Nitroxoline derivative, preparation method therefor, and use thereof
AssigneesJiangsu Yahong Meditech Co., Ltd., Asieris Pharmaceuticals (Shanghai) Co., Ltd.
InventorsLiang Wu, Yijun Deng, Lu Xiao, Ke Pan
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Abstract
The present invention discloses a nitroxoline derivative, a preparation method therefor, and use thereof. Specifically, the present discloses a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing same, and use thereof in treating infectious diseases or cancers. The compound of the present invention has excellent anti-tumor activity and antibacterial activity, and can be developed into a drug for treating tumors and infectious diseases. The definition of each group in general formula (I) is the same as that in the description.
Claims12
A compound of formula (I) or a pharmaceutically acceptable salt thereof,
- R1 is —NRaRb;
- Ra and Rb are each independently selected from the group consisting of hydrogen and C1-C6 alkyl;
- or, Ra and Rb together with the nitrogen atom to which they are attached form a 5- to 7-membered nitrogen-containing heterocyclyl, the 5- to 7-membered nitrogen-containing heterocyclyl optionally comprises one or more heteroatom(s) selected from the group consisting of N, O and S in addition to N;
- and the 5- to 7-membered nitrogen-containing heterocyclyl is optionally further substituted by one or more Qs;
- Q is halogen, oxo, C1-C6 alkyl,—C(O) Rc, —C(O)ORc,—C(O)NRcRd,—C(O)N(Rc)(CH2)qRd or —S(O)pRc;
- Rc and Rd are each independently selected from the group consisting of hydrogen and C1-C6 alkyl, wherein the C1-C6 alkyl is optionally further substituted by one or more halogens;
- or, Rc and Rd together with the nitrogen atom to which they are attached form a 5- to 7-membered nitrogen-containing heterocyclyl, the 5- to 7-membered nitrogen-containing heterocyclyl optionally comprises one or more heteroatom(s) selected from the group consisting of N, O and S in addition to N, the 5- to 7-membered nitrogen-containing heterocyclyl is optionally further substituted by one or more substituent(s) selected from the group consisting of halogen and C1-C6 alkyl;
- p is 1 or 2;
- q is an integer from 0 to 6;
- or,
- R1 is C3-C10 cycloalkyl, wherein the C3-C10 cycloalkyl is optionally further substituted by one or more substituent(s) selected from the group consisting of halogen and C1-C6 alkyl;
- or,
- R1 is selected from the group consisting of C6-C10 aryl and 5- to 10-membered heteroaryl, wherein the C6-C10 aryl and 5- to 10-membered heteroaryl are optionally further substituted by one or more substituent(s) selected from the group consisting of halogen and C1-C6 alkyl;
- R2 is hydrogen;
- R3 is hydrogen;
- R4 is hydrogen;
- R5 is hydrogen.
A compound of formula (I) or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is hydrogen;
- R2 is selected from the group consisting of hydrogen and C3-C6 cycloalkyl;
- R3 is hydrogen;
- R4 is —C(O) ORa, wherein Ra is selected from the group consisting of hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl and C3-C6 cycloalkyl-C1-C6 alkyl;
- R5 is hydrogen.
A compound is selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.