Pyrrolo[2,3-D]pyrimidinyl, pyrrolo[2,3-B]pyrazinyl, pyrrolo[2,3-B]pyridinyl acrylamides and epoxides thereof

Patent metadata

Field	Value
Publication number	US-10703756-B2
Application number	US-201615569874-A
Country	US
Kind code	B2
Filing date	Apr 19, 2016
Priority date	May 1, 2015
Publication date	Jul 7, 2020
Grant date	Jul 7, 2020

Abstract

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

First claim

What is claimed is:

1. The compound 2-{[(2S)-1-acryloylpyrrolidin-2-yl]methoxy}-N-[(2S)-1-methoxypropan-2-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide; or, a pharmaceutically acceptable salt thereof.

2. The compound 2-[(1-acryloylpiperidin-4-yl)amino]-N-(3-fluorobenzyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide; or, a pharmaceutically acceptable salt thereof.

3. The compound 2-[(1-acryloylpiperidin-4-yl)amino]-N-(2-cyclopropylethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide; or, a pharmaceutically acceptable salt thereof.

4. The compound 2-[(1-acryloylpiperidin-4-yl)amino]-N-benzyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide; or, a pharmaceutically acceptable salt thereof.

5. The compound 2-[(1-acryloylpiperidin-4-yl)oxy]-N-[(2R)-1-methoxypropan-2-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide; or a pharmaceutically acceptable salt thereof.

Assignees

• Pfizer

Inventors

• Thorarensen Atli
• Brown Matthew Frank
• Casimiro-Garcia Agustin
• Che Ye
• Flanagan Mark Edward
• Gilbert Adam Matthew
• Hayward Matthew Merrill
• Telliez Jean-Baptiste
• Unwalla Rayomand Jal
• Trujillo John I
• Liang Sidney Xi

Classifications

• Y02A50/30

  Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change · CPC title

• A61P37/02

  Immunomodulators · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P1/04

  for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants · CPC title

• C07D487/04 Primary

  Ortho-condensed systems · CPC title