C07D207/456

Type III deiodinase inhibitors and uses thereof

The present invention relates to compounds that inhibit the activity of Type III deiodinase (DIO3). The present invention further relates to methods for treating or preventing depression, depression associated with other psychiatric or general medical diseases or conditions, condition amenable to treatment with known anti-depressants and cancer, particularly by using the compounds of the invention.

INHIBITORS OF IRES-MEDIATED PROTEIN SYNTHESIS

This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.

INHIBITORS OF IRES-MEDIATED PROTEIN SYNTHESIS

This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.

Curable compound

There is provided a curable compound having good solvent solubility and being capable of forming a cured material having super heat resistance. The curable compound according to the present invention is represented by the following formula (1). In the formula (1), R.sup.1 and R.sup.2 each represent a curable functional group; D.sup.1 and D.sup.2 each represent a single bond or a linking group; and L represents a divalent group having a repeating unit containing a structure represented by the following formula (I) and a structure represented by the following formula (II) (wherein Ar.sup.1 to Ar.sup.3 each represent a group made by eliminating two hydrogen atoms from a structural formula of an aromatic ring or a group made by eliminating two hydrogen atoms from a structural formula in which two or more aromatic rings are bound through a single bond or a linking group; X represents —CO—, —S— or —SO.sub.2—; each Y represents —S—, —SO.sub.2—, —O—, —CO—, —COO— or —CONH—; and n represents an integer of 0 or more): ##STR00001##

Di-substituted maleic amide linker for antibody drug conjugating and preparation method and use thereof

Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.

Di-substituted maleic amide linker for antibody drug conjugating and preparation method and use thereof

Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.

Methods and compositions involving RAD51 inhibitors

The present invention concerns methods and compositions involving inhibitors and of RAD51, a protein involved in homologous recombination. In some embodiments, there are methods for sensitizing cells to the effects of DNA damaging agents, which can have particular applications for cancer patients. In some embodiments of the invention, the RAD51 inhibitor is a small molecule that directly affects RAD51 activity, such as its ability to promote filament formation.

Methods and compositions involving RAD51 inhibitors

The present invention concerns methods and compositions involving inhibitors and of RAD51, a protein involved in homologous recombination. In some embodiments, there are methods for sensitizing cells to the effects of DNA damaging agents, which can have particular applications for cancer patients. In some embodiments of the invention, the RAD51 inhibitor is a small molecule that directly affects RAD51 activity, such as its ability to promote filament formation.

AMINOBENZOIC ACID DERIVATIVES FOR USE AS ANTI-INFLAMMATORY AGENTS, ANTI-METASTATIC AGENTS AND/OR ANTICANCER AGENTS
20210002222 · 2021-01-07 · ·

There are provided compounds of formula (I)

##STR00001##

in which R.sub.2, R.sub.2, R.sub.3, R.sub.4 and Q can represent various different possibilities. These compounds can be useful as anticancer agents as well as anti-inflammatory agents, anti-proliferative agents and/or anti-metastatic agents.

AMINOBENZOIC ACID DERIVATIVES FOR USE AS ANTI-INFLAMMATORY AGENTS, ANTI-METASTATIC AGENTS AND/OR ANTICANCER AGENTS
20210002222 · 2021-01-07 · ·

There are provided compounds of formula (I)

##STR00001##

in which R.sub.2, R.sub.2, R.sub.3, R.sub.4 and Q can represent various different possibilities. These compounds can be useful as anticancer agents as well as anti-inflammatory agents, anti-proliferative agents and/or anti-metastatic agents.