# US 11,304,949 B2 · Treatment of hidradenitis suppurativa using JAK inhibitors

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- Number: US 11,304,949 B2
- Document ID: US11304949B2
- Status: Granted
- Kind: B2
- Application number: 16/370,436
- Filed: 2019-03-29
- Published: 2019-10-31
- Granted: 2022-04-19
- Earliest claimed: 2018-03-30
- Assignees: Incyte Corporation
- Applicants: Incyte Corporation
- Inventors: Michael D. Howell; Paul Smith
- Web page: https://patentgrep.com/patent/US11304949B2

## CPC

- A61K 31/4155: non condensed and containing further heterocyclic rings
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 17/10: Anti-acne agents
- 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 application provides methods of treating hidradenitis suppurativa in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound which inhibits JAK1 and/or JAK2, or a pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A method of treating hidradenitis suppurativa in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound which is:
4[3-(cyanomethyl)-3-(3′,5′-dimethyl-1H,1′H-4,4′-bipyrazol-1-yl)azetidin-1-yl]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]benzamide, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the compound or salt is selective for JAK1 over JAK2, JAK3, and TYK2.

### Claim 3 (depends on 1)

The method of claim 1, wherein the compound is a pharmaceutically acceptable salt of 4[3-(cyanomethyl)-3-(3′,5′-dimethyl-1H,1H-4,4′-bipyrazol-1-yl)azetidin-1-yl]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]benzamide.

### Claim 4 (depends on 3)

The method of claim 3, wherein the salt is 4-[3-(cyanomethyl)-3-(3′,5′-dimethyl-1H, 1′H-4,4′-bipyrazol-1-yl)azetidin-1-yl]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]benzamide phosphoric acid salt.

### Claim 5 (depends on 1)

The method of claim 1, wherein the compound or salt is administered at a dosage of 15, 30, 60 or 90 mg on a free base basis.

### Claim 6 (depends on 1)

The method of claim 1, further comprising administering an additional therapeutic agent.

### Claim 7 (depends on 6)

The method of claim 6, wherein the additional therapeutic agent is an antibiotic, a retinoid, a corticosteroid, an anti-TNF-alpha agent, or an immunosuppressant.

### Claim 8 (depends on 7)

The method of claim 7, wherein the antibiotic is clindamycin, doxycycline, minocycline, trimethoprim-sulfamethoxazole, erythromycin, metronidazole, rifampin, moxifloxacin, dapsone, or a combination thereof.

### Claim 9 (depends on 7)

The method of claim 7, wherein the retinoid is etretinate, acitretin, or isotretinoin.

### Claim 10 (depends on 7)

The method of claim 7, wherein the corticosteroid is triamcinolone, dexamethasone, fluocinolone, cortisone, prednisone, prednisolone or flumetholone.

### Claim 11 (depends on 7)

The method of claim 7, wherein the anti-TNF-alpha agent is infliximab, etanercept, or adalimumab.

### Claim 12 (depends on 7)

The method of claim 7, wherein the immunosuppressant is methotrexate, cyclosporin A, mycophenolate mofetil, or mycophenolate sodium.

### Claim 13 (depends on 6)

The method of claim 6, wherein the additional therapeutic agent is finasteride, metformin, adapalene, or azelaic acid.

### Claim 14 (depends on 1)

The method of claim 1, wherein the administrating of the compound or salt is topical.

### Claim 15 (depends on 1)

The method of claim 1, wherein the administering of the compound or salt is oral.

### Claim 16 (depends on 1)

The method of claim 1, wherein the method results in a 10%, 20%, 30%, 40%, or 50% improvement in HiSCR (Hidradenitis Suppurativa Clinical Response).

### Claim 17 (depends on 1)

The method of claim 1, wherein the compound is 4-[3-(cyanomethyl)-3-(3′,5′-dimethyl-1H,1′H-4,4′-bipyrazol-1-yl)azetidin-1-yl]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]benzamide free base.