# US 11,298,570 B2 · Methods for treating hair loss disorders

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- Number: US 11,298,570 B2
- Document ID: US11298570B2
- Status: Granted
- Kind: B2
- Application number: 16/299,382
- Filed: 2019-03-12
- Published: 2019-08-29
- Granted: 2022-04-12
- Earliest claimed: 2010-11-02
- Assignees: The Trustees of Columbia University in the City of New York
- Applicants: The Trustees of Columbia University In the City of New York
- Inventors: Angela M. Christiano; Raphael Clynes
- Web page: https://patentgrep.com/patent/US11298570B2

## CPC

- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61Q 7/00: Preparations for affecting hair growth
- A61K 8/41: Amines
- A61K 8/4953: {containing pyrimidine ring derivatives, e.g. minoxidil}
- A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/277: having a ring, e.g. verapamil
- A61K 31/407: condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/52: Purines, e.g. adenine
- A61K 31/529: forming part of bridged ring systems
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61K 31/553: having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
- A61K 31/63: Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K 31/7052: having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K 2800/782: Enzyme inhibitors; Enzyme antagonists
- 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)
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

The invention provides for methods for treating a hair loss disorder in a subject by administering a Janus Kinase/Signal Transducers and Activators of Transcription inhibitor.

## Claims

### Claim 1

A method of treating a hair loss disorder in a subject in need thereof, the method consisting of: administering to the subject an effective amount of a small molecule janus kinase (JAK) 1 and/or JAK2 inhibitor, wherein the JAK1 and/or JAK2 inhibitor comprises one or more isotopes.

### Claim 2 (depends on 1)

The method of claim 1, wherein the JAK1 and/or JAK2 inhibitor is selected from ruxolitinib (INCB018424), filgotinib (GLPG0634), Tyrphostin B42 (AG490), momelotinib (CYT387), pacritinib (SB1518), baricitinib (LY3009104), AZD1480, fedratinib (TG101348), BMS-911543, and lestaurtinib (CEP-701), a pharmaceutically acceptable salt thereof, or a combination thereof.

### Claim 3 (depends on 1)

The method of claim 1, wherein the hair loss disorder is androgenetic alopecia, telogen effluvium, tinea capitis, patchy alopecia areata, alopecia totalis, hypotrichosis, hereditary hypotrichosis simplex, alopecia universalis, or a combination thereof.

### Claim 4 (depends on 1)

The method of claim 1, wherein the hair loss disorder is alopecia areata.

### Claim 5 (depends on 1)

The method of claim 1, wherein the hair loss disorder is patchy alopecia areata.

### Claim 6 (depends on 1)

The method of claim 1, wherein the hair loss disorder is alopecia totalis.

### Claim 7 (depends on 1)

The method of claim 1, wherein the hair loss disorder is alopecia universalis.

### Claim 8 (depends on 1)

The method of claim 1, wherein the hair loss disorder is androgenetic alopecia.

### Claim 9 (depends on 1)

The method of claim 1, wherein the JAK1 and/or JAK2 inhibitor is administered topically.

### Claim 10 (depends on 1)

The method of claim 1, wherein the JAK1 and/or JAK2 inhibitor is administered orally.

### Claim 11 (depends on 1)

The method of claim 1, wherein the JAK1 and/or JAK2 inhibitor is administered via a route selected from the group consisting of intra-muscular injection, intra-peritoneal injection, an infusion, intravenous, intradermal, subcutaneous, oral, inhalation, transdermal, topical, transmucosal, nasal, rectal, and a combination thereof.

### Claim 12 (depends on 1)

The method of claim 1, wherein the JAK1 and/or JAK2 inhibitor is administered in a pharmaceutical composition selected from the group consisting of a solution, suspension, capsule, tablet, pill, troche, nasal spray, suppository, ointment, salve, gel, or cream.

### Claim 13 (depends on 1)

The method of claim 1, wherein administering to the human occurs twice daily, daily, weekly, twice weekly, monthly, twice monthly, yearly, 1 time per week, 2 times per week, 3 times per week, 4 times per week, 5 times per week, 6 times per week, 7 times per week, 8 times per week, 9 times per week, 10 times per week, 11 times per week, 12 times per week, 13 times per week, or 14 times per week.

### Claim 14 (depends on 1)

The method of claim 1, wherein treating a hair loss disorder is by inducing hair growth.

### Claim 15 (depends on 1)

The method of claim 1, wherein the compound is suitable for nuclear magnetic resonance (NMR).

### Claim 16 (depends on 1)

The method of claim 1, wherein the one or more isotopes is a radioisotope.

