# US 11,993,603 B2 · Preparation for 6-amino-1H-pyrazolo[3,4-d]pyrimidine-based JAK kinase inhibitor and application thereof

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- Number: US 11,993,603 B2
- Document ID: US11993603B2
- Status: Granted
- Kind: B2
- Application number: 17/275,209
- Filed: 2019-09-05
- Published: 2022-02-17
- Granted: 2024-05-28
- Earliest claimed: 2018-09-11
- Assignees: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College; China Parmaceutical University
- Applicants: Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College; China Pharmaceutical University
- Inventors: Tiantai Zhang; Dayong Zhang; Chengjuan Chen; Yuan Yin; Runan Yu; Lei Shu
- Web page: https://patentgrep.com/patent/US11993603B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/04: for throat disorders
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 19/10: for osteoporosis
- A61P 21/04: for myasthenia gravis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- C07D 471/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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

A medicament with excellent JAK kinase (Janus Kinase) inhibitory activity can be used to prevent, treat and/or improve an autoimmune disease (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus and the like). The present invention also provides a pharmaceutically acceptable composition containing the compound and a method for preparing these compounds.

## Claims

### Claim 1

A compound having the following structure or a pharmaceutically acceptable salt thereof:

### Claim 2 (depends on 1)

The compound or the pharmaceutically acceptable salt thereof according to claim 1, which is a Janus kinase (JAK) inhibitor.

### Claim 3 (depends on 2)

The compound or the pharmaceutically acceptable salt thereof according to claim 2, which is a medicament for treating a JAK-mediated autoimmune disease.

### Claim 4 (depends on 3)

The compound or the pharmaceutically acceptable salt thereof according to claim 3, wherein the JAK-mediated autoimmune disease is psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis or systemic lupus erythematosus.

### Claim 5 (depends on 1)

A method for treating a Janus kinase (JAK)-mediated autoimmune disease comprising a step of administering to a subject in need thereof the compound of claim 1 or its pharmaceutically acceptable salt.

### Claim 6 (depends on 5)

The method according to claim 5, wherein the JAK-mediated autoimmune disease is selected from the group consisting of psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis and systemic lupus erythematosus.