申请人:Hoffmann-La Roche Inc.
公开号:US06150373A1
公开(公告)日:2000-11-21
Amino-substituted dihydropyrimido[4,5-d]pyrimidinones of the formula in which R.sup.1 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, R.sup.2 represents lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, and R.sup.3 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl, lower cycloalkenyl or lower cycloalkyl-lower alkyl, and pharmaceutically acceptable salts thereof are protein kinase inhibitors. They can be used in the treatment or prophylaxis of inflammatory, immunological, oncological, bronchopulmonary, dermatological and cardiovascular disorders, in the treatment of asthma, central nervous system disorders or diabetic complications or for the prevention of graft rejection following transplant surgery.
式中R.sup.1代表氢、低碳基、芳基、芳基-低碳基、杂环芳基、杂环芳基-低碳基、低环烷基或低环烷基-低碳基,R.sup.2代表低碳基、芳基、芳基-低碳基、杂环芳基、杂环芳基-低碳基、低环烷基或低环烷基-低碳基,R.sup.3代表氢、低碳基、芳基、芳基-低碳基、杂环芳基、杂环芳基-低碳基、低环烷基、低环烯基或低环烷基-低碳基,以及其药学上可接受的盐是蛋白激酶
抑制剂。它们可用于治疗或预防炎症、免疫、肿瘤、支气管肺部、皮肤和心血管疾病,在哮喘、中枢神经系统疾病或糖尿病并发症的治疗中,或用于移植手术后预防移植排斥。