IP Library Granted Patent US 10,266,495
Granted Patent B2
US 10,266,495 · App. 15/977,512 · Granted Apr 23, 2019

Phenyl 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.
C07D215/227A61K31/4709C07D401/12C07D405/12C07D409/12C07D471/04
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Quick Facts
Patent No.
US 10,266,495
App. No.
15/977,512
Granted
Apr 23, 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, W 1 , W 2 , W 3 , and R 1 -R 8 are described herein.

Claims (21)

1. A compound of formula I:

or pharmaceutically acceptable salt thereof,

wherein:

W 1 and W 2 are CH;

W 3 is CR 2 ;

A is CN;

B is H or C 1 -C 6 alkoxy;

R 1 is halogen;

R 2 is H;

R 3 is H;

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

R 6 , R 7 , and R 8 are independently 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:

or pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition comprising (S)-4-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-2-methoxybenzonitrile, or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable carrier.

8. A mixture comprising (S)-3-(1-aminoethyl)-6-chloroquinolin-2(1H)-one hydrochloride and 4-fluoro-2-methoxybenzonitrile.

9. The mixture of claim 8 , further comprising (S)-4-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-2-methoxybenzonitrile, or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable carrier.

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 046564/0525 →
Continuity (5)
Continuation 14858174 · Sep 18, 2015
Provisional Application 62206631 · Aug 18, 2015
Provisional Application 62128089 · Mar 4, 2015
Provisional Application 62053006 · Sep 19, 2014
Related Publication 20180327361A1 · Nov 15, 2018
Cited By (1)
US 12,275,715