IP Library Granted Patent US 11,718,602
Granted Patent B2
US 11,718,602 · App. 17/883,006 · Granted Aug 8, 2023

EGFR inhibitors

Inventors: Natasja Brooijmans (Cambridge, MA); Jason D. Brubaker (Cambridge, MA); John Emmerson Campbell (Cambridge, MA); Christopher De Savi (Cambridge, MA); Thomas A. Dineen (Cambridge, MA); Meredith Suzanne Eno (Cambridge, MA); Joseph L. Kim (Cambridge, MA); Aysegul Ozen (Cambridge, MA); Emanuele Perola (Cambridge, MA); Brett D. Williams (Cambridge, MA); Douglas Wilson (Cambridge, MA); Kevin J. Wilson (Cambridge, MA)
Assignee: Blueprint Medicines Corporation
C07D401/14C07D471/04C07D471/08C07D491/048C07D491/107C07D491/113C07D498/08C07D519/00C07B2200/05C07B2200/07
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Quick Facts
Patent No.
US 11,718,602
App. No.
17/883,006
Granted
Aug 8, 2023
Kind
B2
Abstract

The present disclosure provides a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof useful for treating a cancer.

Claims (22)

1. A compound of Formula (II-A):

or a pharmaceutically acceptable salt thereof, wherein:

Z is O;

R is H, halogen, or CH 3 ;

Ring A is piperidinyl optionally substituted with 1-6 R 1 ;

each R 1 is independently halogen, CN, OH, NR a R b , C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 3 -C 6 cycloalkyl or —O-C 3 -C 6 cycloalkyl, wherein the alkyl, alkoxy or cycloalkyl represented by R 1 or in the group represented by R 1 is optionally substituted with 1 to 3 groups selected from deuterium, halogen, OH, NR a R b , C 1 -C 2 alkyl, and C 1 -C 2 alkoxy;

m is 0, 1, 2, 3, 4, 5, or 6;

R 2 is H or isopropyl;

R 4 is H or methyl;

R 5 is H; C 1 -C 4 alkyl optionally substituted with 1 to 3 three groups selected from halogen, CN, and NR a R b ; C 3 -C 6 cycloalkyl; or 4-6 membered monocyclic heterocyclyl optionally substituted with C 1 -C 4 alkyl;

R 6 is H, CH3, or CH2NH2; and

wherein R a and R b are each independently selected from H, methyl and ethyl.

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein m is 1, 2, 3, 4, or 5; and

each R 1 is independently halogen, CN, OH, NR a R b , C 1 -C 4 alkyl, C 1 -C 4 alkoxy, —O-C 3 -C 6 cycloalkyl, wherein the alkyl, alkoxy, or cycloalkyl represented by R 1 or in the group represented by R 1 is optionally substituted with 1 to 3 groups selected from deuterium, halogen, OH, NR a R b , C 1 -C 2 alkyl, and C 1 -C 2 alkoxy.

3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein at least one R 1 is OH, C 1 -C 4 alkoxy, or —O-C 3 -C 6 cycloalkyl, wherein the alkoxy or cycloalkyl represented by R 1 or in the group represented by R 1 is optionally substituted with 1 to 3 groups selected from deuterium, halogen, OH, NR a R b , C 1 -C 2 alkyl, and C 1 -C 2 alkoxy.

4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein each R 1 is independently F, CN, OH, NH 2 , CH 3 , CH 2 CH 3 , CHF 2 , CH(OH)CH 3 , CH 2 OH, CH 2 NH 2 , CH 2 CH 2 NH 2 , OCH 3 , OCD 3 , OCH 2 CH 2 OH, OCH 2 CH(OH)CH 3 , OCH 2 C(OH)(CH 3 ) 2 , OCH 2 CH 2 OCH 3 , OCH 2 CH 2 NH 2 , OCH 2 CH 2 NHCH 3 , OCH 2 CH 2 N(CH 3 ) 2 , —O- cyclopropyl, NHCH 3 , or N(CH 3 ) 2 .

5. The compound of claim 4 , or a pharmaceutically acceptable salt thereof, wherein

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

7. The compound of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

8. A compound, wherein the compound is:

or a pharmaceutically acceptable salt thereof.

Assignments (3)
RELEASE OF SECURITY INTEREST (REEL/FRAME 064748/0552) Recorded Jul 24, 2025
From: TAO TALENTS, LLC
To: BLUEPRINT MEDICINES CORPORATION
Reel/Frame 072249/0280 →
SECURITY INTEREST Recorded Aug 29, 2023
From: BLUEPRINT MEDICINES CORPORATION
To: TAO TALENTS, LLC
Reel/Frame 064748/0552 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2022
From: BROOIJMANS, NATASJA; BRUBAKER, JASON D.; CAMPBELL, JOHN EMMERSON; DE SAVI, CHRISTOPHER; DINEEN, THOMAS A.; ENO, MEREDITH SUZANNE; KIM, JOSEPH L.; OZEN, AYSEGUL; PEROLA, EMANUELE; WILLIAMS, BRETT D.; WILSON, DOUGLAS; WILSON, KEVIN J.
To: BLUEPRINT MEDICINES CORPORATION
Reel/Frame 061025/0178 →
Continuity (4)
Continuation 17514457 · Oct 29, 2021
Continuation PCTUS2020066629 · Dec 22, 2020
Provisional Application 62953030 · Dec 23, 2019
Related Publication 20230026209A1 · Jan 26, 2023
Cited By (1)
US 12,655,129