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US 2022/0033376 A1Published application
Estrogen receptor antagonist
AssigneeChia Tai Tianqing Pharmaceutical Group Co., Ltd.
InventorsShuwen DUAN, Jianyu LU, Lihong HU, Charles Z. DING, Guoping HU, Jian LI, Shuhui CHEN
Life of this patent
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Abstract
Provided is an indole compound. In particular, disclosed are a compound represented by formula (II) or an isomer or pharmaceutically acceptable salt thereof and a use of the same as an estrogen receptor antagonist in preparing a drug for treating estrogen receptor-positive breast cancer.
Claims20
A compound of formula (II), an isomer thereof or a pharmaceutically acceptable salt thereof,
- wherein,
- X is selected from the group consisting of NH, O and S;
- Y is selected from the group consisting of N and CR7;
- Y1 is CH, and Y2 is N;
- or, Y1 is N, and Y2 is CH or CF;
- or, Y1 is CH, and Y2 is CH;
- L is
- ring A is selected from the group consisting of C6-10 aryl and 5-10 membered heteroaryl;
- R1 is selected from the group consisting of H, halogen, CN, COOH, NH2, C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl, the C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl being optionally substituted with 1, 2 or 3 Ra;
- R2 is selected from the group consisting of C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl, the C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl being optionally substituted with 1, 2 or 3 Rb;
- R3 is selected from the group consisting of H, halogen, CN, NO2, OH, COOH, NH2, C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl, the C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl being optionally substituted with 1, 2 or 3 Rc;
- R13 is H or
- R4 is selected from the group consisting of COOH, NH2, C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl, 3-6 membered heterocycloalkyl, phenyl and 5-6 membered heteroaryl, the C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl, 3-6 membered heterocycloalkyl, phenyl and 5-6 membered heteroaryl being optionally substituted with 1, 2 or 3 Rd;
- R5 is selected from the group consisting of H, C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl, the C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl being optionally substituted with 1, 2 or 3 Re;
- R6, R7, R8 and R9 are each independently selected from the group consisting of H, halogen, CN, NO2, OH, COOH, NH2, C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl, the C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl being optionally substituted with 1, 2 or 3 Rf;
- R10, R11 and R12 are each independently selected from the group consisting of H, halogen, CN, NO2, OH, COOH, NH2, C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl, the C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl and 3-6 membered heterocycloalkyl being optionally substituted with 1, 2 or 3 Rg;
- Ra, Rb, Re, Rd, Re, Rf and Rg are each independently selected from the group consisting of H, F, Cl, Br, I, OH, CN, NH2, COOH, C(═O)NH2, C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl, 3-6 membered heterocycloalkyl and C3-6 cycloalkyl-C1-3 alkyl-, the C1-6 alkyl, C1-6 heteroalkyl, C3-6 cycloalkyl, 3-6 membered heterocycloalkyl and C3-6 cycloalkyl-C1-3 alkyl- being optionally substituted with 1, 2 or 3 R;
- R is independently selected from the group consisting of F, Cl, Br, I, OH, CN, NH2, COOH, Me, Et, CF3, CHF2, CH2F, NHCH3, and N(CH3)2;
- the C1-6 heteroalkyl, 3-6 membered heterocycloalkyl and 5-6 membered heteroaryl each comprise 1, 2, 3 or 4 heteroatoms or heteroatom groups each independently selected from the group consisting of —NH—, —O—, —S—, —O—N═, —C(═O)—O—, —C(═O)—S—, —C(═O)—, —C(═S)—, —S(═O)—, —S(═O)2— and N.
16 more elements
Dependencies are inferred from the claim text.