IP Library Granted Patent US 10,517,858
Granted Patent B2
US 10,517,858 · App. 16/298,601 · Granted Dec 31, 2019

Thiazolecarboxamides and pyridinecarboxamide compounds useful as PIM kinase inhibitors

Inventors: Chu-Biao Xue (Hockessin, DE); Yun-Long Li (Chadds Ford, PA); Hao Feng (Glen Mills, PA); Ke Zhang (Wilmington, DE)
Assignees: Incyte Holdings Corporation; Incyte Corporation
A61K31/444C07D401/14C07D405/14C07D417/14C07D471/04C07D491/048C07D495/04
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Quick Facts
Patent No.
US 10,517,858
App. No.
16/298,601
Granted
Dec 31, 2019
Kind
B2
Abstract

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

Claims (23)

1. A method of inhibiting or ameliorating an immune disorder selected from multiple sclerosis, rheumatoid arthritis, allergy, food allergy, asthma, lupus, inflammatory bowel disease, and ulcerative colitis comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound wherein the compound is selected from:

N-{4-[3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;

N-{4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide;

N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide; and

N-{4-[(3R,4R,5S,7S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide; or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is N-{4-[3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the compound is N-{4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein the compound is N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 , wherein the compound is N-{4-[(3R,4R,5S,7S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

6. The method of claim 1 , wherein the immune disorder is multiple sclerosis.

7. The method of claim 1 , wherein the immune disorder is rheumatoid arthritis.

8. The method of claim 1 , wherein the immune disorder is asthma.

9. The method of claim 1 , wherein the immune disorder is lupus.

10. The method of claim 1 , wherein the immune disorder is inflammatory bowel disease.

11. The method of claim 1 , wherein the immune disorder is ulcerative colitis.

12. The method of claim 1 , wherein the immune disorder is food allergy.

13. The method of claim 1 , wherein the immune disorder is allergy.

14. A method of inhibiting or ameliorating multiple sclerosis comprising administering to a patient in need of such treatment a therapeutically effective amount of N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

15. A method of inhibiting or ameliorating inflammatory bowel disease comprising administering to a patient in need of such treatment a therapeutically effective amount of N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

16. A method of inhibiting or ameliorating rheumatoid arthritis comprising administering to a patient in need of such treatment a therapeutically effective amount of N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

17. A method of inhibiting or ameliorating asthma comprising administering to a patient in need of such treatment a therapeutically effective amount of N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

18. A method of inhibiting or ameliorating lupus comprising administering to a patient in need of such treatment a therapeutically effective amount of N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

19. A method of inhibiting or ameliorating ulcerative colitis comprising administering to a patient in need of such treatment a therapeutically effective amount of N-{4-[(3R,4R,5S,7R)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 28, 2019
From: XUE, CHU-BIAO; LI, YUN-LONG; FENG, HAO; PAN, JUN; WANG, ANLAI; ZHANG, KE; YAO, WENQING; ZHANG, FENGLEI; ZHUO, JINCONG
To: INCYTE CORPORATION
Reel/Frame 048726/0753 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 28, 2019
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 048726/0834 →
Continuity (8)
Continuation 15815255 · Nov 16, 2017
Continuation 15373923 · Dec 9, 2016
Continuation 14811038 · Jul 28, 2015
Continuation 14155212 · Jan 14, 2014
Provisional Application 61859118 · Jul 26, 2013
Provisional Application 61790952 · Mar 15, 2013
Provisional Application 61752897 · Jan 15, 2013
Related Publication 20190209537A1 · Jul 11, 2019