Patent classifications
C07D239/90
2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.1e, W, X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, X.sub.6, X.sub.7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated. ##STR00001##
2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.1e, W, X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, X.sub.6, X.sub.7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated. ##STR00001##
COMPOUNDS AND COMPOSITIONS AS EIF4E INHIBITORS AND THE USES THEREOF
Described herein are compounds of Formula I, and their pharmaceutically acceptable salts, solvates, stereoisomers, or prodrugs, as well as their uses (e.g., as eIF4E inhibitors).
COMPOUNDS AND COMPOSITIONS AS EIF4E INHIBITORS AND THE USES THEREOF
Described herein are compounds of Formula I, and their pharmaceutically acceptable salts, solvates, stereoisomers, or prodrugs, as well as their uses (e.g., as eIF4E inhibitors).
PARP inhibitors for treating cancer and asthma
Provided are substituted 8-methylquinazolin-4(3H)-one compounds useful as PARP inhibitors for the treatment of cancer and asthma, as well as pharmaceutical compositions comprising them and methods for their synthesis.
PARP inhibitors for treating cancer and asthma
Provided are substituted 8-methylquinazolin-4(3H)-one compounds useful as PARP inhibitors for the treatment of cancer and asthma, as well as pharmaceutical compositions comprising them and methods for their synthesis.
Compound for Enhancing the Coupling Degree of Complex TRPV4- KCa2.3 and Anti-hypertension Applications thereof
The applicant provides a compound for enhancing the space coupling degree of an endothelial cell ion channel complex TRPV4-KCa2.3 and anti-hypertension applications thereof. By finding the structural domains of the interacting sites of the endothelial cell ion channel complex TRPV4-KCa2.3, a compound with specificity which can act at the two interacting sites is prepared in the present invention. It is found that the compound can enhance the space coupling degree of the TRPV4-KCa2.3 complex and has great significance for the research and development of anti-hypertension drugs.
Compound for Enhancing the Coupling Degree of Complex TRPV4- KCa2.3 and Anti-hypertension Applications thereof
The applicant provides a compound for enhancing the space coupling degree of an endothelial cell ion channel complex TRPV4-KCa2.3 and anti-hypertension applications thereof. By finding the structural domains of the interacting sites of the endothelial cell ion channel complex TRPV4-KCa2.3, a compound with specificity which can act at the two interacting sites is prepared in the present invention. It is found that the compound can enhance the space coupling degree of the TRPV4-KCa2.3 complex and has great significance for the research and development of anti-hypertension drugs.
HETEROAROMATIC NMDA RECEPTOR MODULATORS AND USES THEREOF
Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated modulate the NMDA receptor.
Heterocyclic compound
- Yuhei MIYANOHANA ,
- Yuichi KAJITA ,
- Tatsuki KOIKE ,
- Yasutaka HOASHI ,
- Yasushi Hattori ,
- Norihito Tokunaga ,
- Tsuneo ODA ,
- Tohru Miyazaki ,
- Dilhumar UYGHUR ,
- Yoshiteru ITO ,
- Kohei TAKEUCHI ,
- Keisuke IMAMURA ,
- Takahiro SUGIMOTO ,
- Koichiro FUKUDA ,
- Yasuhisa KOHARA ,
- Rei OKAMOTO ,
- Taiichi OHRA ,
- Naoki MIYAMOTO ,
- Jun CHIBA ,
- Yoshito Terao ,
- Masanori KAWASAKI
The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the description, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.