# US 12,215,123 B2 · Cordycepin-based derivatized compound with anti-tumor effect

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- Number: US 12,215,123 B2
- Document ID: US12215123B2
- Status: Granted
- Kind: B2
- Application number: 18/505,822
- Filed: 2023-11-09
- Published: 2024-04-11
- Granted: 2025-02-04
- Earliest claimed: 2022-07-12
- Assignees: Nanjing Tech University
- Applicants: Nanjing Tech University
- Inventors: Hanjie Ying; Tao Shen; Chenglun Tang; Dong Liu; Yong Chen; Chenjie Zhu; Pengpeng Yang; Wei Zhuang
- Web page: https://patentgrep.com/patent/US12215123B2

## CPC

- C07H 19/20: with the saccharide radical esterified by phosphoric or polyphosphoric acids
- A61P 35/00: Antineoplastic agents
- C07H 19/173: with 2-deoxyribosyl as the saccharide radical
- Y02P 20/55: Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

A cordycepin-based derived compound with an anti-tumor effect, and a structure of the compound is as shown in formula I; a cordycepin derivative and a pharmaceutical composition thereof provided by the invention have a good anti-tumor proliferation effect; compared with a parent drug, the cordycepin derivative has better affinity to cell membranes, so that a half-life period of in-vivo metabolism of the drug is longer, and in-vivo remaining time of the drug is longer; compared with other nucleoside anti-tumor drugs, the cordycepin derivative and the pharmaceutical composition thereof provided by the invention have wider types and action ranges of tumors, have excellent inhibition effects on a gastric cancer, a pancreatic cancer, a liver cancer, a small cell lung cancer, a colorectal cancer, melanoma, an ovarian cancer and the like, and have lower side effects and better curative effects.

## Claims

### Claim 1

A cordycepin derivative is
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising at least one cordycepin derivative of claim 1, or the pharmaceutically acceptable salt thereof; and at least one immune checkpoint inhibitor.

### Claim 3 (depends on 2)

The pharmaceutical composition according to claim 2, wherein the immune checkpoint inhibitor is selected from the group consisting of a PD-1 monoclonal antibody, CTLA4 monoclonal antibody, and a combination of the PD-1 monoclonal antibody and the CTLA4 monoclonal antibody.

### Claim 4 (depends on 2)

The pharmaceutical composition according to claim 2, wherein a ratio of the cordycepin derivative: the immune checkpoint inhibitor is 1:0.2-5 by weight.

### Claim 5 (depends on 4)

The pharmaceutical composition according to claim 4, wherein the ratio of the cordycepin derivative: the immune checkpoint inhibitor is 1:0.8-1.2 by weight.

### Claim 6 (depends on 2)

The pharmaceutical composition according to claim 2, wherein the pharmaceutical composition is prepared as a tablet, a pill, a capsule, a syrup, an injection, a sustained to release agent, or a kit.

### Claim 7 (depends on 1)

A method for preventing and treating a disease by administering the cordycepin derivative of claim 1, or the pharmaceutically acceptable salt thereof to a subject in need, wherein the disease is a tumor.

### Claim 8 (depends on 6)

The method according to claim 6, wherein the tumor is selected from the group consisting of a gastric cancer, a pancreatic cancer, a liver cancer, a small cell lung cancer, a non-small cell lung cancer, a colorectal cancer, an esophageal cancer, a prostate cancer, melanoma, glioma, and an ovarian cancer.