Patent classifications
C07D515/04
HYBRID CYCLIC LIBRARIES AND SCREENS THEREOF
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
HYBRID CYCLIC LIBRARIES AND SCREENS THEREOF
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
Nrf2 regulators
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
Nrf2 regulators
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
Cyanopyridine Derivatives as Liver X Receptor Beta Agonists, Compositions, and Their Use
In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X- receptor (LXR) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
The present invention relates to compounds containing fused dibenzo more-than-six-membered heterocycles or azaheterocycles. These compounds may be useful as host materials for phosphorescent electroluminescent devices.
ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
The present invention relates to compounds containing fused dibenzo more-than-six-membered heterocycles or azaheterocycles. These compounds may be useful as host materials for phosphorescent electroluminescent devices.
INDAZOLE COMPOUNDS
Disclosed herein are compounds and methods of treating diseases and/or conditions associated with FGFR inhibition.
COMPOUNDS AS MODULATORS OF ENDOPLASMIC RETICULUM AMINOPEPTIDASE 1 (ERAP1)
A compound of formula (I-1), or a pharmaceutically accept able salt or hydrate thereof, formula (I-1) wherein: ring A is a monocyclic 5, 6, or 7-membered heterocycloalkyl ring optionally substituted by one or more substituents selected from alkyl, CN, cycloalkyl, OH, alkoxy, halo, haloalkyl and heteroaryl, wherein said heteroaryl group is in turn optionally further substituted with one or more groups selected from halo and alkyl, and wherein one or two carbons in the 5, 6, or 7-membered heterocycloalkyl ring are optionally replaced by a group selected from O, NH, S and CO; L is a linker group which is a 2 to 7-membered saturated or unsaturated aliphatic group, wherein one or two carbon atoms in said group, other than the carbon atom directly bonded to ring A, are optionally replaced by a heteroatom-containing group selected from O, NH and S, and wherein when two carbon atoms are replaced, the heteroatom-containing groups are separated by at least two carbon atoms and the linker group is at least a 5-membered group; the group XY is NR.sub.23SO.sub.2 or SO.sub.2NR.sub.23; R.sub.1 is H, CN or alkyl; R.sub.2 is selected from COOH, tetrazolyl and C(O)NHSO.sub.2R.sub.24; R.sub.3 is selected from H, halo and alkyl; R.sub.4 is selected from H and halo; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.18R.sub.19, CONR.sub.20R.sub.21, heteroaryl and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents select ed from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; R.sub.9 is H, alkyl or halo; R.sub.18-R.sub.21 and R.sub.23 are each independently selected from H and alkyl; R.sub.24 is selected from alkyl and cyclopropyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications.
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COMPOUNDS AS MODULATORS OF ENDOPLASMIC RETICULUM AMINOPEPTIDASE 1 (ERAP1)
A compound of formula (I-1), or a pharmaceutically accept able salt or hydrate thereof, formula (I-1) wherein: ring A is a monocyclic 5, 6, or 7-membered heterocycloalkyl ring optionally substituted by one or more substituents selected from alkyl, CN, cycloalkyl, OH, alkoxy, halo, haloalkyl and heteroaryl, wherein said heteroaryl group is in turn optionally further substituted with one or more groups selected from halo and alkyl, and wherein one or two carbons in the 5, 6, or 7-membered heterocycloalkyl ring are optionally replaced by a group selected from O, NH, S and CO; L is a linker group which is a 2 to 7-membered saturated or unsaturated aliphatic group, wherein one or two carbon atoms in said group, other than the carbon atom directly bonded to ring A, are optionally replaced by a heteroatom-containing group selected from O, NH and S, and wherein when two carbon atoms are replaced, the heteroatom-containing groups are separated by at least two carbon atoms and the linker group is at least a 5-membered group; the group XY is NR.sub.23SO.sub.2 or SO.sub.2NR.sub.23; R.sub.1 is H, CN or alkyl; R.sub.2 is selected from COOH, tetrazolyl and C(O)NHSO.sub.2R.sub.24; R.sub.3 is selected from H, halo and alkyl; R.sub.4 is selected from H and halo; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.18R.sub.19, CONR.sub.20R.sub.21, heteroaryl and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents select ed from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; R.sub.9 is H, alkyl or halo; R.sub.18-R.sub.21 and R.sub.23 are each independently selected from H and alkyl; R.sub.24 is selected from alkyl and cyclopropyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications.
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