneeHoffmann-La Roche Inc.
InventorsMichael G. Klug, Patrizio Mattei, Werner Mueller, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger, Jean-Marc Plancher
Life of this patent
Estimating the term…
Abstract
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
Claims20
A compound of formula I
- wherein
- R1 is —O—R4 or —NR5R6;
- R2 is hydrogen, alkyl, cycloalkyl, alkoxy, halogen, heterocyclyl or amino;
- R3 is hydrogen, alkyl, amino or halogen;
- R4 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl or heterocyclyl;
- R5 and R6 are independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl and heterocyclyl;
- or R5 and R6 together with the N atom to which they are attached form a 5- to 10-membered heterocyclic ring optionally containing a second heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, wherein the heterocyclyc ring is optionally substituted with one or more substituents independently selected from the group consisting of alkyl and alkoxy;
- A1 is a piperidine ring optionally substituted by one to three substituents independently selected from the group consisting of alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, amino, acetylamino, cyano, tetrahydropyranyloxyalkyl and cycloalkylalkoxy;
- A2 is —CH2— or —C(O)—;
- and pharmaceutically acceptable salts and esters thereof.
7 more elements
4-(2-methyl-4-piperidin-1-yl-quinolin-7-ylmethoxy)-benzonitrile.
A method of treating eating disorders or obesity comprising administering to a patient in need of such treatment, an effective amount of a compound of the following formula I
- wherein
- R1 is —O—R4 or —NR5R6;
- R2 is hydrogen, alkyl, cycloalkyl, alkoxy, halogen, heterocyclyl or amino;
- R3 is hydrogen, alkyl, amino or halogen;
- R4 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl or heterocyclyl;
- R5 and R6 are independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl and heterocyclyl;
- or R5 and R6 together with the N atom to which they are attached form a 5- to 10-membered heterocyclic ring optionally comprising a second heteroatom selected from the group consisting of nitrogen, oxygen and sulfur;
- and wherein the heterocyclyc ring is optionally substituted with one or more substituents independently selected from the group consisting of alkyl and alkoxy;
- A1 is a piperidine ring optionally substituted by one to three substituents independently selected from the group consisting of alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, amino, acetylamino, cyano, tetrahydropyranyloxyalkyl and cycloalkylalkoxy;
- A2 is —CH2— or —C(O)—;
- and pharmaceutically acceptable salts and esters thereof.
8 more elements
A pharmaceutical composition comprising:
- a pharmaceutically effective amount of a compound of the following formula I or pharmaceutically acceptable salts and esters thereof wherein formula I is:
- wherein
- R1 is —O—R4 or —NR5R6;
- R2 is hydrogen, alkyl, cycloalkyl, alkoxy, halogen, heterocyclyl or amino;
- R3 is hydrogen, alkyl, amino or halogen;
- R4 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl or heterocyclyl;
- R5 and R6 are independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl and heterocyclyl;
- or R5 and R6 together with the N atom to which they are attached form a 5- to 10-membered heterocyclic ring optionally containing a second heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, wherein the heterocyclyc ring is optionally substituted with one or more substituents independently selected from the group consisting of alkyl and alkoxy;
- A1 is a piperidine ring optionally substituted by one to three substituents independently selected from the group consisting of alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, amino, acetylamino, cyano, tetrahydropyranyloxyalkyl and cycloalkylalkoxy;
- A2 is —CH2— or —C(O)—;
- and
- a pharmaceutically acceptable carrier.
9 more elements
Dependencies are inferred from the claim text.