C07D491/044

FGFR4 INHIBITOR, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF

Provided are an FGFR4 inhibitor having the structure of formula (1), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs.

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Method for producing optically active substance, optically active substance, method for producing chiral molecule, and chiral molecule

Provided is a method for producing an optically active substance, the method including an asymmetric induction, wherein an asymmetry inducer is allowed to act on a chiral molecule having a half-life of enantiomeric excess of shorter than 10 hours, thereby increasing abundance of one enantiomer of the chiral molecule. According to this method, one enantiomer of a chiral molecule that is susceptible to racemization can be selectively and efficiently obtained.

Method for producing optically active substance, optically active substance, method for producing chiral molecule, and chiral molecule

Provided is a method for producing an optically active substance, the method including an asymmetric induction, wherein an asymmetry inducer is allowed to act on a chiral molecule having a half-life of enantiomeric excess of shorter than 10 hours, thereby increasing abundance of one enantiomer of the chiral molecule. According to this method, one enantiomer of a chiral molecule that is susceptible to racemization can be selectively and efficiently obtained.

ANTIVIRAL HETEROCYCLIC COMPOUNDS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:

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which inhibit Human Respiratory Syncytial Virus (HRSV) or Human Metapneumovirus (HMPV) inhibitors. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HRSV or HMPV infection. The invention also relates to methods of treating an HRSV or HMPV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

ANTIVIRAL HETEROCYCLIC COMPOUNDS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:

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which inhibit Human Respiratory Syncytial Virus (HRSV) or Human Metapneumovirus (HMPV) inhibitors. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HRSV or HMPV infection. The invention also relates to methods of treating an HRSV or HMPV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

CHEMICAL COMPOUNDS

The invention is directed to compounds of formula (I), and salts thereof. The compounds are inhibitors of kinase activity, in particular PI3-kinase activity.

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CHEMICAL COMPOUNDS

The invention is directed to compounds of formula (I), and salts thereof. The compounds are inhibitors of kinase activity, in particular PI3-kinase activity.

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Tricyclic compounds as histone methyltransferase inhibitors

The present disclosure provides certain tricyclic compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Tricyclic compounds as histone methyltransferase inhibitors

The present disclosure provides certain tricyclic compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

METHOD FOR PREPARATION OF ASENAPINE
20230159549 · 2023-05-25 ·

The present invention relates to a method for preparing Asenapine. In particular, the present invention relates to a method for preparing pharmaceutically acceptable Asenapine free base and new crystal form thereof, and also relates to methods for preparing the intermediate compounds used in said method.