# US 11,992,490 B2 · Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)

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- Number: US 11,992,490 B2
- Document ID: US11992490B2
- Status: Granted
- Kind: B2
- Application number: 17/072,093
- Filed: 2020-10-16
- Published: 2021-04-22
- Granted: 2024-05-28
- Earliest claimed: 2019-10-16
- Assignees: Incyte Corporation
- Applicants: Incyte Corporation
- Inventors: Paul Smith; Jörg Wenzel
- Web page: https://patentgrep.com/patent/US11992490B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/4155: non condensed and containing further heterocyclic rings
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61P 17/00: Drugs for dermatological disorders
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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 a disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a JAK1 selective inhibitor, or a pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A method of treating cutaneous lupus erythematosus (CLE) in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a JAK1 selective inhibitor, wherein the JAK1 selective inhibitor is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the pharmaceutically acceptable salt is {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile adipic acid salt.

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 3)

The method of claim 3, wherein the additional therapeutic agent is selected from a JAK1/JAK2 inhibitor, a JAK1/JAK3 inhibitor, a TYK2 inhibitor, or a pharmaceutically acceptable salt of any of the aforementioned.

### Claim 5 (depends on 4)

The method of claim 4, wherein the additional therapeutic agent is a JAK1/JAK2 inhibitor, or a pharmaceutically acceptable salt thereof.

### Claim 6 (depends on 4)

The method of claim 4, wherein the JAK1/JAK2 inhibitor, or a pharmaceutically acceptable salt thereof, is selective for JAK1 and JAK2 over JAK3 and TYK2.

### Claim 7 (depends on 4)

The method of claim 4, wherein the JAK1/JAK2 inhibitor is ruxolitinib, or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 7)

The method of claim 7, wherein the method comprises topical administration of the ruxolitinib, or a pharmaceutically acceptable salt thereof, to the patient.

### Claim 9 (depends on 7)

The method of claim 7, wherein the method comprises oral administration of the ruxolitinib, or a pharmaceutically acceptable salt thereof, to the patient.

### Claim 10 (depends on 7)

The method of claim 7, wherein the pharmaceutically acceptable salt is ruxolitinib phosphate.

### Claim 11 (depends on 4)

The method of claim 4, wherein the JAK1/JAK2 inhibitor is ruxolitinib, or a pharmaceutically acceptable salt thereof, wherein one or more hydrogen atoms are replaced by deuterium atoms.

### Claim 12 (depends on 4)

The method of claim 4, wherein the additional therapeutic agent is a JAK1/JAK3 inhibitor, or a pharmaceutically acceptable salt thereof.

### Claim 13 (depends on 4)

The method of claim 4, wherein the JAK1/JAK3 inhibitor is tofacitinib, or a pharmaceutically acceptable salt thereof.

### Claim 14 (depends on 1)

The method of claim 1, wherein the method comprises topical administration of the JAK1 selective inhibitor to the patient.

### Claim 15 (depends on 1)

The method of claim 1, wherein the method comprises oral administration of the JAK1 selective inhibitor to the patient.

### Claim 16 (depends on 1)

The method of claim 1, wherein the cutaneous lupus erythematosus (CLE) is selected from subacute cutaneous lupus erythematosus (SCLE) and chronic discoid lupus erythematosus (CDLE).