Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors

• US 10,639,310 B2
• Filed: 11/01/2018
• Issued: 05/05/2020
• Est. Priority Date: 12/13/2005
• Status: Active Grant

• Current Assignee: Incyte Corporation, Incyte Holdings Corporation (Incyte Corporation)
• Original Assignee: Incyte Corporation
• Inventors: Rodgers, James D., Shepard, Stacey
• Primary Examiner(s): Moore, Susanna
• Application Number:
  US16/177,602
• Publication Number:
  US 20190125750A1
• Time in Patent Office: 551 Days
• Field of Search: 544280, 5142651
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: 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
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/20 Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61P 17/04 Antipruritics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 35/04 specific for metastasis
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: C07B 2200/05 Isotopically modified compounds, e.g. labelled
• CPC Class Codes: C07B 59/002 Heterocyclic compounds
• CPC Class Codes: C07D 417/04 directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 471/04 Ortho-condensed systems
• CPC Class Codes: C07D 487/04 Ortho-condensed systems

Abstract

The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Claims

1. A method of treating atopic dermatitis in a patient in need thereof, comprising administering to the skin of said patient a therapeutically effective amount of a compound, which is 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, wherein the treating refers to ameliorating or inhibiting atopic dermatitis in the patient.

2. The method of claim 1, wherein said compound or salt is administered in the form of a pharmaceutical composition suitable for skin administration, comprising said compound or salt and a pharmaceutically acceptable carrier.

3. A method of treating atopic dermatitis in a patient in need thereof, comprising administering to the skin of said patient a therapeutically effective amount of (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, wherein the treating refers to ameliorating or inhibiting atopic dermatitis in the patient.

4. The method of claim 3, wherein said compound or salt is administered in the form of a pharmaceutical composition suitable for skin administration, comprising said compound or salt and a pharmaceutically acceptable carrier.

5. A method of treating atopic dermatitis in a patient in need thereof, comprising administering to the skin of said patient a therapeutically effective amount of a pharmaceutically acceptable salt of (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, wherein the treating refers to ameliorating or inhibiting atopic dermatitis in the patient.

6. The method of claim 5, wherein said salt is administered in the form of a pharmaceutical composition suitable for skin administration, comprising said salt and a pharmaceutically acceptable carrier.