Patent classifications
C07D239/82
SATURATED-RING-FUSED DIHYDROPYRIMIDINONE OR DIHYDROTRIAZINONE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
The present invention relates to saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds, or pharmaceutically acceptable salts thereof, having ROR antagonist activity, pharmaceutical compositions comprising the same, and pharmaceutical use thereof. A compound of Formula [I] or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and pharmaceutical use thereof are provided:
##STR00001##
wherein each substituent is defined as defined in the description.
SATURATED-RING-FUSED DIHYDROPYRIMIDINONE OR DIHYDROTRIAZINONE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
The present invention relates to saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds, or pharmaceutically acceptable salts thereof, having ROR antagonist activity, pharmaceutical compositions comprising the same, and pharmaceutical use thereof. A compound of Formula [I] or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and pharmaceutical use thereof are provided:
##STR00001##
wherein each substituent is defined as defined in the description.
Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 ##STR00001##
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 ##STR00001##
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
PI3K-ALPHA INHIBITORS AND METHODS OF USE THEREOF
- Alessandro BOEZIO ,
- Lucian V. DIPIETRO ,
- Cary Griffin Fridrich ,
- Hakan GUNAYDIN ,
- Ravi KURUKULASURIYA ,
- Andr? LESCARBEAU ,
- Mary M. MADER ,
- Thomas H. McLean ,
- Levi CharlesThomas PIERCE ,
- Kevin David RAYNOR ,
- Kelley C. SHORTSLEEVES ,
- Yong Tang ,
- Alexander M. Taylor ,
- W. Patrick WALTERS ,
- Hanmo ZHANG ,
- Fabrizio Giordanetto ,
- Yakov PECHERSKY ,
- Qi WANG ,
- Bren-Jordan ATIENZA ,
- Megan BERTRAND-LAPERLE ,
- Andrew J. BURNIE ,
- Fei Chen ,
- Sampada CHITALE ,
- Shorena GELOZIA ,
- Jean-Benoit GIGUERE ,
- Elodie LANDAGARAY ,
- Alexandre LARIVEE ,
- Thomas Lepitre ,
- Gaetan MAERTENS ,
- Johanne OUTIN ,
- Mohan PAL ,
- Claudio Sturino ,
- Kashif TANVEER ,
- Rakesh THORAT ,
- Naresh VEMULA ,
- Elaine B. Krueger ,
- Yue PAN ,
- Michael Paul DENINNO ,
- Yves BOUSQUET ,
- Antoine JOBIN-DES LAURIERS ,
- Jessica LEE ,
- Tarek MOHAMED
The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K-? enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K-? signaling with the compounds and compositions of the disclosure.
PI3K-ALPHA INHIBITORS AND METHODS OF USE THEREOF
- Alessandro BOEZIO ,
- Lucian V. DIPIETRO ,
- Cary Griffin Fridrich ,
- Hakan GUNAYDIN ,
- Ravi KURUKULASURIYA ,
- Andr? LESCARBEAU ,
- Mary M. MADER ,
- Thomas H. McLean ,
- Levi CharlesThomas PIERCE ,
- Kevin David RAYNOR ,
- Kelley C. SHORTSLEEVES ,
- Yong Tang ,
- Alexander M. Taylor ,
- W. Patrick WALTERS ,
- Hanmo ZHANG ,
- Fabrizio Giordanetto ,
- Yakov PECHERSKY ,
- Qi WANG ,
- Bren-Jordan ATIENZA ,
- Megan BERTRAND-LAPERLE ,
- Andrew J. BURNIE ,
- Fei Chen ,
- Sampada CHITALE ,
- Shorena GELOZIA ,
- Jean-Benoit GIGUERE ,
- Elodie LANDAGARAY ,
- Alexandre LARIVEE ,
- Thomas Lepitre ,
- Gaetan MAERTENS ,
- Johanne OUTIN ,
- Mohan PAL ,
- Claudio Sturino ,
- Kashif TANVEER ,
- Rakesh THORAT ,
- Naresh VEMULA ,
- Elaine B. Krueger ,
- Yue PAN ,
- Michael Paul DENINNO ,
- Yves BOUSQUET ,
- Antoine JOBIN-DES LAURIERS ,
- Jessica LEE ,
- Tarek MOHAMED
The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K-? enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K-? signaling with the compounds and compositions of the disclosure.
COMPOUNDS HAVING FLUORENE STRUCTURES
The present invention describes fluorene derivatives substituted by electron-transporting groups, especially for use as triplet matrix materials in electronic devices. The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these.
Tetrahydroquinazoline derivatives as selective cytotoxic agents
The present disclosure is directed to tetrahydroquinazoline derivatives of Formula (I) and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naive cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC). ##STR00001##
Tetrahydroquinazoline derivatives as selective cytotoxic agents
The present disclosure is directed to tetrahydroquinazoline derivatives of Formula (I) and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naive cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC). ##STR00001##
Substituted pyrrolo[3,4-b]pyridines as PI3K-α inhibitors
The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K enzymes with the compounds and compositions of formula I-1. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K signaling with the compounds and compositions of formula I-1. ##STR00001##