# US 11,998,543 B2 · Pharmaceutical composition comprising aldehyde inhibitor and anticancer agent for treatment of brain cancer

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- Number: US 11,998,543 B2
- Document ID: US11998543B2
- Status: Granted
- Kind: B2
- Application number: 17/259,029
- Filed: 2019-05-17
- Published: 2021-09-02
- Granted: 2024-06-04
- Earliest claimed: 2018-07-09
- Assignees: Industry-Academic Cooperation Foundation, Yonsei University; National Cancer Center
- Applicants: Industry-Academic Cooperation Foundation, Yonsei University; National Cancer Center
- Inventors: Seok-Gu Kang; Soo Youl Kim
- Web page: https://patentgrep.com/patent/US11998543B2

## CPC

- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/11: Aldehydes
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- 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 disclosure relates to a pharmaceutical composition for treating brain cancer containing an aldehyde inhibitor and an anticancer drug. Since there are many types of brain cancer and the boundary between brain cells and tumor cells in brain cancer is not clear, brain cancer is particularly difficult to treat. The pharmaceutical composition of the present disclosure may further contain a biguanide-based compound as needed, wherein the compound is preferably phenformin. The pharmaceutical composition of the present disclosure is very effective for the treatment and improvement of prognosis of brain cancer, and has remarkable effects of killing cancer cells and inhibiting cancer stem cell characteristics, compared to when each of the active ingredients is administered alone. Thus, it is expected that the pharmaceutical composition of the present disclosure will be widely used in the field of brain cancer treatment.

## Claims

### Claim 1

A method for preventing or treating brain cancer in a patient or for suppressing brain cancer metastasis in a patient, the method comprising administering to the patient a pharmaceutical composition comprising gossypol, phenformin and temozolomide as active ingredients.

### Claim 2 (depends on 1)

The method of claim 1, wherein the method is for preventing or treating brain cancer in the patient.

### Claim 3 (depends on 2)

The method of claim 2, wherein the brain cancer is primary brain cancer or secondary brain cancer.

### Claim 4 (depends on 3)

The method of claim 3, wherein the brain cancer is any one or more selected from the group consisting of astrocytoma, glioblastoma, ependymoma, oligodendroglioma, mixed glioma, brain stem glioma, optic nerve glioma, pituitary adenoma, craniopharyngioma, medulloblastoma, primitive neuroectodermal tumors, pineal tumors, meningioma, schwannoma, metastatic brain tumors, CNS lymphoma, neurofibromatosis, pseudotumor cerebri, and tuberous sclerosis.

### Claim 5 (depends on 2)

The method of claim 2, wherein the brain cancer includes brain cancer stem cells.

### Claim 6 (depends on 2)

The method of claim 2, wherein the treating includes inhibiting an increase in the number of cancer cells, or inhibiting an increase in the amount of cancer cells, or killing cancer cells, or maintaining the size of cancer tissue, or decreasing the size of cancer tissue, or inhibiting the development of new blood vessels in cancer tissue.

### Claim 7 (depends on 1)

The method of claim 1, wherein the method is for suppressing brain cancer metastasis in the patient.

### Claim 8 (depends on 7)

The method of claim 7, wherein the brain cancer is primary brain cancer or secondary brain cancer.

### Claim 9 (depends on 8)

The method of claim 8, wherein the brain cancer is any one or more selected from the group consisting of astrocytoma, glioblastoma, ependymoma, oligodendroglioma, mixed glioma, brain stem glioma, optic nerve glioma, pituitary adenoma, craniopharyngioma, medulloblastoma, primitive neuroectodermal tumors, pineal tumors, meningioma, schwannoma, metastatic brain tumors, CNS lymphoma, neurofibromatosis, pseudotumor cerebri, and tuberous sclerosis.

### Claim 10 (depends on 7)

The method of claim 7, wherein the brain cancer includes brain cancer stem cells.

### Claim 11

A method for preventing or treating brain cancer or for suppressing brain cancer metastasis in a patient, the method comprising administering to the patient gossypol, phenformin and temozolomide as active ingredients.

### Claim 12 (depends on 11)

The method of claim 11, wherein the method is for preventing or treating brain cancer in the patient.

### Claim 13 (depends on 12)

The method of claim 12, wherein the brain cancer is primary brain cancer or secondary brain cancer.

### Claim 14 (depends on 13)

The method of claim 13, wherein the brain cancer is any one or more selected from the group consisting of astrocytoma, glioblastoma, ependymoma, oligodendroglioma, mixed glioma, brain stem glioma, optic nerve glioma, pituitary adenoma, craniopharyngioma, medulloblastoma, primitive neuroectodermal tumors, pineal tumors, meningioma, schwannoma, metastatic brain tumors, CNS lymphoma, neurofibromatosis, pseudotumor cerebri, and tuberous sclerosis.

### Claim 15 (depends on 12)

The method of claim 12, wherein the brain cancer includes brain cancer stem cells.

### Claim 16 (depends on 12)

The method of claim 12, wherein the treating includes inhibiting an increase in the number of cancer cells, or inhibiting an increase in the amount of cancer cells, or killing cancer cells, or maintaining the size of cancer tissue, or decreasing the size of cancer tissue, or inhibiting the development of new blood vessels in cancer tissue.

### Claim 17 (depends on 11)

The method of claim 11, wherein the method is for suppressing brain cancer metastasis in the patient.

### Claim 18 (depends on 17)

The method of claim 17, wherein the brain cancer is primary brain cancer or secondary brain cancer.

### Claim 19 (depends on 18)

The method of claim 18, wherein the brain cancer is any one or more selected from the group consisting of astrocytoma, glioblastoma, ependymoma, oligodendroglioma, mixed glioma, brain stem glioma, optic nerve glioma, pituitary adenoma, craniopharyngioma, medulloblastoma, primitive neuroectodermal tumors, pineal tumors, meningioma, schwannoma, metastatic brain tumors, CNS lymphoma, neurofibromatosis, pseudotumor cerebri, and tuberous sclerosis.

### Claim 20 (depends on 17)

The method of claim 17, wherein the brain cancer includes brain cancer stem cells.
