US 11,891,398 B2Granted

2,3-dihydro-1H-pyrrolizine-7-formamide derivative and application thereof

AssigneeChia Tai Tianqing Pharmaceutical Group Co., Ltd.

InventorsHaiying He, Jianhua Xia, Zhen Gong, Jian Li, Shuhui Chen

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Abstract

The present application relates to a 2,3-dihydro-1H-pyrrolizine-7-formamide derivative as a nucleoprotein inhibitor and a use in preparation of a drug for treating HBV related diseases. The present application specifically relates to a compound represented by formula (II), and isomers or pharmaceutically acceptable salts thereof.

Claims20

Dependent claims

A compound of formula (II) or a pharmaceutically acceptable salt thereof,

wherein,
m is 1;
L is selected from
T1 is selected from the group consisting of N and C (R43);
R2 is selected from the group consisting of H and C1-6 alkyl, wherein the C1-6 alkyl is optionally substituted by 1, 2, or 3 Rb;
R3 is selected from the group consisting of Cl, F, Br, I, OH, NH2, C1-6 alkyl, and C1-3 alkoxy, wherein the C1-6 alkyl and the C1-3 alkoxy are optionally substituted by 1, 2, or 3 Rc;
R41, R42, R43, R44, and R45 are each independently selected from the group consisting of H, Cl, F, Br, I, OH, NH2, CN, COOH, and C1-3 alkyl, wherein the C1-3 alkyl is optionally substituted by 1, 2, or 3 Rd;
R5 is selected from the group consisting of R51, C3-10 cycloalkyl, and 3-6 membered heterocycloalkyl, wherein the C3-10 cycloalkyl and the 3-6 membered heterocycloalkyl are optionally substituted by 1, 2, or 3 R1;
R51 is selected from the group consisting of C1-7 alkyl and C1-6 heteroalkyl, wherein the C1-7 alkyl and the C1-6 heteroalkyl are optionally substituted by 1, 2, or 3 Re;
R1 is each independently selected from the group consisting of H, Cl, F, Br, I, OH, NH2, CN, COOH, C1-6 alkyl, —COO—C1-6 alkyl, and —C1-3 alkyl-COO—C1-6 alkyl, wherein the C1-6 alkyl, the —COO—C1-6 alkyl, and the —C1-3 alkyl-COO—C1-6 alkyl are optionally substituted by 1, 2, or 3 Ra;
Ra is each independently selected from the group consisting of Cl, F, Br, I, NH2, CN, COOH, C1-3 alkyl, and C1-3 alkoxy, wherein the C1-3 is optionally substituted by 1, 2, or 3 R;
Rb is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, and COOH;
Re is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, COOH, and C1-3 alkyl, wherein the C1-3 is optionally substituted by 1, 2, or 3 R;
Rd is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, and COOH;
Re is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, and COOH;
R is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, and COOH;
and
the C1-6 heteroalkyl and the 3-6 membered heterocycloalkyl each contain 1, 2, 3, or 4 heteroatoms or heteroatom groups independently selected from the group consisting of —NH—, —O—, —S—, and N.

15 more elements

Dependencies are inferred from the claim text.

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Abstract

A compound of formula (II) or a pharmaceutically acceptable salt thereof,

wherein,
m is 1;
L is selected from
T1 is selected from the group consisting of N and C (R43);
R2 is selected from the group consisting of H and C1-6 alkyl, wherein the C1-6 alkyl is optionally substituted by 1, 2, or 3 Rb;
R3 is selected from the group consisting of Cl, F, Br, I, OH, NH2, C1-6 alkyl, and C1-3 alkoxy, wherein the C1-6 alkyl and the C1-3 alkoxy are optionally substituted by 1, 2, or 3 Rc;
R41, R42, R43, R44, and R45 are each independently selected from the group consisting of H, Cl, F, Br, I, OH, NH2, CN, COOH, and C1-3 alkyl, wherein the C1-3 alkyl is optionally substituted by 1, 2, or 3 Rd;
R5 is selected from the group consisting of R51, C3-10 cycloalkyl, and 3-6 membered heterocycloalkyl, wherein the C3-10 cycloalkyl and the 3-6 membered heterocycloalkyl are optionally substituted by 1, 2, or 3 R1;
R51 is selected from the group consisting of C1-7 alkyl and C1-6 heteroalkyl, wherein the C1-7 alkyl and the C1-6 heteroalkyl are optionally substituted by 1, 2, or 3 Re;
R1 is each independently selected from the group consisting of H, Cl, F, Br, I, OH, NH2, CN, COOH, C1-6 alkyl, —COO—C1-6 alkyl, and —C1-3 alkyl-COO—C1-6 alkyl, wherein the C1-6 alkyl, the —COO—C1-6 alkyl, and the —C1-3 alkyl-COO—C1-6 alkyl are optionally substituted by 1, 2, or 3 Ra;
Ra is each independently selected from the group consisting of Cl, F, Br, I, NH2, CN, COOH, C1-3 alkyl, and C1-3 alkoxy, wherein the C1-3 is optionally substituted by 1, 2, or 3 R;
Rb is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, and COOH;
Re is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, COOH, and C1-3 alkyl, wherein the C1-3 is optionally substituted by 1, 2, or 3 R;
Rd is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, and COOH;
Re is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, and COOH;
R is each independently selected from the group consisting of Cl, F, Br, I, OH, NH2, CN, and COOH;
and
the C1-6 heteroalkyl and the 3-6 membered heterocycloalkyl each contain 1, 2, 3, or 4 heteroatoms or heteroatom groups independently selected from the group consisting of —NH—, —O—, —S—, and N.

15 more elements