IP Library Granted Patent US 10,000,507
Granted Patent B2
US 10,000,507 · App. 15/379,783 · Granted Jun 19, 2018

Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors

Inventors: Yun-Long Li (Chadds Ford, PA); David M. Burns (Glen Mills, PA); Hao Feng (Glen Mills, PA); Taisheng Huang (Wilmington, DE); Song Mei (Wilmington, DE); Jun Pan (Media, PA); Hai-Fen Ye (Newark, DE); Wenyu Zhu (Media, PA); Maria Rafalski (Greenville, DE); Anlai Wang (Wilmington, DE); Chu-Biao Xue (Hockessin, DE)
Assignee: Incyte Corporation
C07D495/04C07D491/048
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,000,507
App. No.
15/379,783
Granted
Jun 19, 2018
Kind
B2
Abstract

The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as 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 (28)

1. The compound of Formula (II-6):

or a pharmaceutically acceptable salt thereof, wherein:

n RA is 0;

Cy B is a 3-aminopiperidin-1-yl, wherein said piperidinyl is optionally substituted with 1, 2, 3, or 4 R B ;

each R B is independently selected from halogen, C 1-6 alkyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, CN, OR a2 and NR c2 R d2 ;

R 5 is H, halogen, or C 1-6 alkyl;

R 6 is H, halogen, R 6A , C 1-6 haloalkyl, CN, or OR a4 ;

R 6A is unsubstituted phenyl or phenyl 2,6-disubstituted with substituents independently selected from C 1-6 alkyl, halogen, CN and OR a4 ;

R 7 is H, halogen, C 1-6 alkyl, C 1-6 haloalkyl or O(C 1-6 alkyl);

R a2 , R c2 and R d2 are each independently selected from H, C 1-6 alkyl, C 2-6 alkenyl and C 2-6 alkynyl; and

R a4 is H or C 1-6 alkyl.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the configuration of the carbon atom at the 3-position of the piperidin-1-yl ring forming Cy B is (S).

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the configuration of the carbon atom at the 3-position of the piperidin-1-yl ring forming Cy B is (R).

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Cy B is a group selected from groups of the following Formulae (B-101) to (B-107):

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Cy B is a group selected from groups of the following Formulae (B-115) to (B-121):

6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Cy B is a group of Formula (B-3a):

7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R B is independently selected from methyl, ethyl, cyclopropyl, CF 3 , OH and NH 2 .

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 5 is H, Cl or methyl.

9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 5 is H.

10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 6 is H.

11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 6 is R 6A .

12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 7 is H, Cl, methyl, ethyl, CF 3 , OMe, OEt, On-Pr, or Oi-Pr.

13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 7 is H.

14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein each R a2 , R c2 , and R d2 is independently selected from H and C 1-6 alkyl.

15. The compound of claim 1 , wherein the compound is 2-amino-N-{4-[(3S,5R)-3-amino-5-methylpiperidin-1-yl]pyridin-3-yl}-6-(2,6-difluorophenyl)furo[3,2-b]pyridine-3-carboxamide, or a pharmaceutically acceptable salt thereof.

16. The compound of claim 1 , wherein the compound is 2-amino-N-{4-[(3S,5R)-3-amino-5-methylpiperidin-1-yl]pyridin-3-yl}-6-(2,6-difluorophenyl)furo[3,2-b]pyridine-3-carboxamide.

17. A composition comprising a compound of claim 15 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

18. A composition comprising a compound of claim 16 , and at least one pharmaceutically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2021
From: INCYTE CORPORATION
To: INCYTE CORPORATION; INCYTE HOLDINGS CORPORATION
Reel/Frame 058815/0857 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 7, 2017
From: LI, YUN-LONG; BURNS, DAVID M.; FENG, HAO; HUANG, TAISHENG; MEI, SONG; PAN, JUN; VECHORKIN, OLEG; YE, HAI-FEN; ZHU, WENYU; RAFALSKI, MARIA; WANG, ANLAI; XUE, CHU-BIAO
To: INCYTE CORPORATION
Reel/Frame 043219/0296 →
Continuity (3)
Continuation 14465910 · Aug 22, 2014
Provisional Application 61869442 · Aug 23, 2013
Related Publication 20170190716A1 · Jul 6, 2017