C07J19/00

Compounds for treating neurodegenerative disorders

The invention relates to compounds of formula (I), their method of synthesis as well as their use to treat neurodegenerative disorders. ##STR00001##

Compounds for treating neurodegenerative disorders

The invention relates to compounds of formula (I), their method of synthesis as well as their use to treat neurodegenerative disorders. ##STR00001##

INHIBITION OF INTERACTION BETWEEN OCT4 AND MAPKAPK2 OR DNA-PKCS TO REGULATE C-MYC IN CANCER

Embodiments of the present disclosure pertain to methods of treating a cancer in a subject by administering to the subject a compound that inhibits interaction between octamer-binding transcription factor 4 (OCT4) and Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2), OCT4 and DNA-dependent protein kinase catalytic subunit (DNA-PKcs), or combinations thereof. Additional embodiments of the present disclosure pertain to the compounds of the present disclosure. Further embodiments of the present disclosure pertain to methods of inhibiting interaction between OCT4 and MAPKAPK2 and/or OCT4 and DNA-PKcs by exposing protein complexes to the compounds of the present disclosure. Additional embodiments of the present disclosure pertain to methods of screening potential inhibitors of protein-protein interaction between a first protein and a second protein.

17beta-heterocyclyl-digitalis like compounds for the treatment of heart failure

Disclosed are compounds of formula (I), wherein X, Y, Z are annular atoms comprised in a five-membered carbocyclic or heterocyclic ring, selected from the group consisting of CH, NH, N, O, S; said carbocyclic or heterocyclic ring being optionally substituted with amino (C.sub.1-C.sub.4) linear or branched alkyl or guanidine or guanidino (C.sub.1-C.sub.4) linear or branched alkyl; with the proviso that the heterocycle ring is not furyl; n is 0 or 1; R is H or OH; the dotted line represents an optional double bond C═C; the thick line represents a bond in the β configuration; the wavy line represents a bond both in the α and β configuration; their enantiomeric and/or diastereomeric mixtures, their pharmaceutically acceptable salts, their solvates, hydrates; their metabolite and metabolic precursors. The compounds of formula (I) are for use as medicaments, in particular for the treatment of acute or chronic heart failure. Oral administration is also possible.

Certain chemical entities, compositions, and methods
11325940 · 2022-05-10 · ·

Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

Certain chemical entities, compositions, and methods
11325940 · 2022-05-10 · ·

Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

17BETA-HETEROCYCLYL-DIGITALIS LIKE COMPOUNDS FOR THE TREATMENT OF HEART FAILURE

Disclosed are compounds of formula (I), wherein X, Y, Z are annular atoms comprised in a five-membered carbocyclic or heterocyclic ring, selected from the group consisting of CH, NH, N, O, S; said carbocyclic or heterocyclic ring being optionally substituted with amino (C.sub.1-C.sub.4) linear or branched alkyl or guanidine or guanidino (C.sub.1-C.sub.4) linear or branched alkyl; with the proviso that the heterocycle ring is not furyl; n is 0 or 1; R is H or OH; the dotted line represents an optional double bond C═C; the thick line represents a bond in the β configuration; the wavy line represents a bond both in the α and β configuration; their enantiomeric and/or diastereomeric mixtures, their pharmaceutically acceptable salts, their solvates, hydrates; their metabolite and metabolic precursors. The compounds of formula (I) are for use as medicaments, in particular for the treatment of acute or chronic heart failure. Oral administration is also possible.

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Crystal characteristics, preparation processes and anticancer applications of 17beta-neriifolin crystal forms

The present invention provides the preparation processes for several crystal forms of the compound 17beta-Neriifolin (17bNF) and use thereof in anti-tumor applications. The present invention provides preparation processes for four kinds of non-solvated crystal forms, amorphous powders and eleven kinds of solvated crystalline solids, including ethanol-solvated ones, of 17bNF that are not present in nature, and the identification and characterization of these crystal forms by crystallographic research methods such as X-ray powder diffraction. In addition, through vivo anti-tumor experiments with five of the crystal forms in nude mice, we provide anti-tumor and anti-cancer applications of the crystal forms of 17bNF.

COMPOUNDS FOR TREATING NEURODEGENERATIVE DISORDERS

The invention relates to compounds of formula (I), their method of synthesis as well as their use to treat neurodegenerative disorders.

##STR00001##

Steroid saponins with anti-cancer activity
10925887 · 2021-02-23 ·

The present invention relates to a new class of steroid saponins that have interesting biological activity. In particular the present invention relates to a class of steroid saponins in which the sugar moiety has been selectively functionalised to introduce a moiety that contains either, (i) a hydrogen ion donor, (ii) a hydrogen ion acceptor or (iii) a combination thereof. These new, water-soluble compounds are found to not only have potent anti-cancer properties per se but also have the ability to promote the immune response in a subject and can thus act as adjuvants for T-cell activation in cancer therapy.