A61K31/337

THIOCARBAMATE DERIVATIVES AS A2A INHIBITORS, PHARMACEUTICAL COMPOSITION THEREOF AND COMBINATIONS WITH ANTICANCER AGENTS

The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors

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Especially, the present invention relates to a pharmaceutical composition comprising an A2A inhibitor of Formula (I) and a lipid carrier such as lauroyl macrogol-32 glycerides, D-α-tocopherol-polyethylene glycol-1000 succinate or a mixture thereof. The pharmaceutical composition of the invention is particularly useful for oral dosing in the treatment of cancers.

The present invention also relates to a combination comprising an A2A receptor inhibitor of Formula (I) and an anticancer agent. The anticancer agent is for example an immunotherapeutic agent, such as a checkpoint inhibitor. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination. Additionally, the combination of the invention is particularly useful for the treatment and/or prevention of cancers.

THIOCARBAMATE DERIVATIVES AS A2A INHIBITORS, PHARMACEUTICAL COMPOSITION THEREOF AND COMBINATIONS WITH ANTICANCER AGENTS

The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors

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Especially, the present invention relates to a pharmaceutical composition comprising an A2A inhibitor of Formula (I) and a lipid carrier such as lauroyl macrogol-32 glycerides, D-α-tocopherol-polyethylene glycol-1000 succinate or a mixture thereof. The pharmaceutical composition of the invention is particularly useful for oral dosing in the treatment of cancers.

The present invention also relates to a combination comprising an A2A receptor inhibitor of Formula (I) and an anticancer agent. The anticancer agent is for example an immunotherapeutic agent, such as a checkpoint inhibitor. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination. Additionally, the combination of the invention is particularly useful for the treatment and/or prevention of cancers.

COMPOSITIONS AND FORMULATIONS INCLUDING CABAZITAXEL AND HUMAN SERUM ALBUMIN
20230068363 · 2023-03-02 ·

This document relates to non-covalently bound complexes comprising cabazitaxel and human serum albumin. This document also relates to compositions comprising non-covalently bound complexes comprising cabazitaxel and human serum albumin. This document also relates to compositions comprising cabazitaxel and human serum albumin. This document also relates to compositions consisting essentially of cabazitaxel and human serum albumin.

COMPOSITIONS AND FORMULATIONS INCLUDING CABAZITAXEL AND HUMAN SERUM ALBUMIN
20230068363 · 2023-03-02 ·

This document relates to non-covalently bound complexes comprising cabazitaxel and human serum albumin. This document also relates to compositions comprising non-covalently bound complexes comprising cabazitaxel and human serum albumin. This document also relates to compositions comprising cabazitaxel and human serum albumin. This document also relates to compositions consisting essentially of cabazitaxel and human serum albumin.

RORgT INHIBITOR, PREPARATION METHOD THEREOF AND USE THEREOF

A RORγt inhibitor as well as a preparation method thereof and uses thereof, and a pharmaceutical composition including the compound, a method for preparing the pharmaceutical composition, and use of the compound or the pharmaceutical composition in the treatment or prevention of RORγt-mediated cancer, inflammation, or autoimmune diseases in mammals, especially humans.

RORgT INHIBITOR, PREPARATION METHOD THEREOF AND USE THEREOF

A RORγt inhibitor as well as a preparation method thereof and uses thereof, and a pharmaceutical composition including the compound, a method for preparing the pharmaceutical composition, and use of the compound or the pharmaceutical composition in the treatment or prevention of RORγt-mediated cancer, inflammation, or autoimmune diseases in mammals, especially humans.

AMPHIPHILIC ALGINATE-OLEIC ACID MACROMOLECULES AND PROCESS FOR PREPARATION THEREOF
20230122200 · 2023-04-20 · ·

The present invention provides a new type of hydrophobically -modified sodium alginate, which is synthesized by alginate and oleic acid linked with a spacer. The AGO macromolecule as obtained therefrom is amphiphilic and has clinically-accessible molecular size, and anti- cancer activity. The AGO nanoparticle formed therefrom shows excellent structural stability, colloidal stability, and biocompatibility in-vitro and in-vivo, and is expected to be useful in biomedical area, for example, used as a drug delivery system.

AMPHIPHILIC ALGINATE-OLEIC ACID MACROMOLECULES AND PROCESS FOR PREPARATION THEREOF
20230122200 · 2023-04-20 · ·

The present invention provides a new type of hydrophobically -modified sodium alginate, which is synthesized by alginate and oleic acid linked with a spacer. The AGO macromolecule as obtained therefrom is amphiphilic and has clinically-accessible molecular size, and anti- cancer activity. The AGO nanoparticle formed therefrom shows excellent structural stability, colloidal stability, and biocompatibility in-vitro and in-vivo, and is expected to be useful in biomedical area, for example, used as a drug delivery system.

PHARMACEUTICAL COMPOSITION COMPRISING PROTEIN KINASE INHIBITOR AND CHEMOTHERAPEUTIC DRUG AND USE THEREOF

The present invention relates to the field of biotechnology, and in particular relates to a pharmaceutical composition comprising a protein kinase inhibitor and a chemotherapeutic drug and use thereof. It is found that in the treatment of platinum-refractory/drug-resistant relapsed advanced ovarian cancer, the remission rates of etoposide or paclitaxel in combination with chiauranib is respectively 40% and 50%, while the remission rate of etoposide alone is about 27%, and the remission rate of paclitaxel alone is about 21%, indicating that the combination of chiauranib and etoposide or paclitaxel in the treatment of platinum-refractory/drug-resistant relapsed advanced ovarian cancer has achieved unexpected synergistic effects.

PHARMACEUTICAL COMPOSITION COMPRISING PROTEIN KINASE INHIBITOR AND CHEMOTHERAPEUTIC DRUG AND USE THEREOF

The present invention relates to the field of biotechnology, and in particular relates to a pharmaceutical composition comprising a protein kinase inhibitor and a chemotherapeutic drug and use thereof. It is found that in the treatment of platinum-refractory/drug-resistant relapsed advanced ovarian cancer, the remission rates of etoposide or paclitaxel in combination with chiauranib is respectively 40% and 50%, while the remission rate of etoposide alone is about 27%, and the remission rate of paclitaxel alone is about 21%, indicating that the combination of chiauranib and etoposide or paclitaxel in the treatment of platinum-refractory/drug-resistant relapsed advanced ovarian cancer has achieved unexpected synergistic effects.