IP Library Granted Patent US 8,946,235
Granted Patent B2
US 8,946,235 · App. 13/557,871 · Granted Feb 3, 2015

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

Inventors: Sam Butterworth (Cheshire, GB); Maurice Raymond Verschoyle Finlay (Cheshire, GB); Richard Andrew Ward (Cheshire, GB); Heather Marie Redfearn (Cheshire, GB)
Assignee: AstraZeneca AB
C07D401/02C07D403/04C07D471/04
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Quick Facts
Patent No.
US 8,946,235
App. No.
13/557,871
Granted
Feb 3, 2015
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 said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using such compounds and salts thereof.

Claims (12)

1. A compound, or a pharmaceutically acceptable salt thereof, wherein the compound is N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide.

2. A pharmaceutical composition, which comprises the compound according to claim 1 , or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically-acceptable diluent or carrier.

3. 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 claim 1 , or a pharmaceutically acceptable salt thereof.

4. A compound, wherein the compound is N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide.

5. A pharmaceutical composition, which comprises the compound according to claim 4 , in association with a pharmaceutically-acceptable diluent or carrier.

6. 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 claim 4 .

7. A mesylate salt of N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yppyrimidin-2-yl]amino}phenyl)prop-2-enamide.

8. A pharmaceutical composition, which comprises the mesylate salt according to claim 7 , in association with a pharmaceutically-acceptable diluent or carrier.

9. 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 mesylate salt of claim 7 .

10. The method of claim 3 , wherein the lung cancer is non-small cell lung cancer.

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

12. The method of claim 9 , wherein the lung cancer is non-small cell lung cancer.

Assignments (7)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 9, 2013
From: CHUAQUI, CLAUDIO EDMUNDO
To: ASTRAZENECA PHARMACEUTICALS LP
Reel/Frame 031740/0044 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 9, 2013
From: ASTRAZENECA PHARMACEUTICALS LP
To: ASTRAZENECA UK LIMITED
Reel/Frame 031740/0084 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 9, 2013
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 031740/0127 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2012
From: MURUGAN, CHANDRASHEKAR REDDY C; MURUGAN, ANDIAPPAN; KADAMBAR, VASANTHA KRISHNA
To: ASTRAZENECA INDIA PRIVATE LIMITED
Reel/Frame 029294/0350 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2012
From: ASTRAZENECA INDIA PRIVATE LIMITED
To: ASTRAZENECA AB
Reel/Frame 029294/0400 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2012
From: BUTTERWORTH, SAM; FINLAY, MAURICE RAYMOND VERSCHOYLE; WARD, RICHARD ANDREW; REDFEARN, HEATHER MARIE
To: ASTRAZENECA UK LIMITED
Reel/Frame 029294/0557 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2012
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 029294/0594 →
Continuity (3)
Provisional Application 61512061 · Jul 27, 2011
Provisional Application 61591363 · Jan 27, 2012
Related Publication 20130053409A1 · Feb 28, 2013