Quinoline derivatives
AssigneeHoffmann-La Roche Inc.
InventorsPatrizio Mattei, Werner Mueller, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
Life of this patent
Estimating the term…
Abstract
Compounds of general formula I 1 as well as pharmaceutically acceptable salts and esters thereof, are potent inhibitors of neuropeptide Y and can be used in the form of pharmaceutical preparations for the treatment or prevention of various disease states and related morbidities including obesity.
Claims22
A compound of formula
- 16
- wherein
- R1 and R2 are each independently substituted with hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkylcarbonyl, cycloalkylcarbonyl, cycloalkylalkylcarbonyl, aryl, aralkyl, arylcarbonyl, aralkylcarbonyl, alkoxyalkyl, hydroxyalkyl, heterocyclyl, heterocyclylalkyl, heterocyclylcarbonyl, heterocyclylalkylcarbonyl, carbocyclyl, carbocyclylalkyl, amino, alkyl-SO2—, aryl-SO2—, heterocyclyl-SO2— or amino-SO2—, or R1 and R2 together with the N atom to which they are attached form a 5- to 10-membered heterocyclic ring which optionally comprises a second heteroatom selected from nitrogen or oxygen and wherein the heterocyclyc ring is optionally substituted with one or more substituents independently selected from the group consisting of alkyl and alkoxy;
- R3 is hydrogen, alkyl, amino or halogen;
- R4 is hydrogen, halogen, heterocyclyl, amino or alkyl;
- A 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 A is optionally substituted by one to three substituents independently selected from the group consisting of alkyl, alkoxy, hydroxy, amino, acetylamino, cyano, hydroxyalkyl, alkoxyalkyl, cycloalkylalkoxy and cycloalkylalkoxyalkyl;
- and pharmaceutically acceptable salts and esters thereof.
The compound according to 1, wherein one of R1 and R2 is hydrogen or alkyl and the other is alkyl, cycloalkyl, cycloalkylalkyl, alkylcarbonyl, cycloalkylcarbonyl, phenyl, naphthyl, phenylalkyl, naphthylalkyl, phenylcarbonyl, alkoxyalkyl, hydroxyalkyl, thiophenyl, pyridinyl, furyl, thiophenylalkyl, pyridinylalkyl, furylalkyl, thiophenylcarbonyl, pyridinylcarbonyl, furylalkyl, indanyl, carbocyclylalkyl, amino, alkyl-SO2—, aryl-SO2—, thiophenyl-SO2—, pyridinyl-SO2—, furyl-SO2—, or amino-SO2—, and, wherein the phenyl and naphthyl groups of are optionally each independently further substituted with alkyl, cyano, halogeno, alkoxy or trifluoromethyl.
The compound according to 15, wherein one of R1 and R2 is hydrogen or methyl and the other is alkylcarbonyl, cycloalkylcarbonyl, cyanophenyl, alkoxybenyl, cyanophenylcarbonyl, fluorophenylcarbonyl, thiophenylalkyl, pyridinylcarbonyl, furylcarbonyl, alkyl-SO2—, pyridyl-SO2—, pyridinyl or cycloalkylcarbonyl.
Dependencies are inferred from the claim text.