# US 11,897,869 B2 · JAK1 selective inhibitors

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- Number: US 11,897,869 B2
- Document ID: US11897869B2
- Status: Granted
- Kind: B2
- Application number: 17/188,097
- Filed: 2021-03-01
- Published: 2021-06-24
- Granted: 2024-02-13
- Earliest claimed: 2017-01-17
- Assignees: AstaZeneca AB
- Applicants: AstraZeneca AB
- Inventors: Karl Magnus Nilsson; Annika Birgitta Margareta Åstrand; Anna Ingrid Kristina Berggren; Johan R. Johansson; Matti Juhani Lepistö; Sameer Pralhad Kawatkar; Qibin Su; Jason Grant Kettle
- Web page: https://patentgrep.com/patent/US11897869B2

## CPC

- A61P 37/00: Drugs for immunological or allergic disorders
- C07D 403/14: containing three or more hetero rings
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61P 17/14: for baldness or alopecia
- C07D 403/04: directly linked by a ring-member-to-ring-member bond
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)

## Abstract

Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1-R8 have any of the meanings defined herein. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I) and methods of using the same.

## Claims

### Claim 1

A method of treating a JAK1-related disorder in a subject comprising administering a therapeutically effective amount of the compound (R)-N-(3-(5-fluoro-2-(2-fluoro-3-(methylsulfonyl)phenylamino)pyrimidin-4-yl)-1H-indol-7-yl)-3-methoxy-2-(4-methylpiperazin-1-yl)propanamide, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the JAK1-related disorder is chosen from Type 1 diabetes, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, COPD, vitiligo, and alopecia areata.

### Claim 3 (depends on 2)

The method of claim 2, wherein the JAK1-related disorder is asthma.

### Claim 4

A method of treating a JAK1-related disorder in a subject comprising administering a pharmaceutical composition which includes: a therapeutically effective amount of the compound (R)-N-(3-(5-fluoro-2-(2-fluoro-3-(methylsulfonyl)phenylamino)pyrimidin-4-yl)-1H-indol-7-yl)-3-methoxy-2-(4-methylpiperazin-1-yl)propanamide, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable diluent, excipient, or carrier.

### Claim 5 (depends on 4)

The method of claim 4, wherein the JAK1-related disorder is chosen from Type 1 diabetes, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, COPD, vitiligo, and alopecia areata.

### Claim 6 (depends on 5)

The method of claim 5, wherein the JAK1-related disorder is asthma.

### Claim 7

A method of treating a JAK1-related disorder in a subject comprising administering a therapeutically effective amount of the compound (R)-N-(3-(5-fluoro-2-(2-fluoro-3-(methylsulfonyl)phenylamino)pyrimidin-4-yl)-1H-indol-7-yl)-3-methoxy-2-(4-methylpiperazin-1-yl)propanamide.

### Claim 8 (depends on 7)

The method of claim 7, wherein the JAK1-related disorder is chosen from Type 1 diabetes, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, COPD, vitiligo, and alopecia areata.

### Claim 9 (depends on 8)

The method of claim 8, wherein the JAK1-related disorder is asthma.

### Claim 10

A method of treating a JAK1-related disorder in a subject comprising administering a pharmaceutical composition which includes: a therapeutically effective amount of the compound (R)-N-(3-(5-fluoro-2-(2-fluoro-3-(methylsulfonyl)phenylamino)pyrimidin-4-yl)-1H-indol-7-yl)-3-methoxy-2-(4-methylpiperazin-1-yl)propanamide; and a pharmaceutically acceptable diluent, excipient, or carrier.

### Claim 11 (depends on 10)

The method of claim 10, wherein the JAK1-related disorder is chosen from Type 1 diabetes, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, COPD, vitiligo, and alopecia areata.

### Claim 12 (depends on 11)

The method of claim 11, wherein the JAK1-related disorder is asthma.

### Claim 13

A method of treating a JAK1-related disorder in a subject comprising administering a therapeutically effective amount of a pharmaceutically acceptable salt of the compound (R)-N-(3-(5-fluoro-2-(2-fluoro-3-(methylsulfonyl)phenylamino)pyrimidin-4-yl)-1H -indol-7-yl)-3-methoxy-2-(4-methylpiperazin-1-yl)propanamide.

### Claim 14 (depends on 13)

The method of claim 13, wherein the JAK1-related disorder is chosen from Type 1 diabetes, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, COPD, vitiligo, and alopecia areata.

### Claim 15 (depends on 14)

The method of claim 14, wherein the JAK1-related disorder is asthma.

### Claim 16

A method of treating a JAK1-related disorder in a subject comprising administering a pharmaceutical composition which includes: a therapeutically effective amount of a pharmaceutically acceptable salt of the compound (R)-N-(3-(5-fluoro-2-(2-fluoro-3-(methylsulfonyl)phenylamino)pyrimidin-4-yl)-1H-indol-7-yl)-3-methoxy-2-(4-methylpiperazin -1-yl)propanamide; and a pharmaceutically acceptable diluent, excipient, or carrier.

### Claim 17 (depends on 16)

The method of claim 16, wherein the JAK1-related disorder is chosen from Type 1 diabetes, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, COPD, vitiligo, and alopecia areata.

### Claim 18 (depends on 17)

The method of claim 17, wherein the JAK1-related disorder is asthma.

### Claim 19 (depends on 2)

The method of claim 2, wherein the JAK1-related disorder is COPD.

### Claim 20 (depends on 5)

The method of claim 5, wherein the JAK1-related disorder is COPD.

### Claim 21 (depends on 8)

The method of claim 8, wherein the JAK1-related disorder is COPD.

### Claim 22 (depends on 11)

The method of claim 11, wherein the JAK1-related disorder is COPD.

### Claim 23 (depends on 14)

The method of claim 14, wherein the JAK1-related disorder is COPD.

### Claim 24 (depends on 17)

The method of claim 17, wherein the JAK1-related disorder is COPD.