Patent classifications
C07D498/18
Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
A compound of Formula I, ##STR00001##
and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.
Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
A compound of Formula I, ##STR00001##
and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.
ENDOCYCLIC PYRIMIDINONE COMPOUNDS, AND PREPARATION METHODS, COMPOSITIONS AND USE THEREOF
Disclosed is an endocyclic pyrimidinone compound of Formula (I) or a pharmaceutically acceptable salt thereof, which is an entirely new Lp-PLA2 inhibitor useful in treating neurodegeneration-related diseases such as Alzheimer's disease (AD), glaucoma and age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis.
ENDOCYCLIC PYRIMIDINONE COMPOUNDS, AND PREPARATION METHODS, COMPOSITIONS AND USE THEREOF
Disclosed is an endocyclic pyrimidinone compound of Formula (I) or a pharmaceutically acceptable salt thereof, which is an entirely new Lp-PLA2 inhibitor useful in treating neurodegeneration-related diseases such as Alzheimer's disease (AD), glaucoma and age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis.
Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following formula (I): ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, L, W.sup.1, W.sup.2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following formula (I): ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, L, W.sup.1, W.sup.2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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.
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.
PTEFB inhibiting macrocyclic compounds
The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
PTEFB inhibiting macrocyclic compounds
The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).