Claims for Patent: 8,324,225

Summary for Patent: 8,324,225

Title:	Pyrrolopyrimidine compounds and their uses
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.
Inventor(s):	Brain; Christopher Thomas (Cambridge, MA), Sung; Moo Je (Belmont, MA), Thoma; Gebhard (Lorrach, DE)
Assignee:	Novartis AG (Basel, CH) Astex Therapeutics Limited (Cambridge, GB)
Application Number:	12/302,223
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,324,225
Patent Claims:	1. A compound of Formula I: ##STR00653## or a pharmaceutically acceptable salt thereof, wherein: the dashed line indicates a double bond; A is N; R.sup.2 is hydrogen and R.sup.3 is selected from the group consisting of hydrogen, hydroxyl, C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.8-cycloalkyl, heterocyclyl, aryl, heteroaryl, substituted C.sub.1-C.sub.3-alkyl, substituted C.sub.3-C.sub.8-cycloalkyl, substituted heterocyclyl, substituted aryl and substituted heteroaryl; R.sup.4 is selected from the group consisting of hydrogen, branched C.sub.1-C.sub.5-alkyl, branched C.sub.1-C.sub.5-alkyl substituted by phenyl and C.sub.3-C.sub.6-cycloalkyl; X is CR.sup.11 and Y is CR.sup.12; R.sup.11 is hydrogen or C.sub.1-C.sub.3-alkyl and R.sup.12 is BC(O)NR.sup.13R.sup.14; wherein B is a bond, C.sub.1-C.sub.3-alkyl or branched C.sub.1-C.sub.3-alkyl; wherein R.sup.13 and R.sup.14 are each, independently, selected from the group consisting of hydrogen, C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.8-cycloalkyl, heterocyclyl, aryl, heteroaryl, substituted alkyl, substituted cycloalkyl, substituted heterocyclyl, substituted aryl, and substituted heteroaryl. 2. The compound of claim 1, wherein R.sup.4 is C(H)(CH.sub.2CH.sub.3).sub.2, C(H)(CH.sub.2CH.sub.3)Ph, CH.sub.2CH.sub.3, cyclopropyl, cyclopentyl or cyclohexyl. 3. The compound of claim 1, wherein R.sup.3 is an aryl group, which is further independently substituted one or more times by halogen, C.sub.1-C.sub.4-alkoxy, R.sup.15-amine, R.sup.15-heterocycle, or R.sup.15-heteroaryl, wherein R.sup.15 is a bond, C(O), N(H)C(O), N(H)SO.sub.2, OC(O) or (CH.sub.2).sub.1-4, wherein the (CH.sub.2).sub.1-4 group may be interrupted by O, N(CH.sub.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.sup.3 is phenyl which is further independently substituted one or more times with fluoro, methoxy, diethylamine, R.sup.15-piperazinyl, R.sup.15-morpholinyl, R.sup.15-piperidinyl, R.sup.15-triazolyl, R.sup.15-phenyl, R.sup.15-pyridinyl, R.sup.15-piperazinyl, R.sup.15-indazolyl, R.sup.15-pyrrolidinyl or R.sup.15-imidazolyl, wherein the piperazinyl, morpholinyl, piperidinyl, triazolyl, phenyl, pyridinyl, piperazinyl, indazolyl, pyrrolidinyl or imidazolyl groups may be further substituted with C.sub.1-C.sub.4-alkyl, C(O)C.sub.1-C.sub.4-alkyl, S(O).sub.2C.sub.1-C.sub.4-alkyl, OH, C(O)(CH.sub.2).sub.1-3CN or N(H)C(O)C.sub.1-C.sub.4-alkyl and wherein R.sup.15 is a bond, C(O), N(H)C(O), N(H)SO.sub.2, OC(O) or (CH.sub.2).sub.1-4, wherein the (CH.sub.2).sub.1-4 group may be interrupted by O, N(CH.sub.3) or N(H). 6. The compound of claim 1, wherein R.sup.3 is phenyl which is further substituted by N(H)C(O)aryl, C(O)N(H)C.sub.1-C.sub.4-alkyl, C(O)N(C.sub.1-C.sub.4-alkyl).sub.2 or C(O)N(H)C.sub.3-C.sub.6-cycloalkyl. 7. The compound of claim 1, wherein the compound is selected from the group consisting of ##STR00654## ##STR00655## ##STR00656## ##STR00657## ##STR00658## ##STR00659## ##STR00660## ##STR00661## 8. A compound of Formula I: ##STR00662## or a pharmaceutically acceptable salt thereof, wherein: the dashed line indicates a double bond; A is N; R.sup.2 is hydrogen and R.sup.3 is selected from the group consisting of hydrogen, hydroxyl, C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.8-cycloalkyl, heterocyclyl, aryl, heteroaryl, substituted C.sub.1-C.sub.3-alkyl, substituted C.sub.3-C.sub.8-cycloalkyl, substituted heterocyclyl, substituted aryl and substituted heteroaryl; R.sup.4 is branched or linear C.sub.1-C.sub.5-alkyl, wherein the branched C.sub.1-C.sub.5-alkyl group may be interrupted by one or more heteroatoms, and/or substituted with one or more heteroatoms, halogens, C.sub.3-C.sub.8 cycloalkyl groups, substituted C.sub.3-C.sub.8 cycloalkyl groups, C.sub.3-C.sub.8 hetrocyclyl groups, aryl groups, heteroaryl groups, substituted aryl groups, or substituted heteroaryl groups; X is CR.sup.11 and Y is CR.sup.12; R.sup.11 is hydrogen or C.sub.1-C.sub.3-alkyl and R.sup.12 is BC(O)NR.sup.13R.sup.14; wherein B is a bond, C.sub.1-C.sub.3-alkyl or branched C.sub.1-C.sub.3-alkyl; wherein R.sup.13 and R.sup.14 are each, independently, selected from the group consisting of hydrogen, C.sub.1-C.sub.3-alkyl, C.sub.3-C.sub.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.