IP Library Granted Patent US 10,253,015
Granted Patent B2
US 10,253,015 · App. 15/964,812 · Granted Apr 9, 2019

Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors

Inventors: Jian Lin (Acton, MA); Anna Ericsson (Shrewsbury, MA); Ann-Marie Campbell (Monroe, CT); Gary Gustafson (Ridgefield, CT); Zhongguo Wang (Lexington, MA); R. Bruce Diebold (Waltham, MA); Susan Ashwell (Carlisle, MA); David R. Lancia, Jr. (Boston, MA); Justin Andrew Caravella (Cambridge, MA); Wei Lu (Newton, MA)
Assignee: FORMA TM2, INC.
C07D401/12C07D401/14C07D405/14C07D413/14C07D417/14A61K31/4704
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Quick Facts
Patent No.
US 10,253,015
App. No.
15/964,812
Granted
Apr 9, 2019
Kind
B2
Abstract

The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, U, V, Z, W 1 , W 2 , W 3 , and R 1 -R 6 are described herein.

Claims (25)

1. A compound of formula I:

or a pharmaceutically acceptable salt thereof,

wherein:

W 1 and W 2 are CH;

W 3 is CR 2 ;

U and V are independently N or CH, provided that U and V are not both N;

Z is C;

A is CN;

B is H or C 1 -C 6 alkoxy;

R 1 is halogen;

R 2 is H;

R 3 is H or D;

R 4 and R 5 are independently H or C 1 -C 3 alkyl; and

R 6 is H or C 1 -C 6 alkoxy.

2. The compound of claim 1 , wherein B is methoxy.

3. The compound of claim 2 , wherein R 4 is H and R 5 is methyl.

4. The compound of claim 3 , wherein R 4 is H and R 5 is (S)-methyl.

5. The compound of claim 4 , wherein R 1 is chloro.

6. The compound of claim 1 having the Formula Ia:

7. The compound of claim 1 having the Formula Ia-1:

8. The compound of claim 1 having the Formula Ib:

9. The compound of claim 8 having the Formula Ib-1:

10. A pharmaceutical composition comprising 6-{[(1S)-1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino}-4-methoxypyridine-3-carbonitrile, or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable carrier.

11. A mixture comprising (S)-3-(1-aminoethyl)-6-chloroquinolin-2(1H)-one hydrochloride and 6-chloro-4-methoxynicotinonitrile.

12. The mixture of claim 11 , further comprising 6-{[(1S)-1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino}-4-methoxypyridine-3-carbonitrile, or a pharmaceutically acceptable salt thereof.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2019
From: FORMA TM2, INC.
To: FORMA THERAPEUTICS, INC.
Reel/Frame 049598/0522 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 8, 2018
From: FORMA THERAPEUTICS, INC.
To: FORMA TM2, INC.
Reel/Frame 047457/0946 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 6, 2018
From: LIN, JIAN; ERICSSON, ANNA; CAMPBELL, ANN-MARIE; GUSTAFSON, GARY; WANG, ZHONGGUO; DIEBOLD, R. BRUCE; ASHWELL, SUSAN; LANCIA, DAVID R., JR.; CARAVELLA, JUSTIN ANDREW; LU, WEI
To: FORMA THERAPEUTICS, INC.
Reel/Frame 046564/0503 →
Continuity (6)
Continuation 15677748 · Aug 15, 2017
Continuation 14858170 · Sep 18, 2015
Provisional Application 62150819 · Apr 21, 2015
Provisional Application 62128089 · Mar 4, 2015
Provisional Application 62053006 · Sep 19, 2014
Related Publication 20180327382A1 · Nov 15, 2018
Cited By (1)
US 12,275,715