Patent classifications
C07D233/96
Adenosine monophosphate-activated protein kinase agonist
The present invention discloses a compound of the formula (I), which acts as an agonist of adenosine monophosphate-activated protein kinase, which induce phosphorylation and activation of AMPK, thereby further regulating downstream signaling pathways, inhibiting growth and proliferation of liver cancer cells and breast cancer cells, and also inducing apoptosis of adipocytes. Therefore, the compound provided by the present invention can be utilised for treatment and preparation of pharmaceutical composition for cancer, and lipid metabolism-related diseases or syndromes mediated by AMPK. ##STR00001##
Adenosine monophosphate-activated protein kinase agonist
The present invention discloses a compound of the formula (I), which acts as an agonist of adenosine monophosphate-activated protein kinase, which induce phosphorylation and activation of AMPK, thereby further regulating downstream signaling pathways, inhibiting growth and proliferation of liver cancer cells and breast cancer cells, and also inducing apoptosis of adipocytes. Therefore, the compound provided by the present invention can be utilised for treatment and preparation of pharmaceutical composition for cancer, and lipid metabolism-related diseases or syndromes mediated by AMPK. ##STR00001##
FLUORESCENT PROBE, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a fluorescent probe, a preparation method therefor and a use thereof. The fluorescent probe responds to viscosity sensitively and specifically, can be used for the specific fluorescence labeling of proteins and can also be used in the quantification, detection or kinetic study of proteins and the imaging of cells, tissues and living bodies.
FLUORESCENT PROBE, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a fluorescent probe, a preparation method therefor and a use thereof. The fluorescent probe responds to viscosity sensitively and specifically, can be used for the specific fluorescence labeling of proteins and can also be used in the quantification, detection or kinetic study of proteins and the imaging of cells, tissues and living bodies.
INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
The present disclosure discloses compounds capable of modulating the activity of -amino--carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
The present disclosure discloses compounds capable of modulating the activity of -amino--carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
FERROPORTIN INHIBITORS AND METHODS OF USE
The subject matter described herein is directed to Ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis.
FERROPORTIN INHIBITORS AND METHODS OF USE
The subject matter described herein is directed to Ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis.
CHEMICAL COMPOUNDS
The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers.
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USP30 INHIBITORS
The application relates to phenyl- or naphthylsulfonamide derivatives of the structural formula (I). The compounds are described as inhibitors of USP30 (ubiquitin specific peptidase 30) useful for the treatment of conditions involving mitochondrial defects including neurodegenerative diseases such as Alzheimer's and Parkinson's or a neoplastic disease such as leukemia.
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