A61K38/07

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.

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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.

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SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME

Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.

SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME

Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.

OLIGONUCLEOTIDE CONJUGATES AND PREPARATION AND APPLICATIONS THEREOF

The present invention relates to oligonucleotide conjugates and preparation and applications thereof. In particular, the present invention relates to an oligonucleotide conjugated to a biomolecule (e.g. an antibody) and/or an agent of interest (e.g. a drug). In certain embodiments, the oligonucleotide of the present invention is a hybridized complex of a single strand oligonucleotide carrying a biomolecule and a complementary strand oligonucleotide bearing an agent of interest where the hybridized nucleotide segment acts as a linker to link the biomolecule and the agent of interest in one molecule.

TREATMENT OF CANCERS WITH ANTIBODY DRUG CONJUGATES (ADC) THAT BIND TO 191P4D12 PROTEINS
20230001005 · 2023-01-05 · ·

Provided herein are methods for the treatment of cancers with antibody drug conjugates (ADC) that bind to 191P4D12 proteins.

TREATMENT OF CANCERS WITH ANTIBODY DRUG CONJUGATES (ADC) THAT BIND TO 191P4D12 PROTEINS
20230001005 · 2023-01-05 · ·

Provided herein are methods for the treatment of cancers with antibody drug conjugates (ADC) that bind to 191P4D12 proteins.

Therapy for the Treatment of Cancer

Provided herein are methods of treating and/or managing cancer, which comprise administering to a patient Compound A, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof. Additionally, provided herein are methods of treating and/or managing cancer, which comprise administering to a patient Compound A, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof, in combination with a second agent selected from the group consisting of an anti-CD20 antibody, an HDAC inhibitor, a proteasome inhibitor, an anti-CD38 antibody, an anti-SLAMF7 antibody, a nuclear export inhibitor, a BCL-2 inhibitor, and an immune checkpoint inhibitor. Also provided herein are combination therapies for treating and/or managing cancer, which further comprise dexamethasone as a third agent.

Therapy for the Treatment of Cancer

Provided herein are methods of treating and/or managing cancer, which comprise administering to a patient Compound A, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof. Additionally, provided herein are methods of treating and/or managing cancer, which comprise administering to a patient Compound A, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof, in combination with a second agent selected from the group consisting of an anti-CD20 antibody, an HDAC inhibitor, a proteasome inhibitor, an anti-CD38 antibody, an anti-SLAMF7 antibody, a nuclear export inhibitor, a BCL-2 inhibitor, and an immune checkpoint inhibitor. Also provided herein are combination therapies for treating and/or managing cancer, which further comprise dexamethasone as a third agent.

PROBIOTIC BACTERIAL MOLECULES AND THEIR USE IN METHODS TO TREAT/PREVENT INFECTION BY HARMFUL BACTERIA AND TO PROVIDE NUTRITIONAL HEALTH

This invention provides isolated and characterized secreted molecules from probiotic bacteria for use in compositions and methods for the treatment and/or prevention of infection by harmful pathogenic bacteria. The isolated secreted molecules can also be used in nutritional or medical food products which provide probiotics to the gastrointestinal tract of a mammal.