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3. 发明申请

US20090156601A1 PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的吡嗪衍生物
公开(公告)号：US20090156601A1
公开(公告)日：2009-06-18
申请号：US12089874
申请日：2006-10-10
申请人： Edward McDonald , Jonathan M. Large , Adrian J. Folkes , Stephen J. Shuttleworth , Nan Chi Wan
发明人： Edward McDonald , Jonathan M. Large , Adrian J. Folkes , Stephen J. Shuttleworth , Nan Chi Wan
IPC分类号： A61K31/5377 , C07D413/14 , A61P29/00
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： The invention provides compounds which are pyrimidines of formula (I): wherein —XR3 is bonded at ring position 2 and —YR4 is bonded at ring position 5 or 6; R1 and R2 form, together with the N atom to which they are attached, a morphorine ring which is unsubstituted or substituted; X is a direct bond; R3 is selected from (i) a group of the following formula (1): wherein B is a phenyl ring which is unsubstituted or substituted and Z is selected from —OR, CH2OR and —NRS(O) mR, wherein each R is independently selected from H, C1-C6 alkyl, C3-C10 cycloalkyl and a 5- to 12-membered aryl or heteroaryl group, the group being unsubstituted or substituted, and m is 2; and (ii) an indazole group which is unsubstituted or substituted; and Y is selected from —O—(CH2)n—, —NH—(CH2)n, —NHC(O)—(CH2)n— and —C(O)NH—(CH2)n— wherein n is 0 or an integer of 1 to 3, and R4 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted and a group —NR5R6 wherein R5 and R6, which are the same or different, are each independently selected from H, C1-C6 alkyl which is unsubstituted or substituted, C3-C10 cycloalkyl which is unsubstituted or substituted, —C(O)R, —C(O)N(R)2 and —S(O)mR wherein R and m are as defined above, or R5 and R6 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6- or 7-membered N-containing heterocyclic group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof. These compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供了式（I）的嘧啶的化合物：其中-XR3在环位置2键合，-YR4键合在环位置5或6; R1和R2与它们所连接的N原子一起形成未取代或取代的吗啉环; X是直接的债券; R3选自（i）下式（1）的基团：其中B是未取代或取代的苯基环，Z选自-OR，CH 2 OR和-NRS（O）m R，其中每个R独立地为选自H，C 1 -C 6烷基，C 3 -C 10环烷基和5至12元芳基或杂芳基，该基团是未取代或取代的，m为2; 和（ii）未取代或取代的吲唑基; 并且Y选自-O-（CH 2）n - ， - NH - （CH 2）n，-NHC（O） - （CH 2）n - 和-C（O）NH-（CH 2）或1〜3的整数，R 4选自未取代或取代的不饱和5〜12元碳环或杂环基和-NR 5 R 6基，其中R 5和R 6相同或不同，各自独立地为未取代或未取代的C 1 -C 6环烷基，-C（O）R 1 -C（O）N（R）2和-S（O）m R，其中R 和m如上所定义，或者R 5和R 6与它们所连接的氮原子一起形成未取代或取代的饱和的5-，6-或7-元含氮杂环基; 及其药学上可接受的盐。这些化合物是PI3K的抑制剂，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍等相关的异常细胞生长，功能或行为引起的疾病和障碍，神经障碍。

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