公开(公告)号：US08697693B2

公开(公告)日：2014-04-15

申请号：US13553650

申请日：2012-07-19

申请人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Price ,  Stephen Joseph Shuttleworth ,  Sukhjit Sohai

发明人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Price ,  Stephen Joseph Shuttleworth ,  Sukhjit Sohai

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D495/04

摘要： Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, in particular the p110 delta subtype, such as 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（Ia）或（Ib）的噻吩并嘧啶：其中R1-R3具有本文所述的任何值，并且其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗由异常细胞生长引起的疾病和障碍 ，与PI3激酶，特别是p110δ亚型相关的功能或行为，例如免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。 还描述了合成化合物的方法。

公开(公告)号：US20100016306A1

公开(公告)日：2010-01-21

申请号：US12298507

申请日：2007-04-25

申请人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Price ,  Stephen Joseph Shuttleworth ,  Sukhjit Sohal

发明人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Price ,  Stephen Joseph Shuttleworth ,  Sukhjit Sohal

IPC分类号： A61K31/5377 ,  C07D495/04 ,  A61P35/00

CPC分类号： C07D495/04

摘要： Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as 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, in particular the p110 delta subtype, such as 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（Ia）或（Ib）的噻吩并嘧啶：其中R1-R3具有本文所述的任何值，并且其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗由异常细胞生长引起的疾病和障碍 ，与PI3激酶，特别是p110δ亚型相关的功能或行为，例如免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。 还描述了合成化合物的方法。

公开(公告)号：US08252792B2

公开(公告)日：2012-08-28

申请号：US12298507

申请日：2007-04-25

申请人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Price ,  Stephen Joseph Shuttleworth ,  Sukhjit Sohal

发明人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Price ,  Stephen Joseph Shuttleworth ,  Sukhjit Sohal

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D495/04

摘要： Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as 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, in particular the p110 delta subtype, such as 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（Ia）或（Ib）的噻吩并嘧啶：其中R1-R3具有本文所述的任何值，并且其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗由异常细胞生长引起的疾病和障碍 ，与PI3激酶，特别是p110δ亚型相关的功能或行为，例如免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。 还描述了合成化合物的方法。

公开(公告)号：US20120283257A1

公开(公告)日：2012-11-08

申请号：US13553650

申请日：2012-07-19

申请人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Price ,  Stephen Joseph Shuttleworth ,  Sukhjit Sohal

发明人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Price ,  Stephen Joseph Shuttleworth ,  Sukhjit Sohal

IPC分类号： A61K31/5377 ,  A61P29/00

CPC分类号： C07D495/04

摘要： Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as 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, in particular the p110 delta subtype, such as 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（Ia）或（Ib）的噻吩并嘧啶：其中R1-R3具有本文所述的任何值，并且其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗由异常细胞生长引起的疾病和障碍 ，与PI3激酶，特别是p110δ亚型相关的功能或行为，例如免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。 还描述了合成化合物的方法。

公开(公告)号：US20100256143A1

公开(公告)日：2010-10-07

申请号：US12594543

申请日：2008-04-14

申请人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Joseph Shuttleworth ,  Elsa Amandine Dechaux ,  Sussie Lerche Krintel ,  Stephen Price ,  Jonathan Martin Large ,  Edward McDonald

发明人： Stewart James Baker ,  Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Joseph Shuttleworth ,  Elsa Amandine Dechaux ,  Sussie Lerche Krintel ,  Stephen Price ,  Jonathan Martin Large ,  Edward McDonald

IPC分类号： A61K31/5377 ,  C07D413/14 ,  A61P35/00 ,  A61P31/12 ,  A61P37/00 ,  A61P29/00 ,  A61P25/00 ,  A61P9/00 ,  A61P3/00

CPC分类号： C07D487/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14

摘要： The invention provides a pyrimidine compound of formula (I): wherein R1 and R2 have any of the values defined herein; or a pharmaceutically acceptable salt thereof. The 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： 本发明提供式（I）的嘧啶化合物：其中R1和R2具有本文定义的任何值; 或其药学上可接受的盐。 这些化合物是PI3K的抑制剂，因此可用于治疗由与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。

公开(公告)号：US20100130496A1

公开(公告)日：2010-05-27

申请号：US12594529

申请日：2008-04-14

申请人： Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Joseph Shuttleworth ,  Elsa Amandine Dechaux ,  Stephen Price ,  Jonathan Martin Large ,  Edward McDonald

发明人： Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Joseph Shuttleworth ,  Elsa Amandine Dechaux ,  Stephen Price ,  Jonathan Martin Large ,  Edward McDonald

IPC分类号： A61K31/5377 ,  C07D413/14 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  A61P29/00 ,  A61P31/12 ,  A61P25/00 ,  A61P5/00 ,  A61P3/00

