Pyrimidinone-containing compound, preparation method thereof, pharmaceutical composition and application thereof
AssigneesYunnan University, Kunming Institute of Zoology, Chinese Academy of Sciences
InventorsYanping He, Hongbin Zhang, Yongtang Zheng, Yumeng Wu, Chengrun Tang, Ruomei Rui, Liumeng Yang, Jiangyuan Wang
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Abstract
Disclosed is a pyrimidinone-containing compound represented by formula I, a preparation method thereof, a pharmaceutical composition, and an application thereof. The pyrimidinone-containing compound of the present disclosure can be used as HIV-1 inhibitor and can be also used in the treatment of human immunodeficiency virus infection.
Claims20
A compound selected from the group consisting of a compound represented by formula I, or a N-oxide, tautomer, optical isomer, hydrate, solvate, or pharmaceutically acceptable salt thereof:
- wherein:
- A is S, O, NH or NCH3;
- R1 is H, C1-C6 branched or straight chain alkyl, or C3-C6 cycloalkyl;
- R2 is H or halogen;
- R3 is H, C1-C12 branched or straight chain alkyl, C3-C6 cycloalkyl, C6-C20 aryl, C2-C10 heteroaryl, C6-C20 aryl substituted by one or more R3a, or C2-C10 heteroaryl substituted by one or more R3b;
- wherein each of R3a and R3b is independently selected from hydroxyl, nitro, halogen, amino, cyano, HOS(═O)2—, CH3S(═O)2—, C1-C6 branched or straight chain alkyl-S(═O)2NH—, C1-C6 branched or straight chain alkyl, C1-C6 branched or straight chain alkoxy, C1-C6 branched or straight chain alkylthio, C1-C6 branched or straight chain haloalkyl, when R3a or R3b is present more than once, then each R3a or each R3b is the same or different;
- α ring is cyclohexyl or phenyl, wherein the phenyl is substituted by n R4 where each R4 is the same or different, n is 0, 1, 2, 3 or 4;
- R4 is halogen, hydroxyl, cyano, nitro, amino, C1-C6 branched or straight chain alkyl, or C1-C6 branched or straight chain alkoxy.
Dependencies are inferred from the claim text.