C07D253/08

Neprilysin inhibitors

In one aspect, the invention relates to compounds having the formula XII: ##STR00001##
where R.sup.a, R.sup.b, R.sup.2, R.sup.7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Substituted benzazinones as antibacterial compounds

The present invention relates to LpxC antibacterial compounds of Formula (IA): ##STR00001##
corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.

Substituted benzazinones as antibacterial compounds

The present invention relates to LpxC antibacterial compounds of Formula (IA): ##STR00001##
corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.

BIOREDUCTIVELY-ACTIVATED COMPOUNDS, THEIR PRODRUGS, RADIOPHARMACEUTICALS, THE COMPOSITIONS, AND THEIR APPLICATIONS IN MULTIMODAL THERANOSTIC MANAGEMENT OF HYPOXIA DISEASES INCLUDING CANCER

Described herein are bioreductively-activated compounds, their prodrugs, radiopharmaceuticals, the compositions, and their application in multimodal theranostic management of hypoxia diseases including cancer.

MARKERS, CONJUGATES, COMPOSITIONS AND METHODS FOR HYPOXIA IMAGING, MAPPING, AND THERAPY

Described herein are markers, conjugates, compositions and methods for hypoxia imaging, mapping, and therapy. A compound comprising bio-reductively activated (BA) arm, linker arm and a mapping click wherein BA contains one for more of substituted or unsubstituted 2/4/5-substituted nitroimidazoles, or substituted benzotriazene-1,4-dioxides, or substituted 1,2,3/1,2,4-triazoles, or substituted 1,4-benzoquinones, or a combination of two homo-or hetero BA moieties, wherein linker arm contains C1-16 alkane, alkene, alkyne, alicyclic or aromatic linkers with or without hetero atoms as in ethers, amine, esters, acid, amides, 5 and 6 membered sugar sings with the substitution as described above, both monosaccharides and disaccharides, wherein mapping click contains one of substituted or unsubstituted N3-, CN, SCN, substituted alkynes for click chemistry. Said compound undergoes in situ click reaction after its distribution in cells or tissues to link to a reporting group which may be unchelated or chelated with a metal-radioactive or non-radioactive-, or a radiohalogen for PET/SPECT, or a dye for fluorescent/optical reporting group, thus accomplishing hypoxia imaging

MARKERS, CONJUGATES, COMPOSITIONS AND METHODS FOR HYPOXIA IMAGING, MAPPING, AND THERAPY

Described herein are markers, conjugates, compositions and methods for hypoxia imaging, mapping, and therapy. A compound comprising bio-reductively activated (BA) arm, linker arm and a mapping click wherein BA contains one for more of substituted or unsubstituted 2/4/5-substituted nitroimidazoles, or substituted benzotriazene-1,4-dioxides, or substituted 1,2,3/1,2,4-triazoles, or substituted 1,4-benzoquinones, or a combination of two homo-or hetero BA moieties, wherein linker arm contains C1-16 alkane, alkene, alkyne, alicyclic or aromatic linkers with or without hetero atoms as in ethers, amine, esters, acid, amides, 5 and 6 membered sugar sings with the substitution as described above, both monosaccharides and disaccharides, wherein mapping click contains one of substituted or unsubstituted N3-, CN, SCN, substituted alkynes for click chemistry. Said compound undergoes in situ click reaction after its distribution in cells or tissues to link to a reporting group which may be unchelated or chelated with a metal-radioactive or non-radioactive-, or a radiohalogen for PET/SPECT, or a dye for fluorescent/optical reporting group, thus accomplishing hypoxia imaging

4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE MODULATORS OF GPR139

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1:

##STR00001##

which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE MODULATORS OF GPR139

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1:

##STR00001##

which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

NOVEL PIPERIDINE-2,6-DIONE DERIVATIVE AND USE THEREOF

The present disclosure relates to a novel piperidine-2,6-dione derivative and a use thereof and, more specifically, to a piperidine-2,6-dione derivative compound having a structure of a thalidomide analog. A compound of chemical formula 1 according to the present disclosure specifically binds with CRBN protein, and is involved in functions thereof. Therefore, the compound of the present disclosure can be favorably used in the prevention or treatment of leprosy, chronic graft versus host disease, an inflammatory disease, or cancer, which are caused by actions of CRBN protein.

4-oxo-3,4-dihydro-1,2,3-benzotriazine modulators of GPR139

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: ##STR00001##
which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.