Patent classifications
C07F9/65583
SMALL MOLECULE DEGRADERS OF HELIOS AND METODS OF USE
Disclosed are compounds and pharmaceutically acceptable salts, hydrates, solvates, prodrugs, stereoisomers, or tautomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders associated with Helios and which may benefit from Helios degradation.
COMPOUND AS SHP2 INHIBITOR AND USE THEREOF
The present invention falls within the field of medical chemistry and relates to a class of compounds as SHP2 inhibitors and the use thereof. Specifically, the present invention provides a compound represented by formula (I), or an isomer, a pharmaceutically acceptable salt, a solvate, a crystal or a prodrug thereof, a preparation method therefor, a pharmaceutical composition comprising the compounds, and the use of the compounds or the composition for treating a disease mediated by SHP2.
Heterocyclic compounds for the treatment of neurological and psychological disorders
Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed. ##STR00001##
COMPOUND USED AS EGFR KINASE INHIBITOR AND USE THEREOF
The present invention relates to a compound used as an EGFR kinase inhibitor and the use thereof. The compound has a structure as shown in formula I, and can be used to adjust the kinase activity or treat related diseases, especially non-small cell lung cancer.
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ANTICANCER COMPOUND AND MEDICAL USE THEREOF
A compound of formula (I), or pharmaceutically acceptable salts, solvates, isotopic variants, or isomers thereof, and anticancer medical use are provided.
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Pyrimidine compounds useful as tyrosine kinase inhibitors
The present disclosure provides pyrimidine compounds useful as tyrosine kinase inhibitors, and particularly epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) inhibitors. The disclosed EGFR inhibitors are effective against acquired resistance mutations appearing after treatment of existing EGFR inhibitors. The present disclosure also provides methods of treating cancer using pyrimidine compounds and pharmaceutical compositions comprising pyrimidine compounds. The methods of treating cancer may be directed to cancer with acquired resistance mutations.
Protease Inhibitors for Treatment of Coronavirus Infections
- Arnab K. Chatterjee ,
- Jian Jeffrey Chen ,
- Elshan Nakath ,
- Alireza Rahimi ,
- Anil Kumar Gupta ,
- Gennadii Grabovyi ,
- Katy Wilson ,
- Sourav Ghorai ,
- Armen Nazarian ,
- James Pedroarena ,
- Wrickban Mazumdar ,
- Frank Weiss ,
- Lirui Song ,
- Malina A. Bakowski ,
- Laura Riva ,
- Karen Wolff ,
- Case W. McNamara ,
- Thomas F. Rogers ,
- Jacqueline Malvin ,
- Shuangwei Li ,
- Sean Joseph ,
- Ashley Woods ,
- Yuyin Liu ,
- Neechi Okwor
Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions:
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, and A are defined in the present disclosure. The compounds are potent inhibitors of the main protease (M.sup.pro) of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), and they are useful in treating or preventing COVID-19 in a subject.
PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS
The present disclosure provides selective phosphoinositide 3-kinase gamma inhibitors of Formula (I) including (I-a), (I-b), (I-c), and (I-d), or pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of conditions mediated by one or more PI3K isoforms, such as PI3K gamma (PI3Kγ). The present disclosure further provides methods of inhibiting phosphoinositide 3-kinase gamma using these compounds for treatment of disorders related to phosphatidylinositol 3-kinase gamma activity.
PYRIMIDINE COMPOUND AS AXL INHIBITOR
A pyrimidine compound as an AXL inhibitor is provided. The structure of the pyrimidine compound is as shown in general formula I, and the definition of each substituent is as described in the description. The present invention further provides a preparation method for the pyrimidine compound. The pyrimidine compound of the present invention has significant AXL inhibitory activity, and can be used as an AXL inhibitor.
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COMPOSITIONS AND METHODS FOR THE TREATMENT OF LIVER DISORDERS
The present disclosure is directed to FXR agonists, pharmaceutical compositions thereof, and methods of using the same for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis, either alone or in combination with thyroid receptor agonists.