A61K31/54

ALLOSTERIC EGFR INHIBITORS AND METHODS OF USE THEREOF

The disclosure relates to compounds that act as allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

ALLOSTERIC EGFR INHIBITORS AND METHODS OF USE THEREOF

The disclosure relates to compounds that act as allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

Prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury and inflammation, cell protection agent for transplantation, and bio-preservation agent

The present invention provides a prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury or inflammation, an agent for protecting cells for transplantation, and an agent for preserving organism. A prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury or inflammation, an agent for protecting cells for transplantation, or an agent for preserving organism, containing, as an active ingredient, at least one kind selected from a heterocyclic compound represented by the formula (I) ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof; an isothiocyanate compound represented by the formula S═C═N—R.sup.5 (II) wherein the symbol is as described in the DESCRIPTION; and a TRPA1 agonist.

Prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury and inflammation, cell protection agent for transplantation, and bio-preservation agent

The present invention provides a prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury or inflammation, an agent for protecting cells for transplantation, and an agent for preserving organism. A prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury or inflammation, an agent for protecting cells for transplantation, or an agent for preserving organism, containing, as an active ingredient, at least one kind selected from a heterocyclic compound represented by the formula (I) ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof; an isothiocyanate compound represented by the formula S═C═N—R.sup.5 (II) wherein the symbol is as described in the DESCRIPTION; and a TRPA1 agonist.

Method of treatment of cirrhosis

The invention relates to a method of treating cirrhosis which comprises administering to a subject in need thereof lanifibranor or a deuterated derivative thereof.

Urea-substituted aromatic ring-linked dioxinoquinoline compounds, preparation method and uses thereof

The present invention relates to an urea-substituted aromatic ring-linked dioxinoquinoline compound of formula (I), or a pharmaceutically acceptable salt or a hydrate thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2, C-RAF, B-RAF, and RET) inhibitor is used for treating disorders related to tyrosine kinase. ##STR00001##

Urea-substituted aromatic ring-linked dioxinoquinoline compounds, preparation method and uses thereof

The present invention relates to an urea-substituted aromatic ring-linked dioxinoquinoline compound of formula (I), or a pharmaceutically acceptable salt or a hydrate thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2, C-RAF, B-RAF, and RET) inhibitor is used for treating disorders related to tyrosine kinase. ##STR00001##

Calmodulin inhibitors for the treatment of ribosomal disorders and ribosomapathies

The present invention relates generally to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to methods for the use of calmodulin inhibitors and calcium channel blockers for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA).

Calmodulin inhibitors for the treatment of ribosomal disorders and ribosomapathies

The present invention relates generally to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to methods for the use of calmodulin inhibitors and calcium channel blockers for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA).

KDM1A inhibitors for the treatment of disease

Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.