| abstract |
Disclosed are 5-{ 8-(amino)-9-alkyl-6-[morpholin-4-yl]-9H-purin-2-yl} pyrimidin-2-amine derivatives as represented by the general formula (1a) wherein the substituents are as defined herein. Representative compounds include 5-{ 9-isobutyl-8-[4-(methylsulfonyl)piperazin-1-yl]-6-morpholin-4-yl-9H-purin-2-yl} pyrimidin-2-amine, 5-{ 9-(cyclopropylmethyl)-8-[4-(methylsulfonyl)piperazin-1-yl]-6-morpholin-4-yl-9H-purin-2-yl} pyrimidin-2-amine and 5-{ 8-[(3R)-4-acetyl-3-methylpiperazin-1-yl]-6-morpholin-4-yl-9-(2,2,2-trifluoroethyl)-9H-purin-2-yl} pyrimidin-2-amine. Further disclosed is a pharmaceutical composition which comprises a compound as defined above or a salt thereof and a pharmaceutically acceptable carrier for treating a tumor, especially those selected from the following group: brain tumour, ovarian cancer, lung cancer, breast cancer, colon cancer, gastrointestinal cancer, prostate cancer, endometrial cancer and melanoma. |