# US 12,594,265 B2 · Methods and compositions for inhibition of STAT3

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- Number: US 12,594,265 B2
- Document ID: US12594265B2
- Status: Granted
- Kind: B2
- Application number: 17/821,286
- Filed: 2022-08-22
- Published: 2023-03-30
- Granted: 2026-04-07
- Earliest claimed: 2017-09-27
- Assignees: Ohio State Innovation Foundation
- Applicants: Ohio State Innovation Foundation
- Inventors: Yuhong Yang; Chenglong Li; Michael Racke
- Web page: https://patentgrep.com/patent/US12594265B2

## CPC

- A61K 31/428: condensed with carbocyclic rings
- A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63)
- 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

In one aspect, the disclosure relates to prodrug compositions of a STAT inhibitor compound. In some aspects, the STAT is STAT3. Disclosed are pharmaceutical compositions comprising the prodrug inhibitors of STAT. In various aspects, the prodrug inhibitors of STAT can be used in methods of treating an inflammatory disorder, including multiple sclerosis, or a disorder of uncontrolled cellular proliferation, such as a cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

## Claims

### Claim 1

A method for ameliorating or alleviating cancer in a mammal comprising the step of administering to the mammal a therapeutically effective amount of at least one compound having a structure represented by a formula,
wherein each of R1 and R2 is independently selected from hydrogen and C1-C6 alkyl;
wherein each of R3, R4, R5, R7, R8, and R9 is independently selected from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, halogen, —NO2, —NH2, and —OH; and
wherein R20 is selected from —C(O)—O—(C1-C6 alkylene), —C(O)—(C1-C6 alkylene), —C(O)—(C1-C6 alkylene)-C(O)OH, —C(O)—NR21R22, and —(C1-C6 alkylene)-PO3H2;
wherein each of R21 and R22 is independently selected from hydrogen and C1-C6 alkyl;
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the cancer is selected the group consisting of breast cancer, renal cancer, gastric cancer, colorectal cancer, multiple myeloma, leukemia, lymphoma, cutaneous T-cell lymphoma, Hodgkin's disease, and a solid tumor.

### Claim 3 (depends on 1)

The method of claim 1, wherein the compound has a structure represented by a formula:

### Claim 4 (depends on 1)

The method of claim 1, wherein the compound has a structure represented by a formula:

### Claim 5 (depends on 1)

The method of claim 1, wherein R20 is selected from —C(O)—(C1-C6 alkylene)-C(O)OH, —C(O)—NR21R22, and —(C1-C6 alkylene)-PO3H2; and wherein each of R21 and R22 is independently selected from hydrogen and C1-C6 alkyl.

### Claim 6 (depends on 1)

The method of claim 1, wherein R20 is selected from —C(O)—(C1-C6 alkylene)-C(O)OH, —C(O)—NR21R22, and —(C1-C6 alkylene)-PO3H2; and wherein each of R21 and R22 is independently selected from hydrogen and methyl.

### Claim 7 (depends on 1)

The method of claim 1, wherein R20 is selected from —C(O)—(CH2)2—C(O)OH, —C(O)—NH2, and —(CH2)—PO3H2.

### Claim 8 (depends on 1)

The method of claim 1, wherein the compound has a structure represented by a formula:

### Claim 9 (depends on 1)

The method of claim 1, wherein the compound has a structure represented by a formula:

### Claim 10

A method for ameliorating or alleviating cancer in a mammal comprising the step of administering to the mammal a therapeutically effective amount of at least one compound having a structure represented by a formula:
wherein each of R3, R4, R5, R7, R8, and R9 is independently selected from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, halogen, —NO2, —NH2, and —OH; and
wherein R20 is selected from —C(O)—O—(C1-C6 alkylene), —C(O)—(C1-C6 alkylene), —C(O)—(C1-C6 alkylene)-C(O)OH, —C(O)—NR21R22, and —(C1-C6 alkylene)-PO3H2;
wherein each of R21 and R22 is independently selected from hydrogen and C1-C6 alkyl;
or a pharmaceutically acceptable salt thereof.

### Claim 11 (depends on 10)

The method of claim 10, wherein the cancer is selected the group consisting of breast cancer, renal cancer, gastric cancer, colorectal cancer, multiple myeloma, leukemia, lymphoma, cutaneous T-cell lymphoma, Hodgkin's disease, and a solid tumor.

### Claim 12 (depends on 10)

The method of claim 10, wherein the compound has a structure represented by a formula:

### Claim 13 (depends on 10)

The method of claim 10, wherein the compound has a structure represented by a formula:

### Claim 14 (depends on 10)

The method of claim 10, wherein R20 is —C(O)—(C1-C6 alkylene)-C(O)OH, C(O)—NR21R22, and —(C1-C6 alkylene)-PO3H2; and wherein each of R21 and R22 is independently selected from hydrogen and C1-C6 alkyl.

### Claim 15 (depends on 10)

The method of claim 10, wherein R20 is —C(O)—(C1-C6 alkylene)-C(O)OH, —C(O)—NR21R22, and —(C1-C6 alkylene)-PO3H2; and wherein each of R21 and R22 is independently selected from hydrogen and methyl.

### Claim 16 (depends on 10)

The method of claim 10, wherein R20 is selected from —C(O)—(CH2)2—C(O)OH, —C(O)—NH2, and —(CH2)—PO3H2.

### Claim 17 (depends on 10)

The method of claim 10, wherein the compound has a structure represented by a formula:

### Claim 18 (depends on 10)

The method of claim 10, wherein the compound has a structure represented by a formula:

### Claim 19

A method for inhibiting STAT3 in a mammal comprising the step of administering to the mammal a therapeutically effective amount of at least one compound having a structure represented by a formula,
wherein each of R1 and R2 is independently selected from hydrogen and C1-C6 alkyl;
wherein each of R3, R4, R5, R7, R8, and R9 is independently selected from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, halogen, —NO2, —NH2, and —OH; and
wherein R20 is selected from —C(O)—O—(C1-C6 alkylene), —C(O)—(C1-C6 alkylene), —C(O)—(C1-C6 alkylene)-C(O)OH, —C(O)—NR21R22, and —(C1-C6 alkylene)-PO3H2;
wherein each of R21 and R22 is independently selected from hydrogen and C1-C6 alkyl;
or a pharmaceutically acceptable salt thereof.