Patent classifications
C07D413/06
GLP-1 RECEPTOR AGONIST
The present invention relates to a compound represented by Formula 1 wherein A, B, L, X, and R.sub.1 to R.sub.6 are as described herein, or a pharmaceutically acceptable salt thereof, which serves as a GLP-1 receptor agonist and may be useful in the prevention or treatment of a disease associated with GLP-1 activity.
GLP-1 RECEPTOR AGONIST
The present invention relates to a compound represented by Formula 1 wherein A, B, L, X, and R.sub.1 to R.sub.6 are as described herein, or a pharmaceutically acceptable salt thereof, which serves as a GLP-1 receptor agonist and may be useful in the prevention or treatment of a disease associated with GLP-1 activity.
Macrocyclic chelators and methods of use thereof
Macrocyclic chelators for chelation of alpha-emitting radiometal ions, such as actinium-225 are provided. Also provided are radiometal complexes containing an alpha-emitting radiometal ion bound to the macrocyclic chelator via coordinate bonding, and radioimmunoconjugates containing the radiometal complexes covalently linked to a targeting ligand, such as an antibody or antigen binding fragment thereof. The radioimmunoconjugates can be produced by click chemistry reactions. Methods of using the radiocomplexes and radioimmunoconjugates for selectively targeting neoplastic cells for radiotherapy and for treating neoplastic diseases and disorders are also described.
MATRIPTASE 2 INHIBITORS AND USES THEREOF
The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.
NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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WDR5 INHIBITORS AND MODULATORS
Isoquinolinone compounds and derivatives inhibit WDRS and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
WDR5 INHIBITORS AND MODULATORS
Isoquinolinone compounds and derivatives inhibit WDRS and associated protein-protein interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
Transglutaminase 2 (TG2) inhibitors
Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.
CYCLOPROPYLAMINES AS LSD1 INHIBITORS
This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
CYCLOPROPYLAMINES AS LSD1 INHIBITORS
This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.