Raf inhibitors
AssigneesAgennix USA Inc., Agennix, Inc.
InventorsAlexander BACKES, Joachim VOGT, Peter AMON, Igor IVANOV, Stefan HANNUS, Matthias BORGMANN, Kerrin HANSEN, Rebecca CASAUBON, Chase SMITH, Krishna MURTHI, Arthur KLUGE, Andreas SCHOOP, Lars NEUMANN, Jan EICKHOFF
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Abstract
The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
Claims15
A compound having a structure represented by formula (I)
- or any tautomeric form thereof, wherein
- R1 is selected from hydrogen, —NH2, and substituted or unsubstituted:
- —NH—Cl1-6-alkyl, —NH-cycloalkyl, —NH-heterocycloalkyl, —NH—C1-6-alkylene-OR7, and —NH—C1-6-alkylene-NR72;
- R2 is selected from hydrogen, -halogen, -methyl, —CH2F, —CHF2, —CF3, —O—-methyl, —O—CH2F, —O—CHF2, and —O—CF3;
- one of R3 and R4 is hydrogen, and the other is —NH—C(═O)—(NH)x—(CH2)y—R6, wherein x and y are independently selected from 0 and 1;
- R5 is selected from hydrogen, and substituted or unsubstituted:
- -alkyl, -alkenyl, -alkynyl, -cycloalkenyl, —(C-linked-heterocycloalkyl), —(C-linked-heterocycloalkenyl), -aryl, and -heteroaryl;
- R6 is selected from substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl;
- R7 is independently selected from hydrogen and —C1-6-alkyl;
- or any pharmaceutically acceptable salt or N-oxide thereof;
- provided, however, that compound (A) is excluded:
A pharmaceutical composition, including a compound of claim 16, and a pharmaceutically acceptable diluent, excipient or carrier.
Dependencies are inferred from the claim text.