# US 10,478,492 B2 · Modifications of therapeutic agents for enhanced delivery to target sites

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- Number: US 10,478,492 B2
- Document ID: US10478492B2
- Status: Granted
- Kind: B2
- Application number: 15/660,256
- Filed: 2017-07-26
- Published: 2018-02-01
- Granted: 2019-11-19
- Earliest claimed: 2016-07-27
- Assignees: Claria Partikula LLC
- Applicants: Partikula LLC
- Inventors: David Kolb; Petr Ledin; Tsukasa Mizuhara
- Web page: https://patentgrep.com/patent/US10478492B2

## CPC

- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- A61K 9/5146: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides}
- A61K 47/54: the modifying agent being an organic compound
- A61K 47/541: {Organic ions forming an ion pair complex with the pharmacologically or therapeutically active agent}
- A61K 47/542: {Carboxylic acids, e.g. a fatty acid or an amino acid}
- A61K 47/555: {pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells}
- A61K 47/66: the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
- A61K 47/6801: {Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent}
- A61K 47/6809: {Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin}
- A61K 47/6843: {the antibody targeting a material from animals or humans}
- A61K 47/6851: {the antibody targeting a determinant of a tumour cell}
- A61K 47/6871: {the antibody targeting an enzyme}
- A61K 47/6889: {Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment}
- A61K 47/6927: {the form being a solid microparticle having no hollow or gas-filled cores}
- A61K 47/6929: {the form being a nanoparticle, e.g. an immuno-nanoparticle}
- A61K 2039/585: {wherein the target is cancer}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Compositions of a modulator of cell metabolism, typically targeting cellular glycolysis, preferably with a targeting moiety, attached directly or indirectly to the inhibitor, or to a nanoparticle or other delivery vehicle thereof, and methods of use for treating cancer, proliferative disorders, neurodegenerative diseases, autoimmune disorders, or inflammatory diseases are provided. Pharmaceutical compositions including the targeted modulator and a pharmaceutically acceptable carrier are also provided. The pharmaceutical compositions can be administered to a subject in need thereof in an effective amount to reduce one or symptoms of the cancer, proliferative disorders, neurodegenerative diseases, autoimmune disorders, or inflammatory diseases alone or prior to or in conjunction with a further therapy such as radiotherapy.

## Claims

### Claim 1

A compound selected from the group consisting of:

### Claim 2 (depends on 1)

A composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.

### Claim 3 (depends on 2)

A method of treating cancer comprising administering to a patient in need thereof, a composition according to claim 2.