# US 11,992,481 B2 · Use of 2-substituted indazoles for the treatment and prophylaxis of autoimmune diseases

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- Number: US 11,992,481 B2
- Document ID: US11992481B2
- Status: Granted
- Kind: B2
- Application number: 17/673,644
- Filed: 2022-02-16
- Published: 2022-08-11
- Granted: 2024-05-28
- Earliest claimed: 2016-06-01
- Assignees: Bayer Pharma Aktiengesellschaft
- Applicants: Bayer Pharma Aktiengesellschaft
- Inventors: Alexandra Rausch; Stefan Joachim Jodl; Jörn Krätzschmar; Ulrich Bothe; Nicole Schmidt
- Web page: https://patentgrep.com/patent/US11992481B2

## CPC

- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- 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 relates to substituted indazoles, to the use thereof alone or in combinations for treatment and/or prophylaxis of autoimmune disorders, and to the use thereof for production of medicaments for treatment and/or prophylaxis of autoimmune disorders, especially for treatment and/or prophylaxis of arthritides (especially psoriatic arthritis, rheumatoid arthritis, Bekhterev's disease, reactive arthritis, systematic juvenile idiopathic arthritis), systematic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, allergic eczema and chronic-inflammatory bowel disorders (especially Crohn's disease and ulcerative colitis).

## Claims

### Claim 1

A method of treating multiple sclerosis, in a subject in need thereof, comprising:
administering to the subject an effective amount of a compound, wherein the compound is:
N-[2-(3-Hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2H-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide; or
N-{6-(2-Hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2H-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide,
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the compound is N-[2-(3-Hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2H-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

The method of claim 1, wherein the compound is N-{6-(2-Hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2H-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

The method of claim 1, wherein the subject is a human subject.

### Claim 5 (depends on 1)

The method of claim 1, wherein the subject is an animal subject.

### Claim 6

A method of treating pain in a subject in need thereof, comprising:
administering to the subject an effective amount of a compound, wherein the compound is:
N-[2-(3-Hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2H-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide; or
N-{6-(2-Hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2H-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide,
or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 6)

The method of claim 6, wherein the pain is acute pain, chronic pain, inflammatory pain, or neuropathic pain, or any combination thereof.

### Claim 8 (depends on 6)

The method of claim 6, wherein the pain is hyperalgesia, allodynia, or lower back pain, or any combination thereof.

### Claim 9 (depends on 6)

The method of claim 6, wherein the compound is N-[2-(3-Hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2H-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

### Claim 10 (depends on 6)

The method of claim 6, wherein the compound is N-{6-(2-Hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2H-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

### Claim 11 (depends on 6)

The method of claim 6, wherein the subject is a human subject.

### Claim 12 (depends on 6)

The method of claim 6, wherein the subject is an animal.