Enanta Pharmaceuticals, Inc.

Jiajun Zhang

Yat Sun Or

Hui Cao

Xiaowen Peng

Xuri Gao

Wei Li

Guoqiang Wang

Jorden Kass

Ruichao Shen

Byung-Chul Suh

Yao-Ling Qiu

Xuechao Xing

Joseph D Panarese

Yong He

Matthew C Rhodes

Samuel Bartlett

Kaicheng Zhu

Tao Wang

George G Wu

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof: which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

Spiropyrrolidine derived antiviral agents

Macrocyclic spiropyrrolidine derived antiviral agents

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof: which inhibit picornavirus, norovirus or coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a virus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

The present invention relates to processes for preparing a Compound (1): or a pharmaceutically acceptable salt or solvate thereof. Compound (1) is useful as in many pharmaceutical agents, especially is useful as key intermediate in the synthesis of certain SARS-CoV-2 3CLpro inhibitors.

Processes for the preparation of 4,6,7-trifluoro-1H-indole-2-carboxylic acid

The present invention discloses macrocyclic compounds of Formula (I), and pharmaceutically acceptable salts, thereof: which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

Macrocyclic antiviral agents

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Hepatitis B antiviral agents

The present invention discloses substituted pyrrolo[1,2-c]pyrimidines, such as the compound  which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Substituted pyrrolo[1,2-c]pyrimidines as hepatitis B antiviral agents

The present invention discloses compounds of Formula (Ia), and pharmaceutically acceptable salts, thereof: which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (Ia) or a pharmaceutically acceptable slat thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (Ia) or a pharmaceutically acceptable salt thereof.

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Cambridge, MA, United States of America

Jiajun Zhang