A61K47/548

Osteoadsorptive fluorogenic substrate of cathepsin k for imaging osteoclast activity and migration

In certain embodiments osteoadsorptive fluorogenic substrates of cathepsin K (or other proteases) are provided. Utilizing a bisphosphonate targeting moiety, the fluorogenic substrates provide effective bone-targeted protease sensor(s). In certain embodiments the “probes” comprise cleavable fluorophore-quencher pair linked by a cathepsin K (or other protease) peptide substrate and tethered to a bisphosphonate. Unlike existing probes that are cleared within a few days in vivo, the probes described herein (e.g., OFS-1) allow for monitoring resorption over the course of longer time periods with a single dose.

PRODRUG OF ITRACONAZOLE AND USES THEREOF
20210346506 · 2021-11-11 ·

The present invention relates to itraconazole prodrugs, pharmaceutical compositions comprising the prodrugs, and methods for treatment and/or prophylaxis of lung fibrosis, renal fibrosis, or liver fibrosis using the pharmaceutical compositions.

OLIGONUCLEOTIDE INHIBITORS OF NUCLEAR FACTOR KAPPA-LIGHT-CHAIN-ENHANCER OF ACTIVATED B CELLS AND THE USES THEREOF
20220002730 · 2022-01-06 ·

Disclosed herein, inter alia, are oligonucleotide inhibitors of the Nuclear Factor Kappa-Light-Chain-Enhancer of Activated B Cells (NF-κB) signaling pathway and methods of use thereof.

Compositions and Methods for use of CXCL12 in Treatment of Bone Disorders
20220000980 · 2022-01-06 ·

The present invention provides compositions and methods for treating a disease or disorder associated with bone defects or reduced or abnormal bone formation.

PSMA BINDING LIGAND-LINKER CONJUGATES AND METHODS FOR USING
20210338641 · 2021-11-04 ·

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

CANCER CELL MODULATORS
20230321250 · 2023-10-12 ·

Disclosed are cancer cell- and proliferative cell-selective small molecule compounds that modulate certain cancer cell- or proliferative cell-specific metabolic enzymes or receptors, and methods of their use to treat cancer and other proliferative disorders.

CD47 BINDER AND LIPOSOME COMPLEX FOR CANCER TREATMENT

There is provided a binder, which binds to CD47 overexpressed in cancer cells and has an improved binding affinity for CD47, and a liposome complex. There is also provided a binder, which binds to CD47 overexpressed in cancer cells and includes an amino acid sequence represented by SEQ ID NO: 1 or SEQ ID NO: 2, and a binder-conjugated liposome complex, in which the binder is conjugated to a liposome.

Antimitoscins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells

Antibiotics having intrinsic anti-mitochondrial properties may be chemically modified to target the antibiotics to mitochondria, and the resulting “antimitoscins” may have enhanced anti-cancer properties, among other advantageous properties. Also described are methods for identifying antimitoscins, methods of using antimitoscins to target cancer stem cells, and pharmaceutical compositions for treating cancer containing one or more antimitoscins as the active ingredient. Specific antimitoscins compounds and groups of antimitoscins are also disclosed.

MUSCLE TARGETING COMPLEXES AND FORMULATIONS FOR TREATING MYOTONIC DYSTROPHY

Aspects of the disclosure relate to complexes and other aspects relate to formulations (e.g., aqueous, lyophilized forms) comprising such complexes comprising an oligonucleotide (e.g., useful for targeting DMPK) covalently linked to an antibody (e.g., anti-TfR1 antibody).

SELF-PRESERVING TOPICAL PHARMACEUTICAL COMPOSITIONS COMPRISING DIETHYLENE GLYCOL MONOETHYL ETHER

Topical pharmaceutical compositions comprising diethylene glycol monoethyl ether (DEGEE) maintained at an acidic pH. The pH of the formulation can be maintained at a pH of less than 6.3, or alternatively less than 6.0. Certain pharmaceutical composition further comprise an emulsifier blend of cetearyl alcohol, dicetyl phosphate, and ceteth-10 phosphate, which is manufactured by Croda under the tradename Crodafos™ CES.