A61K31/4523

Anticancer treatment for uveal melanoma

Provided herein are methods for treating uveal melanoma in a subject in need thereof by administering an effective amount of an agent that inhibits expression of FAK protein to the subject. In one aspect, the agent that inhibits expression of FAK protein comprises, or alternatively consists essentially of, or yet further consists of a gene editing agent, such as for example one or more of: RNA interference (RNAi), CRISPR/Cas, ZFN, and/or TALEN. In another aspect, the agent is VS-4718. Also described herein are kits comprising, or alternatively consisting essentially of, or yet further consisting of one or more of: agents that inhibit expression of FAK protein, siRNAs, shRNAs, miRNAs, nucleases and/or guide RNA sequences for carrying out the methods of this disclosure, and optional instructions for use.

Compounds for inhibiting cell proliferation in EGFR-driven cancers

The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: ##STR00001##
wherein the variables are as defined herein.

Compounds for inhibiting cell proliferation in EGFR-driven cancers

The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: ##STR00001##
wherein the variables are as defined herein.

Compounds for inhibiting cell proliferation in EGFR-driven cancers

The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula I: ##STR00001##
wherein the variables are as defined herein.

Phenyl derivative

The compound of the formula (I-1): ##STR00001##
wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P.sub.2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P.sub.2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

Phenyl derivative

The compound of the formula (I-1): ##STR00001##
wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P.sub.2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P.sub.2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND MEK INHIBITOR

Provided is a novel combination therapy that exhibits excellent antitumor effects, and that uses an FGFR-inhibiting compound and an MEK inhibitor. An antitumor agent contains (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient and is administered in combination with an MEK inhibitor.

CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND MEK INHIBITOR

Provided is a novel combination therapy that exhibits excellent antitumor effects, and that uses an FGFR-inhibiting compound and an MEK inhibitor. An antitumor agent contains (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient and is administered in combination with an MEK inhibitor.

CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND MEK INHIBITOR

Provided is a novel combination therapy that exhibits excellent antitumor effects, and that uses an FGFR-inhibiting compound and an MEK inhibitor. An antitumor agent contains (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient and is administered in combination with an MEK inhibitor.

METHODS OF TREATING METABOLIC DISEASES WITH FUSED BICYCLIC PYRAZOLES
20220354844 · 2022-11-10 ·

Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for the treatment of retinal binding protein (RBP4) related diseases, such as obesity and the like.