Disclosed herein are novel carborane hydroxamic acid matrix metalloproteinase (“MMP”) inhibitors and agents bearing borane-containing moieties and methods for their use in treating or preventing a disease, such as cancer and rheumatoid arthritis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: Formula (I) wherein the substituents are as described. ##STR00001##

It discloses a proteolysis targeting chimeric molecule, a preparation method and an application thereof. The proteolysis targeting chimeric molecule provided by the disclosure can inhibit the expression of BCR-ABL and/or CRBN protein in BCR-ABL and/or CRBN positive leukemia K562 cells to varying degrees, and thus can be used to prepare drugs for treating BCR-ABL and/or CRBN positive leukemia, wherein the proteolysis targeting chimeric molecule with n=3 has excellent photo-isomerization activity, and can be used in preparation of the reagents or drugs for light-regulated degradation of BCR-ABL and/or CRBN protein. The disclosure also provides a method for synthesizing the series of proteolysis targeting chimeric molecules.

The present disclosure provides ionophore compounds, which are useful for facilitating delivery of a metal ion to a cell, tissue or organ of interest. The present disclosure provides compositions comprising the subject ionophore compounds. The present disclosure provides methods of delivering a metal ion intracellularly to a target cell. The present disclosure also provides methods of treating a condition associated with a metal deficiency in an individual.

Disclosed herein are methods of treating conditions of the eye comprising delivering an effective amount of a composition comprising tobramycin or a tobramycin derivative exhibiting similar properties complexed to an agent which facilitates improved permeation of corneal cells, retention in corneal cells, or both. In aspects, such compositions further comprise, or such methods further comprise associated administration of (e.g., as a combined product or via co-administration), one or more additional active agents capable of supporting the treatment of the indication for which the compounds of the invention are directed, such as additional antibacterial compounds, anti-inflammatory agents (e.g., steroids), and the like.

The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.

The present invention relates to compound-linker constructs and antibody-drug-conjugates of compounds of formula (I) that are useful as modulators of STING (Stimulator of Interferon Genes).

Provided herein is the conjugation of an amanita toxin compound to a cell-binding molecule with branched linkers for having better targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of an amanita molecule to a cell-binding ligand, as well as methods of using the conjugate in targets treatment of cancer, infection and autoimmune disease.

An anti-CEA antibody-exatecan analog conjugate and a pharmaceutical use thereof. Specifically, the anti-CEA antibody-exatecan analog conjugate is as shown in general formula (Pc-L-Y-D), wherein Pc is an anti-CEA antibody or an antigen-binding fragment thereof; L is a linker unit; Y is selected from —O—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O)—, —O—CR.sup.1R.sup.2—(CR.sup.aR.sup.b).sub.m—, —O—CR.sup.1R.sup.2—, —NH—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O)—, and —S—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O); and n is a decimal or integer from 1 to 10.

##STR00001##

The present invention relates to a bifunctional compound, a preparation method therefor, and a use thereof, wherein the bifunctional compound comprises an E3 ubiquitin ligase-binding moiety; a target protein-binding moiety that binds to an androgen receptor; and a linking moiety that links the E3 ubiquitin ligase-binding moiety and the target protein-binding moiety. The bifunctional compound of the present application allows the androgen receptor to be positioned adjacent to the ubiquitin ligase, so as to achieve the degradation or inhibition of the androgen receptor.

Disclosed are small molecules against cereblon to enhance effector T cell function. Methods of making these molecules and methods of using them to treat various disease states are also disclosed.