ASCENTAGE PHARMA GROUP CORP LIMITED

The invention discloses a solid dispersion, a pharmaceutical preparation, a preparation method and an application thereof. The solid dispersion of the invention comprises carriers and active constituents, which is a compound as shown in formula (I) and/or a pharmaceutically acceptable salt thereof; The carrier is “homopolymer and copolymer of N-vinyl lactam” and/or pH-dependent cellulose derivatives. The preparation of the invention comprises the solid dispersion, fillers and disintegrating agents. The solid dispersion of the invention has good dissolution and significantly improves the solubility of effective constituents. The preparation can effectively improve the bioavailability of Bcl-2 inhibitor, has good dissolution and stability, and can improve the safety of a medication.

Methods for treating systemic lupus erythematosus using compounds or pharmaceutical compositions that modulate the activity of Bcl-2 family proteins are disclosed. In some methods, the patient to be treated is diagnosed with lupus nephritis. In some methods, the compound or pharmaceutical composition is administered to the patient in need thereof at a therapeutically effective dose sufficient to elicit one or more effects selected from: reduced excretion of protein in the urine of the patient, reduced serum anti-dsDNA autoantibody levels in the patient, reduced skin lesion severity in the patient, reduced lymphadenopathy severity in the patient, reduced glomerulonephritis severity in the patient, reduced vasculitis severity in the patient, reduced lymphocyte cell counts in a peripheral blood mononuclear cell (PMBC) panel taken from the patient, reduced lymphocyte cell counts in the spleen of the patient, and reduced lymphocyte infiltration of the kidneys of the patient.

Crystallines form or amorphous forms of bisdiazabicyclic compounds or salts thereof for the treatment and/or prevention of diseases or disorders related to hepatitis virus, and a preparation method and application thereof are provided. The crystalline forms or amorphous forms involved provide important reference value for the development and utilization of drugs in the future.

The present disclosure provides compounds having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein variables are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a disease, disorder, or condition responsive to Bcl-2 protein inhibition, particularly Bcl-2 WT and/or Bcl-2 G101V.

The present invention relates to a combination product comprising a Bcl-2/Bcl-xL inhibitor and a chemotherapeutic agent, in particular a Bcl-2/Bcl-xL inhibitor of formula I-A and homoharringtonine or an active derivative thereof, in free or pharmaceutically acceptable salt or solvate form. The invention also relates to the use of the aforementioned combination for the preparation of a medicament for the prevention and/or treatment of cancer, in particular of hematological malignancies, and to a method for the prevention and/or treatment of cancer, in particular of hematological malignancies, using the aforementioned combination.

The present disclosure relates to compounds that function as degraders or inhibitors of BTK. The present disclosure further relates to pharmaceutical compositions comprising them, and to their use in the treatment of diseases mediated by BTK, such as cancer.

The present disclosure relates to compounds that function as degraders or inhibitors of BTK. The present disclosure further relates to pharmaceutical compositions comprising them, and to their use in the treatment of diseases mediated by BTK, such as cancer.

Disclosed herein are a crystalline or amorphous form of a Bcl-2/Bcl-xL inhibitor compound or a salt thereof, and a preparation method and application thereof.

Described herein are methods of treating a cancer, for example, a hematologic malignancy or a solid tumor, in a patient in need thereof, comprising administering to the patient a Bcl-2 inhibitor in combination with a second anti-cancer agent.

The present invention provides crystalline forms or amorphous forms of N-(phenylsulfonyl) benzoamide compound or its salts or solvates used as a Bcl-2 inhibitor, and the preparation method and the application thereof.