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US 12,570,597 B2Granted
Polyaryl carboxylic fullerene derivative and use thereof in anti-coronavirus infection
AssigneesXiamen University, Xiamen Funano New Material Technology Co., Ltd.
InventorsSuyuan Xie, Changfeng Zhu, Qianyan Zhang, Lansun Zheng, Piaoyang Xu, Tongzong Yang, Linlong Deng, Yuanzhi Tan, Sheng Zhu
Life of this patent
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Abstract
A polyaryl carboxylic fullerene derivative and its use in anti-coronavirus infection are disclosed. Specifically, a compound shown in formula A: fullerene-RR1R2R3R4R5 formula A, or a stereoisomer, prodrug, pharmaceutically acceptable salt, or pharmaceutically acceptable solvate of the compound is provided. The compound or a derivative thereof has promising application prospects in anti-coronavirus infection.
Claims20
A compound of a general formula shown in formula A:
- fullerene-RR1R2R3R4R5 formula A
- or a stereoisomer, prodrug, pharmaceutically acceptable salt, or pharmaceutically acceptable solvate of the compound,
- wherein
- fullerene in the formula A is a cage-like all-carbon structure comprising a five-membered carbon ring, a six-membered carbon ring, and/or a seven-membered carbon ring and/or a four-membered carbon ring, or the fullerene is a metal or cluster-embedded structure;
- the fullerene is selected from the group consisting of C60, C70, C84, C90, and C100;
- wherein
- R is selected from the group consisting of the following:
- (1) H, F, Cl, Br, I, C1-C6 alkyl, and C1-C6 alkoxy;
- (2)
- wherein Y1, Y2, Y3, Y4, and Y5 are not all H and each are independently selected from the group consisting of the following:
- 1) H, and
- 2)
- wherein
- X1, X2, X3, X4, and X5 each are independently selected from the group consisting of H and C1-C6 alkyl substituted with 1, 2, or 3 carboxyl groups, and X1, X2, X3, X4, and X5 are not all H;
- and
- (3)
- wherein
- Z1, Z2, Z3, Z4, and Z5 each are independently selected from the group consisting of H and C1-C6 alkyl substituted with 1, 2, or 3 carboxyl groups, and Z1, Z2, Z3, Z4, and Z5 are not all H;
- R1, R2, R3, R4, and R5 each are independently selected from the group consisting of the following:
- (1),
- wherein
- Z1, Z2, Z3, Z4, and Z5 each are independently selected from the group consisting of H and C1-C6 alkyl substituted with 1, 2, or 3 carboxyl groups, and Z1, Z2, Z3, Z4, and Z5 are not all H;
- and
- (2)
- wherein Y1, Y2, Y3, Y4, and Y5 are not all H and each are independently selected from the group consisting of the following:
- 1) H, and
- 2)
- wherein
- X1, X2, X3, X4, and X5 each are independently selected from the group consisting of H and C1-C6 alkyl substituted with 1, 2, or 3 carboxyl groups, and X1, X2, X3, X4, and X5 are not all H;
- the compound shown in formula A does not comprise the following compounds:
27 more elements
A method of
- preventing and/or treating a disease caused by a coronavirus infection comprising a step of administering a compound shown in formula A or a stereoisomer, prodrug, pharmaceutically acceptable salt, or pharmaceutically acceptable solvate of the compound to a subject in need, wherein the disease is a respiratory disease comprising a simple infection, pneumonia, an acute or severe acute respiratory infection, hypoxemic respiratory failure (HRF) and acute respiratory distress syndrome (ARDS), sepsis, and septic shock, pneumonia, the pneumonia is pneumonia COVID-2019, the simple infection comprises fever, cough, and sore throat;
- or
- the drug is provided to serve as an inhibitor for a coronavirus;
- or
- the drug is provided to inhibit a replication or a reproduction of a coronavirus in a cell,
- fullerene-RR1R2R3R4R5 formula A
- wherein
- fullerene in the formula A is a cage-like all-carbon structure comprising a five-membered carbon ring, a six-membered carbon ring, and/or a seven-membered carbon ring and/or a four-membered carbon ring, or the fullerene is a metal or cluster-embedded structure;
- the fullerene is selected from the group consisting of C60, C70, C84, C90, and C100;
- wherein
- R is selected from the group consisting of the following:
- (1) H, F, Cl, Br, I, C1-C6 alkyl, and C1-C6 alkoxy;
- (2)
- wherein Y1, Y2, Y3, Y4, and Y5 are not all H and each are independently selected from the group consisting of the following:
- 1) H, and
- 2)
- wherein
- X1, X2, X3, X4, and X5 each are independently selected from the group consisting of H and C1-C6 alkyl substituted with 1, 2, or 3 carboxyl groups, and X1, X2, X3, X4, and X5 are not all H;
- and
- (3)
- wherein
- Z1, Z2, Z3, Z4, and Z5 each are independently selected from the group consisting of H and C1-C6 alkyl substituted with 1, 2, or 3 carboxyl groups, and Z1, Z2, Z3, Z4, and Z5 are not all H;
- R1, R2, R3, R4, and R5 each are independently selected from the group consisting of the following:
- (1)
- wherein
- Z1, Z2, Z3, Z4, and Z5 each are independently selected from the group consisting of H and C1-C6 alkyl substituted with 1, 2, or 3 carboxyl groups, and Z1, Z2, Z3, Z4, and Z5 are not all H;
- and
- (2)
- wherein Y1, Y2, Y3, Y4, and Y5 are not all H and each are independently selected from the group consisting of the following:
- 1) H, and
- 2)
- wherein
- X1, X2, X3, X4, and X5 each are independently selected from the group consisting of H and C1-C6 alkyl substituted with 1, 2, or 3 carboxyl groups, and X1, X2, X3, X4, and X5 are not all H.
30 more elements
Dependencies are inferred from the claim text.