# US 10,441,600 B2 · Oligodeoxy nucleotide for preparing drugs for inhibiting tumor growth and application thereof

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- Number: US 10,441,600 B2
- Document ID: US10441600B2
- Status: Granted
- Kind: B2
- Application number: 15/538,288
- Filed: 2015-06-25
- Published: 2018-05-24
- Granted: 2019-10-15
- Earliest claimed: 2014-12-30
- Assignees: Jiangsu Keygen Biotech Corp., Ltd; Nanjing New Industry Investment Group Co., Ltd
- Applicants: Nanjing New Industry Investment Group Co., Ltd.; Jiangsu Keygen Biotech Corp., Ltd
- Inventors: Xuegen Wang; Qing Ye; Yijun Sun
- Web page: https://patentgrep.com/patent/US10441600B2

## CPC

- A61K 31/7125: Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61P 35/00: Antineoplastic agents
- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- C12N 2310/11: Antisense
- C12N 2310/14: interfering nucleic acids [NA]
- C12N 2310/315: Phosphorothioates
- C12N 2330/30: chemically synthesised
- C12Q 2600/106: Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
- C12Q 2600/136: Screening for pharmacological compounds
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES

## Abstract

The present invention provides an oligodeoxy nucleotide for preparing drugs for inhibiting tumor growth and an application thereof. The core sequences of the oligodeoxy nucleotide is TTTCSCGCS, wherein S is C or G. The oligodeoxy nucleotide above further comprises an antisense strand and a modified type thereof. The oligodeoxy nucleotide according to the present invention plays a role of inhibiting the tumor growth in vitro and vivo, and is expected to be used for preparing drugs for inhibiting tumor growth, with high specificity and high inhibition ratio.

## Claims

### Claim 1

An oligodeoxy nucleotide for preparing drugs for inhibiting tumor growth, wherein the oligodeoxy nucleotide is any one of the following sequences:
(SEQ ID NO: 7)
5′-TGACTATTTCCCGCGACTT-3′;
(SEQ ID NO: 8)
5′-TTGACTATTTCCCGCCACTT-3′;
and
(SEQ ID NO: 9)
5′-ATCTATTTCGCGCCCTTATG-3′.

### Claim 2 (depends on 1)

An oligodeoxy nucleotide fully complementary to any of the oligodeoxy nucleotides of claim 1.

### Claim 3 (depends on 1)

The oligodeoxy nucleotide according to claim 1, wherein the oligodeoxy nucleotide is modified.

### Claim 4 (depends on 3)

The oligodeoxy nucleotide according to claim 3, wherein the modification is a phosphorothioate modification; or phosphorothioate modifications of three nucleotides at each end; or full phosphorothioate modification.

### Claim 5 (depends on 1)

A method for preparing drugs for inhibiting tumor growth, comprising:
applying the oligodeoxy nucleotide according to claim 1 in preparing drugs for inhibiting tumor growth; and
purifying the oligodeoxy nucleotide through HPLC, and preparing the oligodeoxy nucleotide into concentration of 1-2 mg/mL by sterilization water, then conducting equal molar ratio mixture to the oligodeoxy nucleotide with an antisense strand thereof, heating the mixture to 80-85° C. for 10-15 min through water bath, cooling the mixture to indoor temperature naturally, and annealing to combine the mixture into double strands for preparing drugs for inhibiting tumor growth.

### Claim 6 (depends on 2)

The oligodeoxy nucleotide according to claim 2, wherein the oligodeoxy nucleotide is modified.

### Claim 7 (depends on 6)

The oligodeoxy nucleotide according to claim 6, wherein the modification is a phosphorothioate modification; or phosphorothioate modifications of three nucleotides at each end; or full phosphorothioate modification.

### Claim 8 (depends on 2)

A method for preparing drugs for inhibiting tumor growth, comprising:
applying the oligodeoxy nucleotide according to claim 2 in preparing drugs for inhibiting tumor growth; and
purifying the oligodeoxy nucleotide through HPLC, and preparing the oligodeoxy nucleotide into concentration of 1-2 mg/mL by sterilization water, then conducting equal molar ratio mixture to the oligodeoxy nucleotide with an antisense strand thereof, heating the mixture to 80-85° C. for 10-15min through water bath, cooling the mixture to indoor temperature naturally, and annealing to combine the mixture into double strands for preparing drugs for inhibiting tumor growth.

### Claim 9 (depends on 3)

A method for preparing drugs for inhibiting tumor growth, comprising:
applying the oligodeoxy nucleotide according to claim 3 in preparing drugs for inhibiting tumor growth; and
purifying the oligodeoxy nucleotide through HPLC, and preparing the oligodeoxy nucleotide into concentration of 1-2mg/mL by sterilization water, then conducting equal molar ratio mixture to the oligodeoxy nucleotide with an antisense strand thereof, heating the mixture to 80-85° C. for 10-15 min through water bath, cooling the mixture to indoor temperature naturally, and annealing to combine the mixture into double strands for preparing drugs for inhibiting tumor growth.

### Claim 10 (depends on 4)

A method for preparing drugs for inhibiting tumor growth, comprising:
applying the oligodeoxy nucleotide according to claim 4 in preparing drugs for inhibiting tumor growth; and
purifying the oligodeoxy nucleotide through HPLC, and preparing the oligodeoxy nucleotide into concentration of 1-2 mg/mL by sterilization water, then conducting equal molar ratio mixture to the oligodeoxy nucleotide with an antisense strand thereof, heating the mixture to 80-85° C. for 10-15 min through water bath, cooling the mixture to indoor temperature naturally, and annealing to combine the mixture into double strands for preparing drugs for inhibiting tumor growth.

### Claim 11

An oligodeoxy nucleotide for preparing drugs for inhibiting tumor growth, wherein a sequence of the oligodeoxy nucleotide consists of the following sequence:
(SEQ ID NO: 10)
5′-TTAAGTTTCGCGCCCTTTCTC-3′.

### Claim 12 (depends on 11)

An oligodeoxy nucleotide fully complementary to the oligodeoxy nucleotide of claim 11.

### Claim 13 (depends on 11)

The oligodeoxy nucleotide according to claim 11, wherein the oligodeoxy nucleotide is modified.

### Claim 14 (depends on 13)

The oligodeoxy nucleotide according to claim 13, wherein the modification is a phosphorothioate modification; or phosphorothioate modifications of three nucleotides at each end; or full phosphorothioate modification.

### Claim 15 (depends on 12)

The oligodeoxy nucleotide according to claim 12, wherein the oligodeoxy nucleotide is modified.

### Claim 16 (depends on 15)

The oligodeoxy nucleotide according to claim 15, wherein the modification is a phosphorothioate modification; or phosphorothioate modifications of three nucleotides at each end; or full phosphorothioate modification.

### Claim 17 (depends on 11)

A method for preparing drugs for inhibiting tumor growth, comprising:
applying the oligodeoxy nucleotide according to claim 11 in preparing drugs for inhibiting tumor growth; and
purifying the oligodeoxy nucleotide through HPLC, and preparing the oligodeoxy nucleotide into concentration of 1-2 mg/mL by sterilization water, then conducting equal molar ratio mixture to the oligodeoxy nucleotide with an antisense strand thereof, heating the mixture to 80-85° C. for 10-15 min through water bath, cooling the mixture to indoor temperature naturally, and annealing to combine the mixture into double strands for preparing drugs for inhibiting tumor growth.