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US 9,868,737 B2Granted
Pyridino[1,2-A]pyrimidone analogue used as MTOR/P13K inhibitor
AssigneeCisen Pharmaceutical Co., Ltd.
InventorsHuiping Guan, Chengde Wu, Tao Yu, Lei Huang, Dongling Hao, Bo Gao, Jikui Sun, Nengyang Shi, Shuhui Chen
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Abstract
The present invention relates to novel pyridino[1,2-α]pyrimidone compounds represented by formula (I) or pharmaceutically acceptable salts thereof; and a method of use thereof for treating tumors.
Claims8
A compound of formula (I), or a pharmaceutically acceptable salt thereof,
- wherein,
- E is selected from the group consisting of C3-6 cycloalkyl or C1-6 alkyl substituted by R3, and the number of R3 is 0, 1, 2 or 3;
- or E is selected from the group consisting of
- or E is selected from the group consisting of
- optionally substituted by 1, 2, or 3 R3,
- wherein,
- zero, one, two or three of G1-5 are selected from N, and the others are selected from C(R3);
- G6 is selected from the group consisting of —C(R3)(R3)—, —N(R3)—, —O—, and —S—;
- zero, one, or two of G7-9 are N, and the others are selected from C(R3);
- zero or one of G10-16 is N, and the others are selected from C(R3);
- G17 is selected from N and C(R3);
- Zero or one of G18-22, is —O—, and the others are selected from —C(R3)(R3)—;
- one of L and Q is —S(═O)2NH—, and the other is a single bond;
- A is N or CH;
- zero or one of X, Y, and Z is N, and the others are CH;
- m1 is 1;
- R1, R2, and R3 are independently selected from the group consisting of H, F, Cl, Br, I, CN, ORa, N(Rb)(Rc), C1-3 alkyl optionally substituted by Rd,
- D1 is selected from the group consisting of a single bond, —C(Re)(Re)—, —C(═O)N(Ra)—, —N(Ra)—, —S(═O)2 N(Ra)—, and —O—;
- D2 is —C(Ra)(Ra)—;
- n is selected from 1, 2, 3, 4, 5, or 6;
- Ra, Rb, and Rc, are independently selected the group consisting of H, C3-6 cycloalkyl or C1-6 alkyl optionally substituted by Rd;
- Re is selected from the group consisting of H, C1-6 alkyl or alkoxy optionally substituted by Rd, and C3-6 cycloalkyl optionally substituted by Rd;
- Rd is selected from the group consisting of F, Cl, Br, I, CN, OH, CHO, COOH, CH3, CF3, CH3O, and CH3CH2O, and the number of Rd is selected from 0, 1, 2, or 3;
- optionally, Ra and Ra in the same D2, two D2, or Ra and one D2, together with the same carbon atom or oxygen atom to which they both attach, form one 3-, 4-, 5- or 6-membered carbocyclic rings or oxygen-containing heterocyclic rings, wherein the number of oxygen atom is 1 or 2.
21 more elements
Dependencies are inferred from the claim text.