# US 12,213,980 B2 · Application of PDE9A inhibitor in preparation of products having elevated Treg content, drugs for preventing and treating inflammatory bowel disease and health care products

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- Number: US 12,213,980 B2
- Document ID: US12213980B2
- Status: Granted
- Kind: B2
- Application number: 17/258,910
- Filed: 2019-07-09
- Published: 2021-10-21
- Granted: 2025-02-04
- Earliest claimed: 2018-07-10
- Assignees: Zhejiang University
- Applicants: Zhejiang University
- Inventors: Huifang Tang
- Web page: https://patentgrep.com/patent/US12213980B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- 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 relates to the field of medicine, and related to an application of a PDE9A inhibitor in the preparation of products having an elevated Treg content, drugs for preventing and treating inflammatory bowel disease, and health care products. The PDE9A inhibitor may improve the secretion of mucosal mucus in an intestinal tract suffering from inflammatory bowel disease, reduce the secretion of TNF-α, IL-6, IL-17 and IL-12/IL-23 pro-inflammatory factors, inhibit DC cell differentiation and migration, increase the ratio Foxp3+Treg cells, promote the movement of CD4+CD25+ Treg cells from the spleen and mesenteric lymph nodes to the colon, thereby inhibiting an intestinal inflammatory response and controlling the occurrence and development of the disease. When PDE9A inhibitor is applied to a drug for preventing and treating inflammatory bowel disease, inflammatory bowel disease may be effectively prevented, alleviated and treated, while healthcare products containing said inhibitor as an active ingredient may regulate the intestinal tract of patients suffering from inflammatory bowel disease and control the occurrence and development of inflammatory bowel disease.

## Claims

### Claim 1

A method for increasing Treg amount, which comprises administering an effective amount of PDE9A inhibitor PF-04447943 or a product comprising PDE9A inhibitor PF-04447943 to a subject in need.

### Claim 2 (depends on 1)

The method of claim 1, wherein the product comprises a medicine, a reagent, or a health care product.

### Claim 3 (depends on 2)

The method of claim 2, wherein the medicine comprises PDE9A inhibitor PF-04447943 and a pharmaceutical carrier.

### Claim 4 (depends on 3)

The method of claim 3, wherein the pharmaceutical carrier is selected from the group consisting of: an absorption enhancer, a surfactant, a lubricant, a stabilizer, a diluent, an adhesive, a wetting agent, a disintegrant, an adsorption vehicle, an excipient, a coloring agent, a sweetener, and a flavoring agent.

### Claim 5 (depends on 2)

The method of claim 2, wherein the medicine has a dosage form selected from the group consisting of: an injection, an oral liquid, an enema, a capsule, a tablet, an enteric agent, a powder, and a granule.

### Claim 6 (depends on 1)

The method of claim 1, wherein the amount of Treg is related to the onset of an autoimmune disease selected from the group consisting of: rheumatoid arthritis, autoimmune thyroiditis, autoimmune liver disease, and kidney disease.

### Claim 7

A method for treating a Treg related disease, which comprises administering an effective amount of PDE9A inhibitor PF-04447943 or a pharmaceutical composition comprising PDE9A inhibitor PF-04447943 to a subject in need,
wherein the Treg related disease is selected from the group consisting of: inflammatory bowel disease, rheumatoid arthritis, autoimmune thyroiditis, autoimmune liver disease, and kidney disease.

### Claim 8 (depends on 7)

The method of claim 7, wherein the Treg related disease is inflammatory bowel disease.

### Claim 9 (depends on 8)

The method of claim 8, wherein the inflammatory bowel disease is ulcerative colitis or Crohn's disease.

### Claim 10 (depends on 7)

The method of claim 7, wherein the pharmaceutical composition comprises PDE9A inhibitor PF-04447943 and a pharmaceutical carrier.

### Claim 11

A method for regulating inflammatory bowel disease, which comprises administering an effective amount of a health care product comprising PDE9A inhibitor PF-04447943 to a subject in need.

### Claim 12 (depends on 11)

The method of claim 11, wherein the health care product further comprises an auxiliary material selected from the group consisting of: an absorption enhancer, a surfactant, a lubricant, a stabilizer, a diluent, an adhesive, a wetting agent, a disintegrant, an adsorption vehicle, an excipient, a coloring agent, a sweetener, and a flavoring agent.