A61K47/548

Phthalocyanine dye compounds, conjugates and methods of use thereof

Disclosed herein are phthalocyanine dyes, and conjugates thereof, useful as fluorescent reporters for bioassays, for optical imaging and as therapeutic conjugates as the photosensitizing agents in light-based therapies including photoimmuno therapy (PIT). Certain phthalocyanine dyes disclosed herein are water soluble, and possess photophysical and photochemical profiles useful for use in imaging or therapy.

Phosphorylcholine conjugates and uses thereof
11458186 · 2022-10-04 · ·

The present invention provides phosphorylcholine conjugates and pharmaceutical compositions comprising same for the prevention or treatment of autoimmune diseases. In particular, the conjugates of the present invention are effective in treating autoimmune diseases associated with pathological inflammation.

Phospholipid ether analogs as cancer-targeting drug vehicles

The present invention is directed to therapeutic compounds capable of targeting cancer cells and cancer stem cells. The present invention is further directed to compositions comprising these therapeutic compounds and methods of treating cancer comprising administering these therapeutic compounds.

FLAVONOID DERIVATIVE FOR TREATING DENTAL CARIES
20220281903 · 2022-09-08 ·

The invention relates to a flavonoid derivative containing a flavonoid that is coupled to an alkylene group via an ether bond, said alkylene group having an adhesion group for adhesion onto a dental surface. The flavonoid derivative has a long-term suppressing effect on the dental disease-causing formation of biofilm on the dental surfaces treated with the flavonoid derivative. The invention further relates to a kit for producing such a flavonoid derivative, and to the use of same.

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CONJUGATES AND CONJUGATES FOR USE IN PREVENTING OR TREATING OF BRAIN DAMAGE AND NEURODEGENERATIVE DISEASES
20220296722 · 2022-09-22 ·

Disclosed are conjugates including one or more compounds selected from of (i) an anti-inflammatory compound, and/or (ii) an antioxidant compound, and/or (iii) and antibiotic compound and/or, (iv) a metal chelating compound and at least one of (v) a blood-brain barrier compound and (vi) solubility enhancer moiety. The compounds of group (i)-(v) and the solubility enhancer moiety (vi), when present, are covalently bound together with one or more linkers. The blood-brain barrier targeting compound is monosaccharide and the solubility enhancer moiety is a phosphate group. Also disclosed are pharmaceutical compositions including such conjugates and uses of these conjugates and compositions for treating and/or prevention of neuro-degenerative diseases and brain damage due to traumatic and/or acquired brain injury.

A PRODRUG PLATFORM USEFUL TO DELIVER AMINES, AMIDES AND PHENOLS
20220281904 · 2022-09-08 ·

A prodrug platform is useful to deliver pharmaceutically active amines, amides and phenols and their use in the diagnosis, prevention and/or treatment of various diseases. Compared with the parent drug (e.g., Gemcitabine), the prodrugs show a significant overall safety improvement (therapeutic index (TI) improvement), especially in liver. The prodrugs can treat several diseases, including, for example, cancer, metabolic disease, viral infection, immunological disease, neurologic disease, and blood disease.

ALK PROTEIN REGULATOR AND ANTI-TUMOR APPLICATION THEREOF

A compound of general formula (I), a compound of general formula (III) and anti-tumor applications thereof. A series of compounds designed and synthesized have a wide range of pharmacological activities, have the function of degrading specific proteins and/or inhibiting activity, and can be used in related tumor and cancer treatments.

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BONE-BINDING COMPOUNDS

Disclosed herein are compounds having the following Formula (I) or a pharmaceutically acceptable salt form thereof: B-L-C (I) wherein B is a bone-binding moiety; L is a linker; and C is a cationic steroid antimicrobial (CSA) moiety, pharmaceutical compositions comprising the compounds, and methods of using the compounds or pharmaceutical compositions for the treatment of an infection or osteomyelitis in a bone of a subject, promotion of bone formation in a subject, or treatment of bone cancer or metastatic bone cancer in a subject.

PSMA binding ligand-linker conjugates and methods for using

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.

Phosphonate-Drug Conjugates

This invention relates to drug conjugates useful for localized treatment of diseases or disorders of the middle ear and/or inner ear. Methods of treating diseases or disorders of the middle ear and/or inner ear, pharmaceutical compositions comprising the conjugates, and methods of inhibiting a Tropomyosin receptor kinase are also provided.