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1. 发明申请

WO2007132171A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007132171A1
公开(公告)日：2007-11-22
申请号：PCT/GB2007/001644
申请日：2007-05-04
申请人： PIRAMED LIMITED , CHUCKOWREE, Irina, S. , FOLKES, Adrian, J. , GOLDSMITH, Paul , HANCOX, Timothy, C. , SHUTTLEWORTH, Stephen, J.
发明人： CHUCKOWREE, Irina, S. , FOLKES, Adrian, J. , GOLDSMITH, Paul , HANCOX, Timothy, C. , SHUTTLEWORTH, Stephen, J.
IPC分类号： C07D493/04 , C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D493/04 , C07D495/04
摘要： Fused pyrimidines of formula (I): wherein A represents a thiophene or furan ring; n is 0, 1 or 2; R 1 is a group of formula: 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 R4 and R5 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 a heteroaryl group which contains I5 2, 3 or 4 ring nitrogen atoms and 0,1 or 2 additional heteroatoms selected from O, N and S, which group is monocyclic or bicyclic and which is unsubstituted or substituted; and R3 is selected from: (a) a group of the following formula: wherein B is a phenyl ring which is unsubstituted or substituted and Z is selected from H, -OR, -SR, CH2OR, -CO 2 R, CF 2 OH, CH(CF 3 )OH, C(CF 3 ) 2 OH, -(CH 2 ) q OR, - (CH 2 ) q NR 2 , -C(O)N(R) 2 , -NR 2 , -NRC(O)R, -S(O) m N(R) 2 , -OC(O)R, OC(O)N(R) 2 , - NRS(O) m R, -RC(O)N(R) 2, CN, halogen and -NO 2 , wherein each R is independently selected from H, C 1 -C 6 alkyl, C 3 - C 10 cycloalkyl and a 5- to 12-membered aryl or heteroaryl group, the group being unsubstituted or substituted, m is 1 or 2 and q is 0, 1 or 2; (b) a heteroaryl group which contains 1, 2, 3 or 4 ring nitrogen atoms and 0, 1 or 2 additional heteroatoms selected from O and S, which group is monocyclic or bicyclic and which is unsubstituted or substituted; and (c) a group comprising a benzene ring which is unsubstituted or substituted and which is fused to a heteroaryl group as defined above; and the pharmaceutically acceptable salt thereof have activity as inhibitors of PBK 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 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0,1或2; R 1是下式的基团：其中m是0或1; R 30是H或C 1 -C 6烷基; R 4和R 5形式与它们所连接的N原子一起形成5或6元饱和的含氮杂环基，其包括0或1个选自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杂环基或被5或6元饱和的含氮杂环基取代的烷基作为以上定义 R 2是含有I5 2,3或4个环氮原子和0,1或2个选自O，N和S的另外的杂原子的杂芳基，该基团是单环或双环的，其是未取代的或取代; 并且R 3选自：（a）下式的基团：其中B是未取代或取代的苯基环，Z选自H，-OR，-SR，CH 2 OR，-CO 2， R 2，CF 2 OH，CH（CF 3）OH，C（CF 3）2 OH ， - （CH 2 CH 2）q - 或 - ， - （CH 2 CH 2）q NR 2，（O）N（R）2，-NR 2，-NRC（O）R，-S（O） N（R）2，-OC（O）R，OC（O）N（R）2， - NRS（O）（R）-C（O）N（R）2，CN，卤素和-NO 2，其中每个R独立地选自H，C 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是1或2，q是0,1或2; （b）含有1,2,3或4个环氮原子和0,1或2个选自O和S的另外的杂原子的杂芳基，该基团是单环或双环的，其是未取代的或被取代的; 和（c）包含苯环的基团，其未被取代或取代，并且与如上定义的杂芳基稠合; 其药学上可接受的盐具有作为PBK抑制剂的活性，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/内分泌紊乱和神经系统疾病。还描述了合成化合物的方法。

