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US 2019/0241559 A1Published application
Novel tetrahydropyridopyrimidines for the treatment and prophylaxis of hbv infection
AssigneeHoffmann-La Roche Inc.
InventorsZhanling Cheng, Xingchun Han, Min Jiang, Jianhua Wang, Yongguang Wang, Song Yang
Life of this patent
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Abstract
The present invention provides novel compounds having the general formula: wherein R1 to R4, A, W, Q and Y are as described herein, compositions including the compounds and methods of using the compounds.
Claims36
A compound of formula I,
- wherein:
- R1 is aminoC1-6alkyl, aminocarbonylC1-6alkyl, C1-6alkyl, C3-7cycloalkyl, carboxyC1-6alkyl, cyanoC1-6alkyl, haloC1-6alkyl, hydrogen or hydroxyC1-6alkyl;
- R2 is C1-6alkoxy, C1-6alkyl, haloC1-6alkoxy, haloC1-6alkyl, halogen or hydrogen;
- one of R3 and R4 is C3-7cycloalkylC1-6alkyl, C1-6alkyl or hydrogen;
- and the other one is 1,1-dioxothianyl, aminocarbonylC1-6alkyl, azetidinyl, C1-6alkylcarbonyl, C1-6alkylcarbonylazetidinyl, C1-6alkyl sufonylpiperidinyl, C1-6alkylsufonyl, C3-7cycloalkylcarbonyl, C3-7cycloalkylsulfonyl, carboxyC1-6alkyl, haloC1-6alkyl, hydroxyC1-6alkylcarbonyl, phenylcarbonyl, phenylsulfonyl or tetrahydropyranyl;
- or
- R3 and R4 together with the nitrogen to which they are attached form 1,1-dioxo-thiazolidinyl;
- 1,1-dioxo-thiazinanyl;
- 2-oxa-6-azaspiro[3.3]heptanyl;
- 2-oxa-7-azaspiro[4.4]nonanyl;
- 3-oxa-8-azabicyclo[3.2.1]octanyl;
- 6-oxo-2-oxa-7-azaspiro[3.4]octanyl;
- azetidinyl;
- oxoimidazolidinyl;
- oxopyrrolidinyl;
- substituted azetidinyl;
- substituted morpholinyl;
- substituted oxooxazolidinyl;
- substituted oxopiperazinyl;
- substituted oxopyrrolidinyl;
- substituted piperazinyl;
- substituted piperidinyl or substituted pyrrolidinyl;
- wherein said substituted azetidinyl, substituted morpholinyl, substituted oxooxazolidinyl, substituted oxopiperazinyl, substituted oxopyrrolidinyl, substituted piperazinyl, substituted piperidinyl and substituted pyrrolidinyl are substituted with one, two or three substituents independently selected from aminocarbonyl, aminocarbonylC1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkoxyC1-6alkylsulfonyl, C1-6alkyl, C1-6alkylcarbonyl, C1-6alkylcarbonyl amino, C1-6alkylsulfonyl, C1-6alkyl sulfonylamino, C1-6alkylsulfonylaminocarbonyl, carboxy, carboxyC1-6alkyl, cyano, halogen, hydroxy and hydroxyC1-6alkyl;
- A is N or CH;
- and
- one of W, Q and Y is N, and the others are CH;
- with the proviso that N-[2-fluoro-6-(5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl)-4-pyridyl]methanesulfonamide and N-[4-fluoro-6-(5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl)-2-pyridyl]methanesulfonamide are excluded;
- or a pharmaceutically acceptable salt, or enantiomer, or diastereomer thereof.
25 more elements
(canceled)
-37. (canceled)
(canceled)
Dependencies are inferred from the claim text.