Patent classifications
C07D295/096
ANTICANCER COMPOUNDS
Disclosed are compounds of formula (I):
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and pharmaceutically acceptable salts thereof. The compounds of the invention are BDII-selective inhibitors of BET proteins, and have therapeutic potential for treating cancer, acute kidney disease, and viral infections, among other diseases.
GLP-1 RECEPTOR AGONIST AND USE THEREOF
- Hong Chul Yoon ,
- Kyung Mi ,
- 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
Disclosed are novel compounds of Chemical Formula 1, optical isomers of the compounds, and pharmaceutically acceptable salts of the compounds or the optical isomers. The compounds, isomers, and salts exhibit excellent activity as GLP-1 receptor agonists. In particular, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used as therapeutic agents for metabolic diseases. Moreover, they exhibit excellent pharmacological safety for cardiovascular systems.
Bicyclic compounds as inhibitors of PD1/PD-L1 interaction/activation
The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation. ##STR00001##
Bicyclic compounds as inhibitors of PD1/PD-L1 interaction/activation
The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation. ##STR00001##
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, are featured (Formula A) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
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Syntheses of N-heterocyclic carbenes and intermediates therefor
A method of preparing a 2,6 disubstituted anilines includes, reacting a 2-amino isophthalic acid diester with sufficient Grignard reagent R.sub.2CH.sub.2MgX to form the corresponding diol product, dehydrating the diol product to the corresponding dialkene; and hydrogenating the diol product to form the corresponding aniline. The 2,6 disubstituted anilines can be used to produce N-Heterocyclic Carbenes (NHCs). The NHCs can find application in various fields such as organic synthesis, catalysis and macromolecular chemistry. Palladium catalysts containing the NHCs are also described.
Syntheses of N-heterocyclic carbenes and intermediates therefor
A method of preparing a 2,6 disubstituted anilines includes, reacting a 2-amino isophthalic acid diester with sufficient Grignard reagent R.sub.2CH.sub.2MgX to form the corresponding diol product, dehydrating the diol product to the corresponding dialkene; and hydrogenating the diol product to form the corresponding aniline. The 2,6 disubstituted anilines can be used to produce N-Heterocyclic Carbenes (NHCs). The NHCs can find application in various fields such as organic synthesis, catalysis and macromolecular chemistry. Palladium catalysts containing the NHCs are also described.
HETEROCYCLIC DERIVATIVES AS TRMP8 ANTAGONISTS
Disclosed are TRPM8 modulators as defined by formula (I) for achieving a cooling effect on skin and mucosa.
HETEROCYCLIC DERIVATIVES AS TRMP8 ANTAGONISTS
Disclosed are TRPM8 modulators as defined by formula (I) for achieving a cooling effect on skin and mucosa.
Antibacterial agents: arylalkylcarboxamido phloroglucinols
The invention provides compounds of formula (I) or (II) and tautomers and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula (I) or (II) or a tautomer or salt thereof, methods of making a compound of formula (I) or (II) or a tautomer or salt thereof, and methods of using a compound of formula (I) or (II) or a tautomer or salt thereof as, e.g., inhibitors of bacterial RNA polymerase or as antibacterial agents. ##STR00001##