PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.

Disclosed herein are compounds and compositions for modulating glycolate oxidase, useful for treating oxalate-related diseases, such as hyperoxaluria, where modulating glycolate oxidase is expected to be therapeutic to a patent in need thereof. Methods of modulating glycolate oxidase activity in a human or animal subject are also provided.

Disclosed herein are compounds and compositions for modulating glycolate oxidase, useful for treating oxalate-related diseases, such as hyperoxaluria, where modulating glycolate oxidase is expected to be therapeutic to a patent in need thereof. Methods of modulating glycolate oxidase activity in a human or animal subject are also provided.

The present invention relates to the pharmaceutically-induced enhancement of DNA damage repair in cells and potential therapeutic applications thereof. In particular, the present invention is directed to an inhibitor of DREAM complex assembly and/or function for use in repairing DNA damage in a cell of a subject. The inhibitor of DREAM complex assembly may be an inhibitory nucleic acid inhibiting the expression of a component of the DREAM complex or an antibody to a component of the DREAM complex. Further disclosed is an inhibitor of DREAM complex assembly and/or function for use in treating and/or preventing a condition associated with DNA damage in a cell in a subject, such as age-related diseases and symptoms of ageing, a progeroid syndrome, acute radiation syndrome, chronic radiation syndrome, Xeroderma pigmentosum, Nijmegen breakage syndrome, Fanconi anemia and ataxia. The invention further discloses a method for obtaining at least one cell with reduced DNA damage, wherein the method comprises steps of providing at least one cell, and treating said at least one cell with an inhibitor of DREAM complex assembly and/or function to repair DNA damage in said cell. Finally, the invention provides pharmaceutical compositions comprising the at least one cell obtainable by said method.

The invention relates to novel compounds of the general formula (I),

##STR00001##

with Het-2 being an optionally substituted bicyclic heteroaryl of the formula

##STR00002##

pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as ferroportin inhibitors, more particularly for the use in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.

The invention relates to novel compounds of the general formula (I),

##STR00001##

with Het-2 being an optionally substituted bicyclic heteroaryl of the formula

##STR00002##

pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as ferroportin inhibitors, more particularly for the use in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.

Amino-pyrazinecarboxamide compounds, conjugates, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. The disclosed compounds are useful, among other things, in the treating of cancer and fibrosis and modulating TGFβR2. Additionally, compounds incorporated into a conjugate with an antibody construct are described herein.

Amino-pyrazinecarboxamide compounds, conjugates, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. The disclosed compounds are useful, among other things, in the treating of cancer and fibrosis and modulating TGFβR2. Additionally, compounds incorporated into a conjugate with an antibody construct are described herein.

The invention relates to carboxamide-pyrimidine derivatives of the general formula I,

##STR00001##

or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

The invention relates to carboxamide-pyrimidine derivatives of the general formula I,

##STR00001##

or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.