# US 10,441,564 B2 · Fructose analogs and their combinations as anti-cancer agents

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- Number: US 10,441,564 B2
- Document ID: US10441564B2
- Status: Granted
- Kind: B2
- Application number: 15/591,046
- Filed: 2017-05-09
- Published: 2018-05-17
- Granted: 2019-10-15
- Earliest claimed: 2016-04-12
- Assignees: Wei Jia
- Applicants: Wei Jia; Wenlian Chen
- Inventors: Wei Jia; Wenlian Chen
- Web page: https://patentgrep.com/patent/US10441564B2

## CPC

- A61K 31/341: not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/7068: having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/12: of the kidneys
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 35/00: Antineoplastic agents
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides a fructose analogue and a composition thereof which can be used for cancer treatment, has a targeting effect and has little effect on normal cells, particularly when used in the treatment of acute myeloid leukemia (‘AML’) and pancreatic cancer and other types of cancer having similar metabolic characteristics. In the present invention, the fructose analog is selected from the group consisting of 2,5-anhydro-D-mannitol and the 2,5-anhydro-D-mannitol derivative substituted at the 1-position or 6-position by an amino group, an alkyl group or an aryl group, anhydro-D-mannitol tetraacetate and 2,5-anhydroglucitol and the like. The fructose analogs of the present invention can be used to prepare and treat cancer drugs and can be prepared as injectable preparations or oral preparations. The fructose analogues of the present invention can be used in combination with conventional anticancer drugs when used in the preparation of a medicament for the treatment of cancer. The fructose analogs of the present invention can be used in combination with glucose analogues in the treatment of cancer or organ fibrosis.

## Claims

### Claim 1

A method of treating a cancer selected from acute myeloid leukemia, pancreatic cancer, and lung cancer, the method comprising administering to a subject in need thereof a fructose analog selected from the group consisting of:
2,5-anhydro-D-mannitol;
a 2,5-anhydro-D-mannitol derivative substituted at the 1-position or 6-position by an amino group, an alkyl group or an aryl group;
2,5-anhydro-D-mannitol tetraacetate; and
2,5-anhydroglucitol.

### Claim 2

A method of treating cancer comprising administering to a subject in need thereof a fructose analog selected from the group consisting of:
2,5-anhydro-D-mannitol;
a 2,5-anhydro-D-mannitol derivative substituted at the 1-position or 6-position by an amino group, an alkyl group or an aryl group;
2,5-anhydro-D-mannitol tetraacetate; and
2,5-anhydroglucitol,
wherein the cancer is selected from acute myeloid leukemia, pancreatic cancer, colorectal cancer and lung cancer.

### Claim 3

A method of treating a cancer selected from acute myeloid leukemia (AMU), pancreatic cancer, lung cancer, and colorectal cancer comprising administering to a subject in need thereof a fructose analog and an anticancer agent, wherein
the fructose analog is selected from the group consisting of:
2,5-anhydro-D-mannitol;
a 2,5-anhydro-D-mannitol derivative substituted at the 1-position or 6-position by an amino group, an alkyl group or an aryl group;
2,5-anhydro-D-mannitol tetraacetate; and
2,5-anhydroglucitol; and
the anticancer agent is selected from the group consisting of cytarabine (Ara-C), daunorubicin, doxorubicin, cisplatin, carboplatin, gemcitabine, capecitabine, sorafenib, docetaxel, paclitaxel, adriamycin, and 5-fluorouracil.