Back to results
US 10,519,133 B2Granted
Vinyl compounds as FGFR and VEGFR inhibitors
AssigneesMedshine Discovery Inc., Harbin Zhenbao Pharmaceutical Co., Ltd.
InventorsShuhui Chen, Zhengxia Chen, Meibi Dai, Cheng Xie, Peng Li, Yang Zhang, Guibai Liang, Qiang Wang, Jiangpeng Liao, Fei Sun, Guoping Hu, Jian Li
Life of this patent
Estimating the term…
Abstract
FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.
Claims16
A compound represented by formula (I) or formula (II), a pharmaceutically acceptable salt or a tautomer thereof,
- wherein, one of R1 and R2 is selected from the group consisting of F, Cl, Br, I, CN, OH and NH2, the other is selected from the group consisting of H, F, Cl, Br, I, CN, OH and NH2;
- B1 is selected from the group consisting of
- L1 and L3 are each independently selected from the group consisting of —(CRR)0-3—, —(CRR)0-3—N(R)—(CRR)0-3— and —(CRR)0-3—O—(CRR)0-3—;
- B2 is selected from a 5- to 10-membered aryl or heteroaryl which is optionally substituted with R;
- B4 is selected from a 5- to 6-membered aryl or heteroaryl and a 5- to 6-membered cycloalkyl or heterocycloalkyl, each of which is optionally substituted with R;
- T31-34 are each independently selected from N or C(R);
- optionally, any two of T31-34 are connected to the same atom or atom group to form a 3-6 membered ring;
- n is 1;
- R is selected from the group consisting of H, F, Cl, Br, I, CN, SH, NH2, CHO, COOH, C(═O)NH2, S(═O)NH2, S(═O)2NH2, or selected from a C1-12 alkyl or heteroalkyl, a C3-12 cyclocarbyl or heterocyclocarbyl, and a C1-12 alkyl or heteroalkyl substituted with a C3-12 cyclocarbyl or heterocyclocarbyl;
- and the C1-12 alkyl or heteroalkyl and the C3-12 cyclocarbyl or heterocyclocarbyl is optionally substituted with R′;
- R′ is selected from the group consisting of F, Cl, Br, I, CN, OH, SH, NH2, CHO, COOH, C(═O)NH2, S(═O)NH2, S(═O)2NH2, ═NH, ═O, ═S, or selected from the group optionally substituted with R″ consisting of NHC(═O)CH3, a C1-12 alkyl, a C1-12 alkylamino, N,N-di(C1-12 alkyl)amino, a C1-12 alkoxy, a C1-12 alkanoyl, a C1-12 alkoxycarbonyl, a C1-12 alkylsulfonyl, a C1-12 alkylsulfinyl, a 3- to 12-membered cycloalkyl, a 3- to 12-membered cycloalkylamino, a 3- to 12-membered heterocycloalkylamino, a 3- to 12-membered cycloalkyloxy, a 3- to 12-membered cycloalkylcarbonyl, a 3- to 12-membered cycloalkyloxycarbonyl, a 3- to 12-membered cycloalkylsulfonyl, a 3- to 12-cycloalkylsulfinyl, a 5- to 12-membered aryl or heteroaryl, a 5 to 12-membered aralkyl or heteroaralkyl;
- R″ is selected from the group consisting of F, Cl, Br, I, CN, OH, N(CH3)2, NH(CH3), NH2, CHO, COOH, C(═O)NH2, S(═O)NH2, S(═O)2NH2, ═NH, ═O, ═S, trihalomethyl, dihalomethyl, monohalomethyl, aminomethyl, hydroxymethyl, methyl, methoxy, formyl, methoxycarbonyl, methanesulfonyl, methylsulfinyl;
- “hetero” represents a heteroatom or a heteroatom group selected from the group consisting of —C(═O)N(R)—, —N(R)—, —C(═NR)—, —S(═O)2N(R)—, —S(═O)N(R)—, —O—, —S—, ═O, ═S, —C(═O)O—, —C(═O)—, —C(═S)—, —S(═O)—, —S(═O)2— and/or —N(R)C(═O)N(R)—;
- in each of the above cases, the number of R, R′, R″, heteroatoms or heteroatom groups is independently selected from 0, 1, 2 or 3.
11 more elements
Dependencies are inferred from the claim text.