IP Library Granted Patent US 10,221,154
Granted Patent B2
US 10,221,154 · App. 15/222,523 · Granted Mar 5, 2019

Inhibitors of the fibroblast growth factor receptor

Inventors: Neil Bifulco, Jr. (Sudbury, MA); Lucian V. DiPietro (Gloucester, MA); Brian L. Hodous (Cambridge, MA); Chandrasekhar V. Miduturu (Cambridge, MA)
Assignee: BLUEPRINT MEDICINES CORPORATION
C07D401/04C07D235/30C07D239/84C07D401/12C07D403/12C07D403/14C07D405/12C07D409/12C07D471/04C07D475/00
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Quick Facts
Patent No.
US 10,221,154
App. No.
15/222,523
Granted
Mar 5, 2019
Kind
B2
Abstract

Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

Claims (18)

1. A compound of Formula II or a pharmaceutically acceptable salt thereof:

wherein:

ring A is a tetrahydrofuranyl or tetrahydropyranyl;

R 1 is halo, cyano, C 1-6 alkoxy, hydroxy, oxo, amino, amido, or C 1-6 alkyl;

each R 2 is, independently, halo or C 1-6 alkoxy;

R 3 is halo; and

m is 0-1;

n is 1-4; and

p is 0.

2. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein ring A is tetrahydrofuranyl.

3. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein ring A is tetrahydropyranyl.

4. A compound selected from the compounds below or a pharmaceutically acceptable salt thereof:

5. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein the portion of the compound represented by

6. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein n is 4.

7. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein m is 0.

8. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein ring A is tetrahydropyranyl and m is 0.

9. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of claim 1 or a pharmaceutically acceptable salt thereof.

10. A method of treating a hepatocellular carcinoma mediated by FGFR-4, the method comprising administering to a subject in need thereof a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

Assignments (4)
RELEASE OF SECURITY INTEREST (REEL/FRAME NUMBER 060616/0923) Recorded Jul 23, 2025
From: TAO TALENTS, LLC
To: BLUEPRINT MEDICINES CORPORATION
Reel/Frame 072193/0847 →
SECURITY INTEREST Recorded Jul 8, 2022
From: BLUEPRINT MEDICINES CORPORATION
To: TAO TALENTS, LLC
Reel/Frame 060616/0923 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 9, 2018
From: BIFULCO, NEIL, JR; DIPIETRO, LUCIAN V.; HODOUS, BRIAN L.; MIDUTURU, CHANDRASEKHAR V.
To: BLUEPRINT MEDICINES CORPORATION
Reel/Frame 046512/0756 →
ASSIGNEE CHANGE OF ADDRESS Recorded Jul 9, 2018
From: BLUEPRINT MEDICINES CORPORATION
To: BLUEPRINT MEDICINES CORPORATION
Reel/Frame 046513/0149 →
Continuity (4)
Continuation 14521909 · Oct 23, 2014
Provisional Application 61927782 · Jan 15, 2014
Provisional Application 61895472 · Oct 25, 2013
Related Publication 20170174652A1 · Jun 22, 2017
Cited By (4)
US 12,448,366 US 12,539,303 US 12,655,128 US 12,692,251