IP Library › Granted Patent US 9,732,058
Granted Patent B2
US 9,732,058 · App. 14/576,721 · Granted Aug 15, 2017

2-(2,4,5-substituted-anilino)pyrimidine compounds

Inventors: Sam Butterworth (Macclesfield, GB); Maurice Raymond Verschoyle Finlay (Macclesfield, GB); Richard Andrew Ward (Macclesfield, GB); Heather Marie Redfearn (Macclesfield, GB)
Assignee: ASTRAZENECA AB
C07D401/04C07D401/02C07D401/14C07D403/04C07D471/04C07D487/10
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Quick Facts
Patent No.
US 9,732,058
App. No.
14/576,721
Granted
Aug 15, 2017
Kind
B2
Abstract

The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising such compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of such compounds and to methods of treatment of diseases mediated by various different forms of EGFR using such compounds and salts thereof.

Claims (11)

1. A compound of Formula (I)

or a pharmaceutically acceptable salt thereof, wherein:

G is 1H-indol-3-yl or 1-methyl-1H-indol-3-yl;

R 1 is hydrogen;

R 2 is methoxy; and

R 3 is [2-(dimethylamino)ethyl](methyl)amino or [2-(methylamino)ethyl](methyl)amino.

2. The compound of Formula (I) as claimed in claim 1 which is: N-(2-[2-dimethylaminoethyl-methylamino]-5-{[4-(1H-indol-3-yl)pyrimidin-2-yl]amino}-4-methoxyphenyl)-prop-2-enamide or a pharmaceutically acceptable salt thereof.

3. The compound of Formula (I) as claimed in claim 1 which is: N-(4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}-2-[methyl-(2-methylaminoethyl)amino]-phenyl)prop-2-enamide or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition comprising a compound of Formula (I) as claimed in any one of claims 1 to 3 , or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically-acceptable diluent or carrier.

5. A method for treating lung cancer in a warm-blooded animal in need of such treatment, which comprises administering to said animal an effective amount of the compound of Formula (I) as claimed in any one of claims 1 to 3 , or a pharmaceutically acceptable salt thereof.

6. The method of claim 5 , wherein the lung cancer is non-small cell lung cancer.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2018
From: KADAMBAR, KRISHNA; REDDY C, CHANDRASEKHARA; MURUGAN, ANDIAPPAN
To: ASTRAZENECA INDIA PRIVATE LIMITED
Reel/Frame 046356/0295 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2018
From: CHUAQUI, CLAUDIO EDMUNDO
To: ASTRAZENECA PHARMACEUTICALS LP
Reel/Frame 046356/0482 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2018
From: BUTTERWORTH, SAM; FINLAY, MAURICE RAYMOND VERSCHOYLE; WARD, RICHARD ANDREW; REDFEARN, HEATHER MARIE
To: ASTRAZENECA UK LIMITED
Reel/Frame 046356/0573 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2018
From: ASTRAZENECA PHARMACEUTICALS LP
To: ASTRAZENECA UK LIMITED
Reel/Frame 046356/0675 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2018
From: ASTRAZENECA INDIA PRIVATE LIMITED
To: ASTRAZENECA AB
Reel/Frame 046356/0754 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2018
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 046547/0972 →
Continuity (4)
Division 13557871 · Jul 25, 2012
Provisional Application 61591363 · Jan 27, 2012
Provisional Application 61512061 · Jul 27, 2011
Related Publication 20150119379A1 · Apr 30, 2015