Patent classifications
C07D213/74
BENZOTHIOPHENE DERIVATIVE REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.
##STR00001##
GLP-1 Receptor Agonist and Use Thereof
- Hong Chul Yoon ,
- Kyung Mi An ,
- Myong Jae Lee ,
- Jin Hee Lee ,
- Jeong-geun Kim ,
- A-rang Im ,
- Woo Jin Jeon ,
- Jin Ah Jeong ,
- Jaeho Heo ,
- Changhee Hong ,
- Kyeojin Kim ,
- Jung-Eun Park ,
- Te-ik Sohn ,
- Changmok Oh ,
- Da Hae Hong ,
- Sung Wook Kwon ,
- Jung Ho Kim ,
- Jae Eui Shin ,
- Yeongran Yoo ,
- Min Whan Chang ,
- Eun Hye Jang ,
- In-Gyu Je ,
- Ji Hye Choi ,
- Gunhee Kim ,
- Yearin Jun
The present invention provides novel compounds of chemical formula 1, optical isomers of the compounds, or a pharmaceutically acceptable salts of the compounds, or the optical isomers. The compounds, isomers, and salts exhibits excellent activity as GLP-1 receptor agonists. Particularly, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used therapeutic agents for metabolic diseases. In addition, they exhibits excellent pharmacological safety for cardiovascular systems.
GLP-1 Receptor Agonist and Use Thereof
- Hong Chul Yoon ,
- Kyung Mi An ,
- Myong Jae Lee ,
- Jin Hee Lee ,
- Jeong-geun Kim ,
- A-rang Im ,
- Woo Jin Jeon ,
- Jin Ah Jeong ,
- Jaeho Heo ,
- Changhee Hong ,
- Kyeojin Kim ,
- Jung-Eun Park ,
- Te-ik Sohn ,
- Changmok Oh ,
- Da Hae Hong ,
- Sung Wook Kwon ,
- Jung Ho Kim ,
- Jae Eui Shin ,
- Yeongran Yoo ,
- Min Whan Chang ,
- Eun Hye Jang ,
- In-Gyu Je ,
- Ji Hye Choi ,
- Gunhee Kim ,
- Yearin Jun
The present invention provides novel compounds of chemical formula 1, optical isomers of the compounds, or a pharmaceutically acceptable salts of the compounds, or the optical isomers. The compounds, isomers, and salts exhibits excellent activity as GLP-1 receptor agonists. Particularly, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used therapeutic agents for metabolic diseases. In addition, they exhibits excellent pharmacological safety for cardiovascular systems.
PYRIDINE DERIVATIVES WITH N-LINKED CYCLIC SUBSTITUENTS AS cGAS INHIBITORS
The invention relates to new proline derivatives of formula (I) as cGAS inhibitors,
##STR00001##
wherein
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and G are defined as in claim 1,
and prodrugs or pharmaceutically acceptable salts of these compounds
for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), non-alcoholic steatotic hepatitis (NASH), interstitial lung disease (ILD) and idiopathic pulmonary fibrosis (IPF).
ARYLAMIDE DERIVATIVE HAVING ANTITUMOR ACTIVITY
The present disclosure provides, for example, a compound represented by general formula (6) below or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of the compound or salt:
##STR00001##
wherein X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are each independently —CR.sub.2═ or —N═, R.sub.2 is, for example, a halogen atom, R.sub.1 is, for example, —S(═O).sub.2—NH—R.sub.8, R.sub.8 is, for example, a C1-6 alkyl group, R.sub.3 is, for example, a hydrogen atom, R.sub.5 is, for example, a halogen atom, R.sub.6 is, for example, a hydrogen atom, and R.sub.4 is, for example, a cyclopropyl group. The compounds, salts or solvates provided by the present disclosure exhibit high RAF/MEK complex-stabilizing activity and can be used for the treatment or prevention of cell proliferative disorders, particularly cancers.
ARYLAMIDE DERIVATIVE HAVING ANTITUMOR ACTIVITY
The present disclosure provides, for example, a compound represented by general formula (6) below or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of the compound or salt:
##STR00001##
wherein X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are each independently —CR.sub.2═ or —N═, R.sub.2 is, for example, a halogen atom, R.sub.1 is, for example, —S(═O).sub.2—NH—R.sub.8, R.sub.8 is, for example, a C1-6 alkyl group, R.sub.3 is, for example, a hydrogen atom, R.sub.5 is, for example, a halogen atom, R.sub.6 is, for example, a hydrogen atom, and R.sub.4 is, for example, a cyclopropyl group. The compounds, salts or solvates provided by the present disclosure exhibit high RAF/MEK complex-stabilizing activity and can be used for the treatment or prevention of cell proliferative disorders, particularly cancers.
Therapeutic compositions, combinations, and methods of use
This invention relates to methods comprising administering a FAK inhibitor and an immunotherapeutic agent such as anti-PD-1 or anti-PD-L1; that are useful in the treatment of abnormal cell growth, such as cancer, in mammals, especially humans.
Therapeutic compositions, combinations, and methods of use
This invention relates to methods comprising administering a FAK inhibitor and an immunotherapeutic agent such as anti-PD-1 or anti-PD-L1; that are useful in the treatment of abnormal cell growth, such as cancer, in mammals, especially humans.
HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
##STR00001##
HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
##STR00001##