# US 10,370,387 B2 · Tricyclic fused thiophene derivatives as JAK inhibitors

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- Number: US 10,370,387 B2
- Document ID: US10370387B2
- Status: Granted
- Kind: B2
- Application number: 15/874,140
- Filed: 2018-01-18
- Published: 2018-05-31
- Granted: 2019-08-06
- Earliest claimed: 2012-11-01
- Assignees: Incyte Holdings Corporation; Incyte Corporation
- Applicants: Incyte Corporation; Incyte Holdings Corporation
- Inventors: Yun-Long Li; Wenyu Zhu; Song Mei
- Web page: https://patentgrep.com/patent/US10370387B2

## CPC

- C07D 495/14: Ortho-condensed systems
- 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 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 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 13/12: of the kidneys
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 17/10: Anti-acne agents
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/10: for osteoporosis
- A61P 21/04: for myasthenia gravis
- A61P 25/00: Drugs for disorders of the nervous system
- 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 37/06: 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 495/12: in which the condensed system contains three hetero rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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 invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

## Claims

### Claim 1

A method of ameliorating or inhibiting an autoimmune disease in a patient, comprising administering to said patient a compound, which is ((2R,5S)-5-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl}tetrahydro-2H-pyran-2-yl)acetonitrile, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the compound is ((2R,5S)-5-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl}tetrahydro-2H-pyran-2-yl)acetonitrile monohydrate.

### Claim 3 (depends on 1)

The method of claim 1, wherein the autoimmune disease is multiple sclerosis.

### Claim 4 (depends on 1)

The method of claim 1, wherein the autoimmune disease is rheumatoid arthritis.

### Claim 5 (depends on 1)

The method of claim 1, wherein the autoimmune disease is type I diabetes.

### Claim 6 (depends on 1)

The method of claim 1, wherein the autoimmune disease is lupus.

### Claim 7 (depends on 6)

The method of claim 6, wherein the lupus is systemic lupus erythematosus.

### Claim 8 (depends on 1)

The method of claim 1, wherein the autoimmune disease is Crohn's disease.

### Claim 9 (depends on 1)

The method of claim 1, wherein the autoimmune disease is ulcerative colitis.

### Claim 10 (depends on 1)

The method of claim 1, wherein the autoimmune disease is myasthenia gravis.

### Claim 11 (depends on 1)

The method of claim 1, wherein the autoimmune disease is psoriasis.

### Claim 12 (depends on 1)

The method of claim 1, wherein the autoimmune disease is pemphigus vulgaris.

### Claim 13 (depends on 1)

The method of claim 1, wherein the autoimmune disease is asthma.

### Claim 14

A method of ameliorating or inhibiting allograft rejection or graft versus host disease in a patient, comprising administering to said patient a compound, which is ((2R,5S)-5-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl }tetrahydro-2H-pyran-2-yl)acetonitrile, or a pharmaceutically acceptable salt thereof.

### Claim 15 (depends on 14)

The method of claim 14, wherein the compound is ((2R,5S)-5-{2-[(1R)-1-hydroxyethyl]-1H-imidazo[4,5-d]thieno[3,2-b]pyridin-1-yl}tetrahydro-2H-pyran-2-yl)acetonitrile monohydrate.