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1. 发明申请

US20100016306A1 PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS 失效
标题翻译：吡嗪衍生物作为PI3K抑制剂
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。

2. 发明授权

US08252792B2 Pyrimidine derivatives as PI3K inhibitors 失效
标题翻译：嘧啶衍生物作为PI3K抑制剂
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。

3. 发明申请

US20120283257A1 PHARMACEUTICAL COMPOUNDS 失效
标题翻译：药物化合物
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。

4. 发明授权

US08697693B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
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。

5. 发明申请

US20100256143A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
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。

6. 发明申请

US20100130496A1 PYRIMIDINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3-KINASE 审中-公开
标题翻译：作为磷脂酰肌醇三激酶的抑制剂的吡嗪衍生物
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。

7. 发明申请

US20100210646A1 2-MORPHOLIN-4-YL-PYRIMIDINES AS PI3K INHIBITORS 审中-公开
标题翻译： 2-MORPHOLIN-4-YL-PYRIMININES作为PI3K抑制剂
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。

8. 发明授权

US08981087B2 Benzo [E] [1,3] oxazin-4-one derivatives as phosphoinositide 3-kinase inhibitors 有权
标题翻译：苯并[E] [1,3]恶嗪-4-酮衍生物作为磷酸肌醇3-激酶抑制剂
公开(公告)号：US08981087B2
公开(公告)日：2015-03-17
申请号：US13384310
申请日：2010-07-23
申请人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Alexander Richard Liam Cecil , Thomas James Hill
发明人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Alexander Richard Liam Cecil , Thomas James Hill
IPC分类号： C07D265/24 , C07D413/04 , A61K31/536 , A61K31/5365 , A61P19/02
CPC分类号： C07D265/24
摘要： Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)-alkyl. —C(O)—NH2, —C(O)—NH-alkyl, —SO2-alkyl, —SO2—NH2 or —SO2—NH-alkyl; R2 is aryl substituted with at least one nitrogen-containing group or R2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C1-C6 mono alkylamino, C1C6 bis alkylamino, C1C6 acylamino, C1-C6 aminoalkyl, mono (C1C6 alkyl)amino C1-C6 alkyl, bis (C1C6 alkyl)amino C1C6 alkyl, C1-C6-acylamino or C1 C6 alkynyl-NR11, R11 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, halogen, O-alkyl, NH-alkyl, N-dialkyl, —C(O)—R7, —C(O)—NH2, —C(O)—NH—R7, —SO2—R7, —SO2—NH2, —SO2—NH—R7, NH-acyl, NH-sulfonyl, NR7-acyl, NR7-sulfonyl, N—C(O)—NH—R7, N—SO2—NH—R7, N—C(O)—NR7R7 or N—SO2—NR7R7; and R7 is alkyl, aryl or heteroaryl, are useful as PI3K inhibitors and are useful in therapy.
摘要翻译：式（I）的化合物：其中：W是O，N-H，N-烷基，N-烯基，N-炔基，N-芳基，N-杂芳基或S; 每个X独立地是CH或N; R1是式（b）或R3是H，烷基，NH2，OH，= 0或卤素; 每个A和B独立地是CH或N; D是NHR4; R4是H，烷基，-C（O） - 烷基。 -C（O）-NH 2，-C（O）-NH-烷基，-SO 2 - 烷基，-SO 2 -NH 2或-SO 2 -NH-烷基; R2是被至少一个含氮基取代的芳基，或R2是含氮杂芳基，被含氮基取代的环烷基，含氮环烷基，C1-C6单烷基氨基，C1C6双烷基氨基，C1C6酰基氨基，C1- C 1 -C 6烷基，单（C 1 -C 6烷基）氨基C 1 -C 6烷基，双（C 1 -C 6烷基）氨基C 1 -C 6烷基，C 1 -C 6酰基氨基或C 1 -C 6炔基-NR 11，R 11是H，烷基，烯基，炔基，芳基，杂芳基，，O-烷基，NH-烷基，N-二烷基，-C（O）-R 7，-C（O）-NH 2，-C（O）-NH-R7，-SO 2 -R 7，-SO 2 -NH 2 - SO2-NH-R7，NH-酰基，NH-磺酰基，NR7-酰基，NR7-磺酰基，N-C（O）-NH-R7，N-SO2-NH-R7，N-C（O）-NR7R7或 N-SO2-NR7R7; 和R7是烷基，芳基或杂芳基，可用作PI3K抑制剂，并且可用于治疗。

9. 发明授权

US08614193B2 Depsipeptides and their therapeutic use 失效
标题翻译： Depsipeptides及其治疗用途
公开(公告)号：US08614193B2
公开(公告)日：2013-12-24
申请号：US12991491
申请日：2009-05-22
申请人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Cyrille Davy Tomassi , Alexander Richard Liam Cecil , Thomas James Hill
发明人： Stephen Joseph Shuttleworth , Franck Alexandre Silva , Cyrille Davy Tomassi , Alexander Richard Liam Cecil , Thomas James Hill
IPC分类号： A61K38/12 , A61K31/542 , C07K11/00 , C07K11/02 , C07K7/54
CPC分类号： C07K5/02 , C07K5/1008 , C07K5/101 , C07K5/1016 , C07K5/1021 , C07K5/1024 , Y02P20/55
摘要： The subject application pertains to a compound of structure IX or X: or a pharmaceutically acceptable salt thereof, wherein: X is —C(═O)N(R10)— or —CH(OPr3) —; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.
摘要翻译：本申请涉及结构IX或X的化合物或其药学上可接受的盐，其中：X为-C（= O）N（R 10） - 或-CH（OPr 3） - ; R7，R9和R10相同或不同，代表氢或氨基酸侧链部分，来自天然或非天然氨基酸; Pr1和Pr2相同或不同，表示氢或硫醇保护基; Pr3是氢或醇保护基; R 1，R 2，R 5和R 6相同或不同，表示氢或氨基酸侧链部分，与天然或非天然氨基酸或R1和R2和/或R5和R6一起与碳原子一起它们连接，形成螺环部分，条件是：R 1和R 2各自不是氢，或者R 5和R 6中的每一个不是氢。

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