Urea compound and preparation method and application thereof
AssigneeShenzhen Chipscreen Biosciences Co., Ltd.
InventorsQianjiao YANG, Xianping LU, Zhibin LI, Lijun XIN, Yonglian SONG, Chao FU
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Abstract
The present invention relates to a urea compound and a preparation method and an application thereof. The structure of the present compound is represented by formula (I), the definition of each variable in the formula being as described in the description. The compound can block interaction between the PD-1/PD-L1 signalling pathways. The compound of the present invention can be used for treating or preventing diseases related to the signalling pathways, such as cancer, autoimmune disease, chronic infectious disease, and other diseases.
Claims27
A compound of Formula I,
- or a prodrug, a stereoisomer, and a pharmaceutically acceptable salt or a hydrate thereof;
- wherein,
- R1 is one or more substituents independently selected from the group consisting of H, C1-C4 alkyl, CN, halogen, NH2, COOH, C1-C4 alkylamino, C1-C4 alkyloxy, C1-C4 haloalkyl and Ar1, which substituents are the same or different;
- wherein,
- Ar1 is selected from the group consisting of
- wherein,
- R4 is one or more substituents independently selected from the group consisting of H, C1-C4 alkyl, CN, halogen, NH2, COOH, C1-C4 alkylamino, C1-C4 alkyloxy and C1-C4 haloalkyl, which substituents are the same or different;
- i is an integer from 1 to 5;
- Z is selected from the group consisting of C, NH, O, C(O), S, S(O) and S(O)2;
- R2 is selected from the group consisting of H, C1-C4 alkyl, —CH2—(CH2)k—CN and —(CH2)k—Ar2;
- wherein,
- k is an integer from 0 to 6;
- Ar2 is selected from
- wherein,
- R5 is one or more substituents independently selected from the group consisting of H, C1-C4 alkyl, CN, halogen, NH2, COOH, C1-C4 alkylamino, C1-C4 alkyloxy and C1-C4 haloalkyl, which substituents are the same or different;
- v is an integer from 1 to 5;
- R3 is one or more substituents independently selected from the group consisting of H, C1-C4 alkyl, CN, halogen, C1-C4 alkyloxy and C1-C4 haloalkyl, which substituents are the same or different;
- X is selected from C and N;
- Y is selected from NH, O, S, S(O) and S(O)2;
- A is selected from the group consisting of
- or A is a side chain of an amino acid selected from the group consisting of Gly, Ala, Ser, Lys, Arg, Thr, Asn, Gln, Phe or Glu, for example
- or A is a side chain of an amino acid selected from the group consisting of Gly, Ala, Ser, Lys, Arg, Thr, Asn, Gln, Phe and Glu, which is substituted with R6, for example,
- wherein,
- R6 is one or more substituents independently selected from the group consisting of H, C1-C4 alkyl, C1-C4 alkylcarbonyl, C1-C4 alkenylcarbonyl and C1-C4 alkylamino C1-C4 alkyl C1-C4 alkenylcarbonyl, which substituents are the same or different;
- het is selected from saturated or aromatic heterocycles, for example morpholine, N-methylpiperazine, tetrahydropyrrole, pyridine, thiophene, thiazole, triazole and tetrazole;
- w is an integer from 0 to 2;
- m is an integer from 1 to 5;
- n is an integer from 1 to 3;
- p is independently an integer from 0 to 2;
- and
- q is an integer from 0 to 2.
Dependencies are inferred from the claim text.