A61K31/513

Formulations

The present invention relates to formulations comprising dolutegravir or a pharmaceutically acceptable salt thereof, abacavir or a pharmaceutically acceptable salt thereof and lamivudine, processes for making such formulations, and the use of such formulations in the treatment of HIV infection, in particular in the treatment of HIV infection in pediatric patients.

DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
20230002316 · 2023-01-05 · ·

The present invention concerns a compound of following formula (I): where: —R.sub.1 is H or OH, —R.sub.2 is a (C.sub.1-C.sub.6)alkyl, COOH, COO—((C.sub.1-C.sub.6)alkyl) or thiazolyl group, —R.sub.3 is H or a (C.sub.1-C.sub.6)alkyl group, and —R.sub.4 is: .square-solid.a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR.sub.5R.sub.6, .square-solid.—(CH.sub.2CH.sub.2X.sub.1)(CH.sub.2CH.sub.2X.sub.2).sub.a2(CH.sub.2CH.sub.2X.sub.3).sub.a3(CH.sub.2CH.sub.2X.sub.4).sub.a4(CH.sub.2CH.sub.2X.sub.5).sub.a5R.sub.7, .square-solid.an aryl-(C.sub.1-C.sub.8)alkyl group substituted by one or more groups chosen from among OH and NR.sub.9R.sub.10 groups, or .square-solid.a heterocycle-(C.sub.1-C.sub.8)alkyl group optionally substituted by one or more groups chosen from among (C.sub.1-C.sub.6)alkyl, OH and NR.sub.12R.sub.13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

##STR00001##

DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
20230002316 · 2023-01-05 · ·

The present invention concerns a compound of following formula (I): where: —R.sub.1 is H or OH, —R.sub.2 is a (C.sub.1-C.sub.6)alkyl, COOH, COO—((C.sub.1-C.sub.6)alkyl) or thiazolyl group, —R.sub.3 is H or a (C.sub.1-C.sub.6)alkyl group, and —R.sub.4 is: .square-solid.a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR.sub.5R.sub.6, .square-solid.—(CH.sub.2CH.sub.2X.sub.1)(CH.sub.2CH.sub.2X.sub.2).sub.a2(CH.sub.2CH.sub.2X.sub.3).sub.a3(CH.sub.2CH.sub.2X.sub.4).sub.a4(CH.sub.2CH.sub.2X.sub.5).sub.a5R.sub.7, .square-solid.an aryl-(C.sub.1-C.sub.8)alkyl group substituted by one or more groups chosen from among OH and NR.sub.9R.sub.10 groups, or .square-solid.a heterocycle-(C.sub.1-C.sub.8)alkyl group optionally substituted by one or more groups chosen from among (C.sub.1-C.sub.6)alkyl, OH and NR.sub.12R.sub.13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

##STR00001##

DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
20230002316 · 2023-01-05 · ·

The present invention concerns a compound of following formula (I): where: —R.sub.1 is H or OH, —R.sub.2 is a (C.sub.1-C.sub.6)alkyl, COOH, COO—((C.sub.1-C.sub.6)alkyl) or thiazolyl group, —R.sub.3 is H or a (C.sub.1-C.sub.6)alkyl group, and —R.sub.4 is: .square-solid.a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR.sub.5R.sub.6, .square-solid.—(CH.sub.2CH.sub.2X.sub.1)(CH.sub.2CH.sub.2X.sub.2).sub.a2(CH.sub.2CH.sub.2X.sub.3).sub.a3(CH.sub.2CH.sub.2X.sub.4).sub.a4(CH.sub.2CH.sub.2X.sub.5).sub.a5R.sub.7, .square-solid.an aryl-(C.sub.1-C.sub.8)alkyl group substituted by one or more groups chosen from among OH and NR.sub.9R.sub.10 groups, or .square-solid.a heterocycle-(C.sub.1-C.sub.8)alkyl group optionally substituted by one or more groups chosen from among (C.sub.1-C.sub.6)alkyl, OH and NR.sub.12R.sub.13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

##STR00001##

ECLITASERTIB FOR USE IN TREATING CONDITIONS INVOLVING SYSTEMIC HYPERINFLAMMATORY RESPONSE

This disclosure relates to the field of therapeutic protein kinase inhibitors, in particular receptor-interacting protein kinase 1 (“RIPK1”) inhibitor for treatment of subjects with conditions involving systemic hyperinflammatory responses, such as Cytokine Release Syndrome (CRS), or Systemic Inflammatory Response Syndrome (SIRS), sepsis, organ damage, or hyperinflammatory state associated with infectious diseases.

ECLITASERTIB FOR USE IN TREATING CONDITIONS INVOLVING SYSTEMIC HYPERINFLAMMATORY RESPONSE

This disclosure relates to the field of therapeutic protein kinase inhibitors, in particular receptor-interacting protein kinase 1 (“RIPK1”) inhibitor for treatment of subjects with conditions involving systemic hyperinflammatory responses, such as Cytokine Release Syndrome (CRS), or Systemic Inflammatory Response Syndrome (SIRS), sepsis, organ damage, or hyperinflammatory state associated with infectious diseases.

Glycan-Interacting Compounds and Methods of Use

Methods of treating cancer are provided that include administering glycan-interacting antibodies. Included are anti-sialyl Tn antigen antibodies and related compositions and formulations suitable to achieve desirable bioactivity, bioavailability, and toxicity levels.

Glycan-Interacting Compounds and Methods of Use

Methods of treating cancer are provided that include administering glycan-interacting antibodies. Included are anti-sialyl Tn antigen antibodies and related compositions and formulations suitable to achieve desirable bioactivity, bioavailability, and toxicity levels.

COMPOUND FOR TARGETING AND DEGRADING PROTEIN, AND PREPARATION METHOD THEREFOR AND USE THEREOF
20230234936 · 2023-07-27 ·

A class of bifunctional compounds for targeting and degrading an IRAK4 kinase protein, a pharmaceutical composition and a preparation method therefor are provided. The compounds not only effectively inhibits and/or degrades the IRAK4 kinase protein in cells, but also effectively inhibit the production of IL-6 by immune cells, and has good degradation selectivity. The compounds can be used in the preparation of a drug for treating and/or preventing IRAK4-mediated related diseases or conditions, such as cancer, immunological diseases and inflammatory diseases.

METHODS AND COMPOSITIONS PRODUCED THEREBY

The invention relates to a method of enhancing the solubility and/or the rate of dissolution of a Class II or Class IV low solubility molecule, a method of producing a spray-dried composition, and a spray-dried composition comprising a Class II or Class IV low solubility molecule, albumin and an agent that prevents self-aggregation of albumin.