IP Library Granted Patent US 8,324,225
Granted Patent B2
US 8,324,225 · App. 12/302,223 · Granted Dec 4, 2012

Pyrrolopyrimidine compounds and their uses

Assignees: Novartis AG; Astex Therapeutics Limited
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Quick Facts
Patent No.
US 8,324,225
App. No.
12/302,223
Granted
Dec 4, 2012
Kind
B2
Abstract

The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.

Claims (25)

1. A compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

the dashed line indicates a double bond;

A is N;

R 2 is hydrogen and R 3 is selected from the group consisting of hydrogen, hydroxyl, C 1 -C 3 -alkyl, C 3 -C 8 -cycloalkyl, heterocyclyl, aryl, heteroaryl, substituted C 1 -C 3 -alkyl, substituted C 3 -C 8 -cycloalkyl, substituted heterocyclyl, substituted aryl and substituted heteroaryl;

R 4 is selected from the group consisting of hydrogen, branched C 1 -C 5 -alkyl, branched C 1 -C 5 -alkyl substituted by phenyl and C 3 -C 6 -cycloalkyl;

X is CR 11 and Y is CR 12 ;

R 11 is hydrogen or C 1 -C 3 -alkyl and

R 12 is BC(O)NR 13 R 14 ; wherein B is a bond, C 1 -C 3 -alkyl or branched C 1 -C 3 -alkyl; wherein R 13 and R 14 are each, independently, selected from the group consisting of hydrogen, C 1 -C 3 -alkyl, C 3 -C 8 -cycloalkyl, heterocyclyl, aryl, heteroaryl, substituted alkyl, substituted cycloalkyl, substituted heterocyclyl, substituted aryl, and substituted heteroaryl.

2. The compound of claim 1 , wherein R 4 is C(H)(CH 2 CH 3 ) 2 , C(H)(CH 2 CH 3 )Ph, CH 2 CH 3 , cyclopropyl, cyclopentyl or cyclohexyl.

3. The compound of claim 1 , wherein R 3 is an aryl group, which is further independently substituted one or more times by halogen, C 1 -C 4 -alkoxy, R 15 -amine, R 15 -heterocycle, or R 15 -heteroaryl, wherein R 15 is a bond, C(O), N(H)C(O), N(H)SO 2 , OC(O) or (CH 2 ) 1-4 , wherein the (CH 2 ) 1-4 group may be interrupted by O, N(CH 3 ) or N(H).

4. The compound of claim 3 , wherein the aryl group is phenyl.

5. The compound of claim 1 , wherein the phenyl group is R 3 is phenyl which is further independently substituted one or more times with fluoro, methoxy, diethylamine, R 15 -piperazinyl, R 15 -morpholinyl, R 15 -piperidinyl, R 15 -triazolyl, R 15 -phenyl, R 15 -pyridinyl, R 15 -piperazinyl, R 15 -indazolyl, R 15 -pyrrolidinyl or R 15 -imidazolyl, wherein the piperazinyl, morpholinyl, piperidinyl, triazolyl, phenyl, pyridinyl, piperazinyl, indazolyl, pyrrolidinyl or imidazolyl groups may be further substituted with C 1 -C 4 -alkyl, C(O)C 1 -C 4 -alkyl, S(O) 2 C 1 -C 4 -alkyl, OH, C(O)(CH 2 ) 1-3 CN or N(H)C(O)C 1 -C 4 -alkyl and wherein R 15 is a bond, C(O), N(H)C(O), N(H)SO 2 , OC(O) or (CH 2 ) 1-4 , wherein the (CH 2 ) 1-4 group may be interrupted by O, N(CH 3 ) or N(H).

6. The compound of claim 1 , wherein R 3 is phenyl which is further substituted by N(H)C(O)aryl, C(O)N(H)C 1 -C 4 -alkyl, C(O)N(C 1 -C 4 -alkyl) 2 or C(O)N(H)C 3 -C 6 -cycloalkyl.

7. The compound of claim 1 , wherein the compound is selected from the group consisting of

8. A compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein:

the dashed line indicates a double bond;

A is N;

R 2 is hydrogen and R 3 is selected from the group consisting of hydrogen, hydroxyl, C 1 -C 3 -alkyl, C 3 -C 8 -cycloalkyl, heterocyclyl, aryl, heteroaryl, substituted C 1 -C 3 -alkyl, substituted C 3 -C 8 -cycloalkyl, substituted heterocyclyl, substituted aryl and substituted heteroaryl;

R 4 is branched or linear C 1 -C 5 -alkyl, wherein the branched C 1 -C 5 -alkyl group may be interrupted by one or more heteroatoms, and/or substituted with one or more heteroatoms, halogens, C 3 -C 8 cycloalkyl groups, substituted C 3 -C 8 cycloalkyl groups, C 3 -C 8 hetrocyclyl groups, aryl groups, heteroaryl groups, substituted aryl groups, or substituted heteroaryl groups;

X is CR 11 and Y is CR 12 ;

R 11 is hydrogen or C 1 -C 3 -alkyl and

R 12 is BC(O)NR 13 R 14 ; wherein B is a bond, C 1 -C 3 -alkyl or branched C 1 -C 3 -alkyl; wherein R 13 and R 14 are each, independently, selected from the group consisting of hydrogen, C 1 -C 3 -alkyl, C 3 -C 8 -cycloalkyl, heterocyclyl, aryl, heteroaryl, substituted alkyl, substituted cycloalkyl, substituted heterocyclyl, substituted aryl, and substituted heteroaryl.

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

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2021
From: NOVARTIS AG
To: NOVARTIS PHARMACEUTICALS CORPORATION
Reel/Frame 056549/0645 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 27, 2011
From: NOVARTIS AG
To: NOVARTIS AG; ASTEX THERAPEUTICS LIMITED
Reel/Frame 026658/0381 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2011
From: BRAIN, CHRISTOPHER THOMAS; THOMA, GEBHARD; SUNG, MOO JE
To: NOVARTIS AG
Reel/Frame 026579/0815 →
Continuity (2)
Provisional Application 60808605 · May 26, 2006
Related Publication 20090318441A1 · Dec 24, 2009