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US 2020/0048242 A1Published application
Dihydropyrimidine derivatives and uses thereof in the treatment of hbv infection or of hbv-induced diseases
AssigneeJanssen Sciences Ireland Unlimited Company
InventorsGang DENG, Yimin JIANG, Qian LIU, Chao LIANG, Zhao-Kui WAN, Wing Shun CHEUNG, Zhanling CHENG, Yanping XU
Life of this patent
Estimating the term…
Abstract
The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
Claims16
A compound of formula (I)
- including the deuterated isomers, stereoisomers and the tautomeric forms thereof,
- wherein
- Y1 represents a bond or CR7R8;
- wherein
- Y2 represents a bond or CR7R8, wherein R7 and R8 are independently selected from hydrogen and C1-C4 alkyl, and A represents CH or N;
- or
- Y2 is CR9 and A is C thus forming a C═C bond, wherein R9 is hydrogen or C1-C4 alkyl;
- wherein Y3 represents CH;
- or Y1 and Y2 represent a bond, and a further —CH2— is present directly connecting A and Y3 to form a bridged 5-membered cyclic hydrocarbon;
- wherein Y4 represents OH, OR14 or R14 wherein R14 is C1-C4 alkyl;
- wherein Q represents a bond or a 5- to 6-membered aromatic ring,
- wherein said 5- to 6-membered aromatic ring optionally comprises 1-3 heteroatoms,
- wherein said 5- to 6-membered aromatic ring is optionally substituted with one or more substituents each independently selected from the group consisting of C1-C4 alkyl,
- halogen,
- OR13 wherein R13 is H or C1-C4 alkyl,
- NR10R11 where R10 and R11 are independently selected from H and C1-C4 alkyl, or R10 and R11 form a C4, C5 or C6 membered ring,
- C1-C4 alkyl substituted with one or more halogen,
- C1-C4 alkyl substituted with OR12 wherein each R12 is H or C1-C4 alkyl;
- wherein if Q represents a bond, Y4 is selected from the group consisting of
- phenyl,
- pyrazolyl,
- isoxazolyl,
- thiadiazolyl,
- phenyl substituted with C1-C4 alkyl,
- pyrazolyl substituted with C1-C4 alkyl,
- isoxazolyl substituted with C1-C4 alkyl, and
- thiadiazolyl substituted with C1-C4 alkyl;
- wherein L1 is selected from the group consisting of
- a bond,
- C1-C4 alkyl, and
- C1-C4 alkyl substituted with one or more substituents each independently selected from the group consisting of
- C1-C4 alkyl,
- halogen,
- oxo,
- OR7 wherein R7 independently is hydrogen or C1-C4 alkyl, and
- C1-C4 alkyl substituted with one or more halogen;
- wherein L2 is selected from the group consisting of
- a bond,
- C1-C4 alkyl, and
- a 3-7 membered saturated ring optionally containing one or more heteroatom(s), the heteroatom being a nitrogen
- wherein each of said C1-C4 alkyl and said 3-7 membered saturated ring are optionally substituted with one or more substituents each independently selected from the group consisting of
- C1-C4 alkyl,
- halogen,
- OR15 wherein R15 independently is hydrogen or C1-C4 alkyl, and
- C1-C4 alkyl substituted with one or more halogen;
- wherein p is an integer selected from 0 and 1;
- wherein R1 is selected from the group consisting of thiazolyl, pyridyl, thiazolyl substituted with one or more halogen and pyridyl substituted with one or more halogen;
- wherein R3 is C1-C3alkyl;
- and
- wherein R4, R5 and R6 each independently are selected from the group consisting of hydrogen, C1-C3 alkyl and halogen;
- or a pharmaceutically acceptable salt or a solvate thereof.
48 more elements
(canceled)
Dependencies are inferred from the claim text.