CPC分类号： C07D403/04 ,  C07D401/14 ,  C07D417/14

摘要： The invention provides a pyrimidine compound of formula (I): wherein R1, R2, and Y have any of the values defined herein; or a pharmaceutically acceptable salt thereof. The 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： 本发明提供式（I）的嘧啶化合物：其中R1，R2和Y具有本文定义的任何值; 或其药学上可接受的盐。 这些化合物是PI3K的抑制剂，因此可用于治疗由与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。

公开(公告)号：US20100210646A1

公开(公告)日：2010-08-19

申请号：US12594552

申请日：2008-04-14

申请人： Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Joseph Shuttleworth ,  Jonathan Martin Large ,  Edward McDonald

发明人： Paul John Goldsmith ,  Timothy Colin Hancox ,  Neil Anthony Pegg ,  Stephen Joseph Shuttleworth ,  Jonathan Martin Large ,  Edward McDonald

IPC分类号： A61K31/5377 ,  C07D413/14 ,  A61P35/00 ,  A61P37/00 ,  A61P31/12 ,  A61P29/00 ,  A61P25/00 ,  A61P9/00 ,  A61P5/00 ,  A61P3/00

CPC分类号： C07D401/14

摘要： The invention provides a pyrimidine compound of formula (I): wherein R1 and R2 have any of the values defined herein; or a pharmaceutically acceptable salt 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： 本发明提供式（I）的嘧啶化合物：其中R1和R2具有本文定义的任何值; 或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。

公开(公告)号：US20110098270A1

公开(公告)日：2011-04-28

申请号：US12986317

申请日：2011-01-07

申请人： Timothy Colin Hancox ,  Neil Anthony Pegg ,  Mandy Christine Beswick ,  Toby Jonathan Blench ,  Elsa Amandine Dechaux ,  Jahusz Jozef Kulagowski ,  Alan John Nadin ,  Stephen Price

发明人： Timothy Colin Hancox ,  Neil Anthony Pegg ,  Mandy Christine Beswick ,  Toby Jonathan Blench ,  Elsa Amandine Dechaux ,  Jahusz Jozef Kulagowski ,  Alan John Nadin ,  Stephen Price

IPC分类号： A61K31/397 ,  A61K31/5377 ,  A61P35/00

CPC分类号： C07D513/04

摘要： Thiazolopyrimidine compounds of formula I, where W represents a thiazole ring, selectively inhibit the p110 delta subtype of PI3 Kinase (PI3K), and are useful for treating 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： 式I的噻唑并嘧啶化合物，其中W表示噻唑环，选择性地抑制PI3激酶（PI3K）的p110δ亚型，并且可用于治疗由与PI3激酶例如癌症相关的异常细胞生长，功能或行为引起的疾病和障碍 ，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

公开(公告)号：US08293735B2

公开(公告)日：2012-10-23

申请号：US12739435

申请日：2008-10-27

申请人： Timothy Colin Hancox ,  Neil Anthony Pegg ,  Alan John Nadin ,  Stephen Price

发明人： Timothy Colin Hancox ,  Neil Anthony Pegg ,  Alan John Nadin ,  Stephen Price

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D495/04 ,  C07D519/00

摘要： Thienopyrimidines of formula (I) wherein W and R1 to R4 are as defined in the claims, and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behavior 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： 其中W和R 1至R 4如权利要求中所定义的式（I）的噻吩并嘧啶及其药学上可接受的盐是PI3K的抑制剂，并且对于作为Ia类PI3激酶的p110δ同种型，对于其它1a类 和1b类激酶。 该化合物可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍相关的异常细胞生长，功能或行为引起的疾病和障碍。

公开(公告)号：US07893060B2

公开(公告)日：2011-02-22

申请号：US12663823

申请日：2008-06-12

申请人： Timothy Colin Hancox ,  Neil Anthony Pegg ,  Mandy Christine Beswick ,  Toby Jonathan Blench ,  Elsa Amandine Dechaux ,  Janusz Jozef Kulagowski ,  Alan John Nadin ,  Stephen Price

发明人： Timothy Colin Hancox ,  Neil Anthony Pegg ,  Mandy Christine Beswick ,  Toby Jonathan Blench ,  Elsa Amandine Dechaux ,  Janusz Jozef Kulagowski ,  Alan John Nadin ,  Stephen Price

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： C07D513/04

摘要： Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; R3 is H or C1-C6 alkyl; and R4 is an indole group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PD kinase, over both other class Ia and class Ib kinases. The compounds may 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： 式（I）的噻唑并嘧啶：其中W表示噻唑环; R1和R2与它们所连接的N原子一起形成下式（IIa）的基团：其中A是环系; m为0,1或2; R3是H或C1-C6烷基; R4是未取代或取代的吲哚基; 其药学上可接受的盐是PI3K的抑制剂，并且对于其它1a类和1b类激酶对p110δ同种型是Ia Ia激酶的选择性。 该化合物可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍相关的异常细胞生长，功能或行为引起的疾病和障碍。