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1. 发明申请

WO2006046031A8 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药用化合物
公开(公告)号：WO2006046031A8
公开(公告)日：2007-06-07
申请号：PCT/GB2005004129
申请日：2005-10-25
申请人： PIRAMED LTD , SHUTTLEWORTH STEPHEN J , FOLKES ADRIAN J , CHUCKOWREE IRINA S , WAN NAN CHI , HANCOX TIMOTHY C , BAKER STEWART J , SOHAL SUKHJIT , LATIF MOHAMMED A
发明人： SHUTTLEWORTH STEPHEN J , FOLKES ADRIAN J , CHUCKOWREE IRINA S , WAN NAN CHI , HANCOX TIMOTHY C , BAKER STEWART J , SOHAL SUKHJIT , LATIF MOHAMMED A
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04
摘要： Fused pyrimidines of formula (I); wherein A represents a thiophene or furan ring; n is 1 or 2; R 1 is a group of formula (II); wherein m is 0 or 1; R 30 is H or C 1 -C 6 alkyl; R 4 and R 5 form, together with the N atom to which they are attached, a 5- or 6-membered saturated N-containing heterocyclic group which includes 0 or 1 additional heteroatoms selected from N, S and O, which may be fused to a benzene ring and which is unsubstituted or substituted; or one of R 4 and R 5 is alkyl and the other is a 5- or 6-membered saturated N-containing heterocyclic group as defined above or an alkyl group which is substituted by a 5- or 6-membered saturated N-containing heterocyclic group as defined above; R 2 is selected from formula (a); wherein R 6 and R 7 form, together with the nitrogen atom to which they are attached, a morpholine, thiomorpholine, piperidine, piperazine, oxazepane or thiazepane group which is unsubstituted or substituted; and formula (b); wherein Y is a C 2 -C 4 alkylene chain which contains, between constituent carbon atoms of the chain and/or at one or both ends of the chain, 1 or 2 heteroatoms selected from O, N and S, and which is unsubstituted or substituted; and R 3 is an indazole group which is unsubstituted or substituted; and the pharmaceutically acceptable salt thereof have activity as inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
摘要翻译：式（I）的稠合嘧啶; 其中A表示噻吩或呋喃环; n为1或2; R 1是式（II）的基团; 其中m为0或1; R 30是H或C 1 -C 6烷基; R 4和R 5形成与它们所连接的N原子一起形成5或6元饱和的含N杂环基，其包括0或1 选自N，S和O的另外的杂原子，其可以与苯环稠合并且是未取代或取代的; 或者R 4和R 5中的一个是烷基，另一个是如上定义的5或6元饱和的含N杂环基或烷基，被如上定义的5或6元饱和的含N的杂环基取代; R 2选自式（a）; 其中R 6和R 7与它们所连接的氮原子一起形成未取代的吗啉，硫代吗啉，哌啶，哌嗪，氧氮杂环庚烷或噻吩甲基，取代; 和式（b）; 其中Y是C 2 -C 4亚烷基链，其在链的组成碳原子和/或链的一端或两端含有1或2个选自O，N和S的杂原子，其为未取代或取代的; R 3是未取代或取代的吲唑基; 其药学上可接受的盐具有作为P13K抑制剂的活性，因此可用于治疗与P13激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症等相关的异常细胞生长，功能或行为引起的疾病和病症，代谢/内分泌紊乱和神经障碍。还描述了用于合成化合物的方法。

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