### Claim 17 (depends on 1)

The method of claim 1, wherein the one or more isotopes are isotopes of carbon or hydrogen.

### Claim 18 (depends on 17)

The method of claim 17, wherein the hair loss disorder is patchy alopecia areata.

### Claim 19 (depends on 17)

The method of claim 17, wherein the hair loss disorder is alopecia totalis.

### Claim 20 (depends on 17)

The method of claim 17, wherein the hair loss disorder is alopecia universalis.

### Claim 21 (depends on 17)

The method of claim 17, wherein the JAK1 and/or JAK2 inhibitor is administered topically.

### Claim 22 (depends on 17)

The method of claim 17, wherein JAK1 and/or JAK2 inhibitor is administered orally.

### Claim 23 (depends on 17)

The method of claim 17, wherein the JAK1 and/or JAK2 inhibitor is suitable for NMR.

### Claim 24 (depends on 1)

The method of claim 1, wherein the effective amount of the JAK1 and/or JAK2 inhibitor administered to the subject is selected from about 0.0001 μg/kg body weight, about 0.00025 μg/kg body weight, about 0.0005 μg/kg body weight, about 0.00075 μg/kg body weight, about 0.001 μg/kg body weight, about 0.0025 μg/kg body weight, about 0.005 μg/kg body weight, about 0.0075 μg/kg body weight, about 0.01 μg/kg body weight, about 0.025 μg/kg body weight, about 0.05 μg/kg body weight, about 0.075 μg/kg body weight, about 0.1 μg/kg body weight, about 0.25 μg/kg body weight, about 0.5 μg/kg body weight, about 0.75 μg/kg body weight, about 1 μg/kg body weight, about 5 μg/kg body weight, about 10 μg/kg body weight, about 25 μg/kg body weight, about 50 μg/kg body weight, about 75 μg/kg body weight, about 100 μg/kg body weight, about 150 μg/kg body weight, about 200 μg/kg body weight, about 250 μg/kg body weight, about 300 μg/kg body weight, about 350 μg/kg body weight, about 400 μg/kg body weight, about 450 μg/kg body weight, about 500 μg/kg body weight, about 550 μg/kg body weight, about 600 μg/kg body weight, about 650 μg/kg body weight, about 700 μg/kg body weight, about 750 μg/kg body weight, about 800 μg/kg body weight, about 850 μg/kg body weight, about 900 μg/kg body weight, about 950 μg/kg body weight, about 1000 μg/kg body weight, about 2000 μg/kg body weight, about 3000 μg/kg body weight, about 4000 μg/kg body weight, about 5000 μg/kg body weight, about 6000 μg/kg body weight, about 7000 μg/kg body weight, about 8000 μg/kg body weight, about 95000 μg/kg body weight, or about 10,000 μg/kg body weight, about 1 mg/kg body weight, about 1.5 mg/kg body weight, about 2 mg/kg body weight, about 2.5 mg/kg body weight, about 3 mg/kg body weight, about 3.5 mg/kg body weight, about 4 mg/kg body weight, about 4.5 mg/kg body weight, about 5 mg/kg body weight, about 5.5 mg/kg body weight, about 6 mg/kg body weight, about 6.5 mg/kg body weight, about 7 mg/kg body weight, about 7.5 mg/kg body weight, about 8 mg/kg body weight, about 9.5 mg/kg body weight, about 10 mg/kg body weight, about 10.5 mg/kg body weight, about 11.0 mg/kg body weight, about 11.5 mg/kg body weight, about 12 mg/kg body weight, about 12.5 mg/kg body weight, about 13 mg/kg body weight, about 13.5 mg/kg body weight, about 14 mg/kg body weight, about 14.5 mg/kg body weight, about 15 mg/kg body weight, about 15.5 mg/kg body weight, about 16 mg/kg body weight, about 16.5 mg/kg body weight, about 17 mg/kg body weight, about 17.5 mg/kg body weight, about 18 mg/kg body weight, about 19.5 mg/kg body weight, about 20 mg/kg body weight, about 21.5 mg/kg body weight, about 22 mg/kg body weight, about 22.5 mg/kg body weight, about 23 mg/kg body weight, about 23.5 mg/kg body weight, about 24 mg/kg body weight, about 24.5 mg/kg body weight, about 25 mg/kg body weight, about 25.5 mg/kg body weight, about 26 mg/kg body weight, about 26.5 mg/kg body weight, about 27 mg/kg body weight, about 27.5 mg/kg body weight, about 28 mg/kg body weight, about 29.5 mg/kg body weight, or about 30 mg/kg body weight.

### Claim 25 (depends on 1)

The method of claim 1, wherein administering to the subject occurs for at least 1 week.