2. 发明申请

WO2006046040A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006046040A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004146
申请日：2005-10-25
申请人： PIRAMED LIMITED , 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 (1); wherein A represents a thiophene or a furan ring; n is 1 or 2; R 1 is a group of formula (); 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; R 2 is selected from a) formula (3) 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 b) formula (4) 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 selected from: (a) a group of the following formula: (5) wherein B is a phenyl ring which is unsubstituted or substituted and Z is selected from H, -OR, -SR, CH 2 OR, -CO 2 R, CF 2 OH, CH(CF 3 )OH, C(CF 3 ) 2 OH, -(CH 2 ) q OR, -(CH 2 )qNR 2 , -C(O)N(R) 2 , -NR 2 , -NRC(O)R, -S(O) m N(R) 2 , -OC(O)R, OC(O)N) 2 , -NRS(O) m R, -NRC(O)N(R) 2 , CN, halogen and -NO 2 , wherein each R is independently selected from H, C 1 -C 6 alkyl, C 3 - C 10 cycloalkyl and a 5- to 12- membered aryl or heteroaryl group, the group being unsubstituted or substituted, m is 1 or 2 and q is 0, 1 or 2; (b) a heteroaryl group which contains, 1, 2, 3 or 4 ring nitrogen atoms and 0, 1 or 2 additional heteroatoms selected from O and S, which group is monocyclic or bicyclic and which is unsubstituted or substituted; and (c) a group comprising a benzene ring which is unsubstituted or substituted and which is fused to a heteroaryl group as defined above; or a pharmaceutically acceptable salt thereof; provided that R 3 is not an indole group or an indazole group, which group 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（1）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（）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原子一起含有0或1个额外的5或6元饱和的含N的杂环基选自N，S和O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; R 2选自其中R 6和R 7形式的a）式（3），以及它们所连接的氮原子，未取代或取代的吗啉，硫代吗啉，哌啶，哌嗪，氧氮杂环庚烷或噻吩甲基; 和b）式（4）其中Y是C 2 -C 4亚烷基链，其在链的组成碳原子和/或在一端或两端含有的链，1或2个选自O，N和S的杂原子，并且是未取代或取代的; R 3选自：（a）下式的基团：（5）其中B是未取代或取代的苯基环，Z选自H，-OR，-SR CH 2 CO 2，-CO 2 R，CF 2 OH，CH（CF 3）OH，C （CF 3）2 OH， - （CH 2 CH 2）q - 或 - ， - （CH 2） -C（O）N（R）2，-NR 2，-NRC（O）R 2，，-S（O）N（R）2，-OC（O）R，OC（O）N）2 - ， - NRS（O）m R，-NRC（O）N（R）2，CN，卤素和-NO 2，其中每个R 独立地选自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，该基团为未取代或取代的，m为1或2，q为0,1或2; （b）杂环基，其含有1,2,3或4个环氮原子和0,1或2个选自O和S的另外的杂原子，该基团是单环或双环的，其是未取代的或取代的; 和（c）包含苯环的基团，其未被取代或取代，并且与如上定义的杂芳基稠合; 或其药学上可接受的盐; 条件是R 3不是吲哚基或吲唑基，该基团是未取代的或取代的; 并且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障碍，代谢/内分泌紊乱和神经系统疾病。还描述了合成化合物的方法。

3. 发明申请

WO2006046035A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006046035A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004137
申请日：2005-10-25
申请人： PIRAMED LIMITED , 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 (1); 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; R2 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 in an indole group which is unsubstituted or substituted ; and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseased 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 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（1）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形式与它们所连接的N原子一起形成5或6元饱和的含氮杂环基，其包括0或1个选自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-杂环基团取代; R2选自式（a）; 其中R 6和R 7形成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; 未取代或取代的吲哚基中的R 3和R 3，其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗由与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症等引起的异常细胞生长，功能或行为引起的疾病和病症，代谢/内分泌紊乱和神经系统疾病。还描述了合成化合物的方法。

4. 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。

5. 发明申请

WO2006046031A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006046031A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004129
申请日：2005-10-25
申请人： PIRAMED LIMITED , 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的其它杂原子，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; 并且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障碍，代谢/内分泌紊乱和神经系统疾病。还描述了合成化合物的方法。

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