IP Library Granted Patent US 11,753,404
Granted Patent B2
US 11,753,404 · App. 17/226,531 · Granted Sep 12, 2023

Aminothiazole compounds as c-Kit inhibitors

Inventors: Nicholas E. Bencivenga (Cambridge, MA); David C. Dalgarno (Cambridge, MA); Joseph M. Gozgit (Cambridge, MA); Wei-Sheng Huang (Cambridge, MA); Anna Kohlmann (Cambridge, MA); Feng Li (Cambridge, MA); Jiwei Qi (Cambridge, MA); William C. Shakespeare (Cambridge, MA); Ranny M. Thomas (Cambridge, MA); Yihan Wang (Cambridge, MA); Xiaotian Zhu (Cambridge, MA)
Assignee: Ariad Pharmaceuticals, Inc.
C07D417/14C07D277/46C07D417/04C07D417/12
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Quick Facts
Patent No.
US 11,753,404
App. No.
17/226,531
Granted
Sep 12, 2023
Kind
B2
Abstract

The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: wherein A, L, R 1 , R 2 , R 3 , and n are described herein.

Claims (12)

1. A compound having one of the following formulae (Ig) or (Ih):

or a pharmaceutically acceptable salt thereof, wherein

R 1 is H;

R 2 is —C(O)NR 9 R 10 ;

R 3 is (C 1 -C 6 ) alkyl or halogen;

R 4 is (C 1 -C 6 ) haloalkyl;

R 5 is H;

R 9 and R 10 together with the nitrogen atom to which they are attached form a 4- to 6-membered heterocycloalkyl ring comprising 1 to 3 heteroatom selected from N, O, and S, optionally substituted with one or more substituents each independently selected from (C 1 -C 6 ) alkyl, (C 1 -C 6 ) hydroxyalkyl, -(CH 2 ) q —(C 1 -C 6 ) dialkylamino, —C(O)(C 1 -C 6 ) alkyl, OH, or 6-membered heterocycloalkyl comprising 1 to 3 heteroatom selected from N, O, and S, and optionally substituted with (C 1 -C 6 ) alkyl; and

q is 0, 1 or 2.

2. The compound of claim 1 , wherein R 4 is CF 3 .

3. The compound of claim 1 , wherein R 3 is methyl.

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

Assignments (2)
MERGER Recorded Jan 7, 2025
From: ARIAD PHARMACEUTICALS, INC.
To: TAKEDA PHARMACEUTICALS U.S.A., INC.
Reel/Frame 069769/0320 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 2, 2021
From: BENCIVENGA, NICHOLAS E.; DALGARNO, DAVID C.; GOZGIT, JOSEPH M.; HUANG, WEI-SHENG; KOHLMANN, ANNA; LI, FENG; QI, JIWEI; SHAKESPEARE, WILLIAM C.; THOMAS, RANNY M.; WANG, YIHAN; ZHU, XIAOTIAN
To: ARIAD PHARMACEUTICALS, INC.
Reel/Frame 056747/0386 →
Continuity (3)
Continuation 16469517
Provisional Application 62434845 · Dec 15, 2016
Related Publication 20220033392A1 · Feb 3, 2022