| US 7,511,040 B2 | ||
| Imidazopyrazines as protein kinase inhibitors | ||
| David B. Belanger, Cambridge, Mass. (US); M. Arshad Siddiqui, Newton, Mass. (US); Timothy J. Guzi, Sudbury, Mass. (US); Patrick J. Curran, Winthrop, Mass. (US); Praveen K. Tadikonda, Norwood, Mass. (US); Blake Hamann, Linthicum, Md. (US); Panduranga Adulla P. Reddy, Walpole, Mass. (US); and Lianyun Zhao, Burlington, Mass. (US) | ||
| Assigned to Schering Corporation, Kenilworth, N.J. (US) | ||
| Filed on Nov. 07, 2007, as Appl. No. 11/936,380. | ||
| Claims priority of provisional application 60/858244, filed on Nov. 08, 2006. | ||
| Prior Publication US 2008/0139571 A1, Jun. 12, 2008 | ||
| Int. Cl. C07D 471/02 (2006.01) | ||
| U.S. Cl. 514—249 [544/350] | 17 Claims |
1. A compound of the formula:
 L is selected from the group consisting of S, S(O) and S(O)2;
G is alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, heteroaryl, heterocyclenyl or heterocyclyl, wherein each of said alkyl,
alkenyl, cycloalkyl, cycloalkenyl, aryl, heteroaryl, heterocyclenyl or heterocyclyl can be unsubstituted or optionally independently
substituted with one or more moieties which are independently selected from the group consisting of —OR5, halo, —CN, —C(O)NR5R6, —N(H)—C(O)R5,—N(H)—C(O)—NR5R6, S(O)2NR5R6, —NR5R6, —C(O)R5, —C(O)2R5, —SR5, —S(O)R5, —S(O)2R5;
R1 is H, halo, alkyl, aryl or heteroaryl, wherein each of said alkyl, aryl and heteroaryl can be unsubstituted or substituted
with one or more moieties which can be the same or different each moiety being independently selected from the group consisting
of halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, —C(O)NR5R6 and —OR5;
R2 is heteroaryl, wherein said heteroaryl can be unsubstituted or optionally independently substituted with one or more moieties
which can be the same or different, each moiety being independently selected from the group consisting of halo, alkyl, alkenyl,
alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, CF3, CN, —OCF3, —OR6, —C(O)R7, —NR5R6, —C(O)2R6, —C(O)NR5R6, —SR6, —S(O)2R7, —S(O)2NR5R6, —N(R5) —S(O)2R7, —N(R5)C(O)R7 and —N(R5)C(O)NR5R6;
R3 is heteroaryl, wherein said heteroaryl can be substituted or optionally substituted with one or more moieties which can be
the same or different, each moiety being independently selected from the group consisting of halo, alkyl, aryl, cycloalkyl,
CF3, CN, —OCF3, —OR5, —NR5R6, —C(O)2R5, —C(O)NR5R6, —SR6, —S(O)2R6, —S(O)2NR5R6, —N(R5)—S(O)2R7, —N(R5)C(O)R7 and —N(R5)C(O)NR5R6;
R5 is H, alkyl, aryl, heteroaryl, heterocyclyl or cycloalkyl; and
R6 is selected from the group consisting of H, alkyl, aryl, heteroaryl, arylalkyl- and heteroarylalkyl-, wherein each of said
alkyl, heteroarylalkyl, aryl, heteroaryl and arylalkyl can be unsubstituted or optionally substituted with one or more moieties
which can be the same or different, each moiety being independently selected from the group consisting of halogen, alkyl,
aryl, cycloalkyl, CF3, OCF3, CN, —OR5, —NR5R6, —CH2OR5, —C(O)2R5, —C(O)NR5R6, —SR6, —S(O)2R7, —S(O)2NR5R6, —N(R5)—S(O)2R7, —N(R5)C(O)R7 and —N(R5)C(O)NR5R6;
R7 is selected from the group consisting of alkyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl-, wherein each of said alkyl,
heteroarylalkyl, aryl, heteroaryl and arylalkyl can be unsubstituted or optionally substituted with one or more moieties which
can be the same or different, each moiety being independently selected from the group consisting of halogen, alkyl, aryl,
cycloalkyl, CF3, OCF3, CN, —OR5, —NR5R6, —CH2OR5, —C(O)2R5, —C(O)NR5R6, —SR6, —S(O)2)R7, —S(O)2NR5R6, —N(R5)—S(O)2R7, —N(R5)C(O)R7 and —N(R5)C(O)NR5R6;
R8 is selected from the group consisting of R6, —C(O)NR5R6, —S(O)2NR5R6, —C(O)R7, —C(O)2R6, —S(O)2R7 and —(CH2)-aryl;
R9 is selected from the group consisting of halogen, CN, NR5R6, —C(O)2R6, —C(O)NR5R6, —OR6, —C(O)R7, —SR6, —S(O)2R7, —S(O)2NR5R6, —N(R5)—S(O)2R7, —N(R5)C(O)R7 and —N(R5)C(O)NR5R6;
m is 0 to 4; and
p is 0-3.
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