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US 10,093,671 B2Granted
2-oxo-6,7-dihydrobenzo[a]quinolizine-3-carboxylic acid derivatives for the treatment and prophylaxis of hepatitis B virus infection
AssigneeHoffmann-La Roche Inc.
InventorsXingchun Han, Min Jiang, Song Yang
Life of this patent
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Abstract
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5 and Ar are as described herein, compositions including the compounds and methods of using the compounds.
Claims17
A compound of formula I
- wherein
- R1, R2, R3 and R4 are independently selected from C1-6alkyl, haloC1-6alkyl, hydrogen, halogen, cyano, amino, C1-6alkylamino, diC1-6alkylamino, pyrrolidinyl and OR6;
- R5 is hydrogen or C1-6alkyl;
- R6 is hydrogen;
- C1-6alkyl;
- haloC1-6alkyl;
- C3-7cycloalkylC1-6alkyl;
- phenylC1-6alkyl;
- hydroxyC1-6alkyl;
- C1-6alkoxyC1-6alkyl;
- carboxyC1-6alkyl;
- C1-6alkylsulfanylC1-6alkyl;
- C1-6alkylsulfonylC1-6alkyl;
- cyanoC1-6alkyl;
- aminoC1-6alkyl;
- C1-6alkylaminoC1-6alkyl;
- diC1-6alkylaminoC1-6alkyl;
- C1-6alkylcarbonylaminoC1-6alkyl;
- C1-6alkylsulfonylaminoC1-6alkyl;
- C1-6alkoxycarbonylaminoC1-6alkyl;
- pyrazolylC1-6alkyl;
- triazolylC1-6alkyl;
- or heterocycloalkylC1-6alkyl, wherein heterocycloalkyl is N-containing monocyclic heterocycloalkyl;
- and
- Ar is phenyl;
- phenyl substituted by one, two or three groups independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halogen and phenylC1-6alkoxy;
- thienyl;
- thienyl substituted by one, two or three groups independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halogen and phenylC1-6alkoxy;
- benzothiophenyl;
- benzothiophenyl substituted by one, two or three groups independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halogen and phenylC1-6alkoxy;
- pyridinyl;
- pyridinyl substituted by one, two or three groups independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halogen and phenylC1-6alkoxy;
- pyrimidinyl;
- pyrimidinyl substituted by one, two or three groups independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halogen and phenylC1-6alkoxy;
- pyrrolyl;
- pyrrolyl substituted by one, two or three groups independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halogen and phenylC1-6alkoxy;
- pyrazolyl;
- pyrazolyl substituted by one, two or three groups independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halogen and phenylC1-6alkoxy;
- thiazolyl;
- or thiazolyl substituted by one, two or three groups independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halogen and phenylC1-6alkoxy;
- or a pharmaceutically acceptable salt or enantiomer thereof.
38 more elements
Dependencies are inferred from the claim text.