The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of choice concerning inflammation and atherosclerosis progression. Thus, the present invention relates to radiolabeled Darapladib and analogs thereof and their use as imaging compounds.

The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

A hydrate inhibitor comprising a boronic acid moiety and associated methods and compositions.

The present invention relates to heteroaryl heterocyclic compounds, e.g., the compound of the formula shown below, pharmaceutical compositions comprising same, methods for preparing same, and uses thereof.

##STR00001##

Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.

The present disclosure describes a synthetic process and novel intermediates related to spirocyclic azetidenyl-isobenzofuran derivatives having an isothiazoline moiety, which are useful as antiparasitics.

The present invention relates to a boron hydroxyl-containing organic compound having a structural formula shown in formula I. The present invention also relates to a method for preparing the boron hydroxyl-containing organic compound and use thereof in an organic electronic device, particularly an organic light-emitting diode. The present invention further relates to an organic electronic device, particularly an organic light-emitting diode, including the boron hydroxyl-containing organic compound according to the present invention and use thereof in display and lighting technology. By optimizing the structure of the device and altering the concentration of the boron hydroxyl-containing organic compound in the substrate, the optimal device performance can be achieved so as to produce an OLED device with high efficiency, high brightness and high stability, which provides a better material option for use in full-color display and lighting.

An object of the present invention is to provide a compound useful as a therapeutic drug for an autoimmune disease such as systemic lupus erythematosus (SLE) and lupus nephritis of SLE patients by suppressing immune cell function by inhibiting proliferation of activated T cells and production of interferon alpha (IFN-α).

The present invention provides a compound represented by formula (I):

##STR00001##

wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined in the specification,
or a pharmaceutically acceptable salt thereof.

A compound of formula F.sub.a-L-I.sub.a (A) or F.sub.a-I.sub.a (B), wherein Fa is a fibroblast activation protein alpha (FAPα) targeting moiety, L is a linker, and I.sub.a is an inhibitor of a signaling pathway necessary for fibrosis in cancer-associated fibroblasts (CAFs); a pharmaceutical composition comprising same; and methods for treating a tumor, a cancer or a fibrotic disease in a subject.

The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to triazolopyrimidine and imidazolopyrimidine inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.