Patent classifications
C07B59/002
IMAGING METHODS USING DEUTERATED COMPOUNDS
The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V):
##STR00001##
##STR00002##
and salts thereof, wherein R.sup.1, R.sup.2, A, and X.sub.10-X.sub.19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.
Compounds and methods for DCAF-mediated protein degradation
Disclosed herein are methods and compounds for inducing DDB1- and CUL4-associated factor 16 (DCAF16)-mediated protein degradation in mammalian cells. In some embodiments, also disclosed herein are methods of modulating the substrate selectivity of a DCAF16-CUL4-RBX1-DDB1 complex (CRL4) for modulating protein degradation.
Condensed cyclic compound and organic light-emitting device including the same
Provided are a condensed cyclic compound represented by Formula 1 and an organic light-emitting device including the same: ##STR00001##
wherein, in Formula 1, X.sub.1, A.sub.1, L.sub.11, a11, Ar.sub.11, Ar.sub.12, b11, R.sub.11, R.sub.12, c11, and c12 are the same as defined in the specification.
2-alkoxy-6-[18F]fluoronicotinoyl substituted lys-c(O)-glu derivatives as efficient probes for imaging of PSMA expressing tissues
6-[.sup.18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [.sup.18F]DCFPyL, [.sup.68Ga]HBED-CC-PSMA, [.sup.18F]PSMA-1007 and [Al.sup.18F]HBED-CC-PSMA. Unexpectedly, the 6-[.sup.18F]fluoro-2-alkoxy and 6-[.sup.18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [.sup.18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the .sup.18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[.sup.18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [.sup.68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.
Low affinity poly(AD-ribose) polymerase 1 dependent cytotoxic agents
The present disclosure provides compounds of Formula (I) or (II), pharmaceutically acceptable salt, isotopic variant, stereoisomer, or a mixture thereof. Also provided are pharmaceutical compositions comprising a compound, methods of treating a poly(ADP-ribose)polymerase-1-mediated disease or disorder in a subject, methods of detecting a poly(ADP-ribose)polymerase-1-mediated neurodegenerative disease or disorder, or methods of monitoring cancer treatment in a subject. In some embodiments, the poly(ADP-ribose)polymerase-1-mediated disease or disorder is a neurodegenerative disease or cancer. ##STR00001##
MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
CRF RECEPTOR ANTAGONISTS AND METHODS OF USE
Compounds are provided herein, as well as related preparations, compositions and methods for treating diseases and/or disorders that would benefit from the same such as congenital adrenal hyperplasia (CAH).
ORGANIC ELECTROLUMINESCENCE DEVICE AND POLYCYCLIC COMPOUND FOR ORGANIC ELECTROLUMINESCENCE DEVICE
An organic electroluminescence device includes a first electrode, a hole transport region disposed on the first electrode, an emission layer disposed on the hole transport region, an electron transport region disposed on the emission layer, and a second electrode disposed on the electron transport region, wherein the hole transport region includes a polycyclic compound represented by Formula 1, and the device shows high emission efficiency:
##STR00001##
COMPOUND OR SALT THEREOF
The present invention relates to a compound represented by the following General Formula (1) or a salt thereof.
##STR00001##
In General Formula (1), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a linear or branched alkyl group which may have a substituent or the like. R.sup.1 and R.sup.2 may be bonded to each other to form a ring. R.sup.3 and R.sup.4 may be bonded to each other to form a ring. R.sup.1 and/or R.sup.2 may be bonded to a 6-membered ring to which —NR.sup.1R.sup.2 is bonded to form a ring. R.sup.3 and/or R.sup.4 may be bonded to a 6-membered ring to which —NR.sup.3R.sup.4 is bonded to form a ring. R.sup.5 represents —.sup.11CH.sub.3, a linear or branched alkyl group which may have a substituent or the like. R.sup.6 represents —F, —.sup.18F or the like. X, Y and Z each independently represent a carbon atom, an oxygen atom or the like. n is 0 or 1.
ORGANIC LIGHT-EMITTING ELEMENT
Provided is an organic light-emitting device including a light-emitting layer comprising a compound of Chemical Formula 1, and a first organic material layer comprising a compound of Chemical Formula 2:
##STR00001## wherein: Cy1 to Cy5 are each independently one selected from the group consisting of a substituted or unsubstituted: aromatic hydrocarbon ring, aliphatic hydrocarbon ring, and an aromatic hetero ring, or a ring in which two or more rings selected from the above group are fused, one or more of Cy1 to Cy5 are a ring of the following Chemical Formula 1-A,
##STR00002##
wherein: Ar1 and Ar2 are the same as or different from each other, and are each independently a phenyl, a biphenyl, a terphenyl, a naphthyl, a phenanthrenyl, or a triphenylenyl, where the naphthyl, phenanthrenyl, and triphenylenyl can be substituted with a phenyl.