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US 2003/0158179 A1Published application
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 1 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.
Claims29
A compound of formula I
- 20
- wherein
- R1 is —O—R4 or —NR5R6;
- R1 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 hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl or 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 nitrogen, oxygen or sulfur and, wherein the heterocyclyc ring is optionally substituted with one or more substituents independently selected from alkyl or alkoxy;
- A1 is a 5- to 7-membered saturated heterocyclic ring comprising the nitrogen atom which is attached to the quinoline ring and optionally a second heteroatom which is selected from oxygen, sulfur or nitrogen and, wherein the ring is optionally substituted by one to three substituents independently selected from alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, amino, acetylamino, cyano, tetrahydropyranyloxyalkyl or cycloalkylalkoxy;
- A2 is —CH2— or —C(O)—;
- and pharmaceutically acceptable salts and esters thereof.
8 more elements
A method of treating or preventing an illness caused by disorders associated with the NPY receptor comprising administering to a patient in need of such treatment, an effective amount of a compound of the following formula I
- 25
- 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 hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl or 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 nitrogen, oxygen or sulfur and, wherein the heterocyclyc ring is optionally substituted with one or more substituents independently selected from alkyl or alkoxy;
- A1 is a 5- to 7-membered saturated heterocyclic ring comprising the nitrogen atom which is attached to the quinoline ring and optionally a second heteroatom which is selected from oxygen, sulfur or nitrogen and, wherein the ring is optionally substituted by one to three substituents independently selected from alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, amino, acetylamino, cyano, tetrahydropyranyloxyalkyl or 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
- 26
- 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 hydrogen, alkyl, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, alkoxyalkyl, hydroxyalkyl or 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 nitrogen, oxygen or sulfur and, wherein the heterocyclyc ring is optionally substituted with one or more substituents independently selected from alkyl or alkoxy;
- A1 is a 5- to 7-membered saturated heterocyclic ring comprising the nitrogen atom which is attached to the quinoline ring and optionally a second heteroatom which is selected from oxygen, sulfur or nitrogen and, wherein the ring is optionally substituted by one to three substituents independently selected from alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, amino, acetylamino, cyano, tetrahydropyranyloxyalkyl or cycloalkylalkoxy;
- A2 is —CH2— or —C(O)—;
- and pharmaceutically acceptable salts and esters thereof;
- and
- a pharmaceutically acceptable carrier.
11 more elements
Dependencies are inferred from the claim text.