# US 10,370,375 B2 · Heterocyclyl-substituted cyclohexylsulfonamides as JAK inhibitors

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- Number: US 10,370,375 B2
- Document ID: US10370375B2
- Status: Granted
- Kind: B2
- Application number: 16/055,560
- Filed: 2018-08-06
- Published: 2018-12-06
- Granted: 2019-08-06
- Earliest claimed: 2014-03-28
- Assignees: Elanco Tiergesundheit AG
- Applicants: Elanco Tiergesundheit AG
- Inventors: Noelle Gauvry; Chouaib Tahtaoui; Pascal Furet; Pierre Ducray
- Web page: https://patentgrep.com/patent/US10370375B2

## CPC

- C07D 471/14: Ortho-condensed systems
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/00: Drugs for disorders of the endocrine system
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/04: Antipruritics
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/14: Decongestants or antiallergics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 239/42: One nitrogen atom (nitro radicals C07D239/30)
- C07D 239/46: Two or more oxygen, sulphur or nitrogen atoms
- C07D 239/48: Two nitrogen atoms
- C07D 471/04: Ortho-condensed systems
- C07D 473/34: attached in position 6, e.g. adenine
- C07D 487/04: Ortho-condensed systems
- C07D 495/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to a compound of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful as therapeutic agent for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis. Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, inflammatory bowel diseases, Crohn's disease, Alzheimer's disease, leukemia, osteoarthritis, control of pruritus, chronic respiratory disease or keratoconjunctivitis in mammals.

## Claims

### Claim 1

A compound of formula
wherein
R is C1-C4-alkyl or C3-C5-cycloalkyl; and
A is a radical of formula
wherein R0 is H, C1-C4-alkyl, hydroxy-C1-C4-alkyl, C1-C4-alkoxy-C1-C4-alkyl or NH2;
or a veterinary acceptable salt thereof.

### Claim 2 (depends on 1)

The compound of claim 1 which is 1-[trans-4-((2-amino)imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl]-N-methylmethanesulfonamide and can be structurally represented as
or a veterinary acceptable salt thereof.

### Claim 3 (depends on 1)

A pharmaceutical composition comprising a compound according to claim 1 or a veterinary acceptable salt thereof, and a pharmaceutical acceptable carrier.

### Claim 4 (depends on 1)

A method of treating atopic dermatitis, eczema, psoriasis, scleroderma, pruritus and other pruritic conditions, or allergic dermatitis, the method comprising administering to a mammal in need thereof an effective amount of a compound according to claim 1 or a veterinary acceptable salt thereof.

### Claim 5 (depends on 4)

The method according to claim 4, wherein the mammal is a dog.