Patent classifications
A61K31/497
RNA METHYLTRANSFERASE INHIBITOR, SCREENING METHOD THEREFOR, ANTI-CANCER AGENT EFFICACY ASSESSMENT MARKER, AND KIT FOR EFFECTIVELY PREDICTING FTSJ1 INHIBITOR
An RNA methyltransferase inhibitor comprising sulfonamide-based compounds and/or pyrazoline-based compounds is provided
CHRONIC KIDNEY DISEASE TREATMENT OR PREVENTION METHOD
One aim of the present invention is to treat or prevent chronic kidney disease. Provided is a treatment or prophylactic pharmaceutical composition for chronic kidney disease, that contains an SGLTl-inhibiting compound or a pharmaceutically acceptable salt thereof.
CHRONIC KIDNEY DISEASE TREATMENT OR PREVENTION METHOD
One aim of the present invention is to treat or prevent chronic kidney disease. Provided is a treatment or prophylactic pharmaceutical composition for chronic kidney disease, that contains an SGLTl-inhibiting compound or a pharmaceutically acceptable salt thereof.
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.
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.
Aryl hydrocarbon receptor modulators
The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.
Aryl hydrocarbon receptor modulators
The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, ##STR00001## R′ is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3, ##STR00002##
two R.sub.a is independently H, or two R.sub.a together form ═O or ═N—W.sub.3—R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.
Compounds useful as inhibitors of helios protein
Disclosed are compounds of Formula (I): ##STR00001##
or a salt thereof, wherein: Z is CR.sub.6R.sub.6 or C═O; Ring A is: ##STR00002##
and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, m, and n are defined herein. Also disclosed are methods of using such compounds to inhibit Helios protein, and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors
The present invention covers combinations of at least two components, component A and component B, comprising component A being an inhibitor of ATR kinase, particularly an inhibitor of ATR kinase selected from VX-803, VX-970, AZD-6738, a compound of general formula (I) described herein, a compound of general formula (Ib) described herein and Compound A described infra, and component B being a PD-1/PD-L1 inhibitor described herein. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.
Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors
The present invention covers combinations of at least two components, component A and component B, comprising component A being an inhibitor of ATR kinase, particularly an inhibitor of ATR kinase selected from VX-803, VX-970, AZD-6738, a compound of general formula (I) described herein, a compound of general formula (Ib) described herein and Compound A described infra, and component B being a PD-1/PD-L1 inhibitor described herein. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.