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US 12,570,615 B2Granted
Quinazolinone derivatives
AssigneeHoffmann-La Roche Inc.
InventorsCosimo Dolente, David Stephen Hewings, Daniel Hunziker, Daniela Krummenacher, Piergiorgio Francesco Tommaso Pettazzoni, Fabienne Ricklin, Claus Riemer, Juergen Wichmann
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Abstract
The invention relates to a compound of formula (I) Wherein A, L, R1, R2, R3 and R4 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
Claims18
A compound of formula (I)
- wherein
- A is —O— or —NH—;
- L is —(CH2)n-, with n=1, 2, 3 or 4;
- R1 is alkoxycarbonyl, alkoxycarbonylheterocycloalkyl, alkoxycarbonylamino, phenyl, alkoxycarbonyl(alkylamino), alkylcarbonyl(alkylamino), alkoxycarbonyl(alkylamino)alkylphenyl, alkoxyalkylaminocarbonyl, alkylcarbonylheterocycloalkyl, alkoxycarbonylaminoalkoxyalkoxy, phenylalkoxy, aminoalkoxyalkoxy, hydroxycarbonyl, alkoxycarbonylheterocycloalkylcarbonyl, alkoxycarbonylheterocycloalkylaminocarbonyl or alkoxycarbonyl(alkylamino)alkylaminocarbonyl;
- R2 and R3 are independently selected from the group consisting of hydrogen, fluorine and cyano;
- R4 is dialkylamino, (cycloalkyl)(alkyl)amino, haloheterocycloalkyl, heterocycloalkyl, cycloalkyl or alkyl;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, comprising one of the following steps:
- (a) the reaction of a compound of formula (A1)
- with a compound of formula (A2)
- in the presence of a base;
- (b) the reaction of a compound of formula (B1)
- with a compound of formula (B2)
- in the presence of a base, a palladium catalyst and a suitable ligand;
- or
- (c) the reaction of a compound of formula (C1)
- with a compound of formula (C2)
- in the presence of a base;
- wherein
- A is —O— or —NH—;
- L is —(CH2)n-, with n=1, 2, 3 or 4;
- R1 is alkoxycarbonyl, alkoxycarbonylheterocycloalkyl, alkoxycarbonylamino, phenyl, alkoxycarbonyl(alkylamino), alkylcarbonyl(alkylamino), alkoxycarbonyl(alkylamino)alkylphenyl, alkoxyalkylaminocarbonyl, alkylcarbonylheterocycloalkyl, alkoxycarbonylaminoalkoxyalkoxy, phenylalkoxy, aminoalkoxyalkoxy, hydroxycarbonyl, alkoxycarbonylheterocycloalkylcarbonyl, alkoxycarbonylheterocycloalkylaminocarbonyl or alkoxycarbonyl(alkylamino)alkylaminocarbonyl;
- R2 and R3 are independently selected from the group consisting of hydrogen, fluorine and cyano;
- and
- R4 is dialkylamino, (cycloalkyl)(alkyl)amino, haloheterocycloalkyl, heterocycloalkyl, cycloalkyl or alkyl.
14 more elements
Dependencies are inferred from the claim text.