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1. 发明申请

US20120258966A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：US20120258966A1
公开(公告)日：2012-10-11
申请号：US13415672
申请日：2012-03-08
申请人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
发明人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
IPC分类号： A61K31/5377 , A61P35/00
CPC分类号： C07D495/04
摘要： Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts 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 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R1-R3，A和n具有说明书中描述的任何值; 及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/内分泌失调和神经系统疾病相关的异常细胞生长，功能或行为引起的疾病和障碍疾病还描述了合成化合物的方法。

2. 发明申请

US20100280027A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20100280027A1
公开(公告)日：2010-11-04
申请号：US12835533
申请日：2010-07-13
申请人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
发明人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
IPC分类号： A61K31/5377 , A61P35/00 , A61P37/00 , A61P9/00 , A61P3/00 , A61P25/00 , A61P29/00 , A61P31/12 , A61P3/10 , A61P3/04 , A61P35/02
CPC分类号： C07D495/04
摘要： Provided herein are methods of treating diseases or disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, which method includes administering to a patient in need thereof a compound that is a fused pyrimidine of formula (I):
摘要翻译：本文提供了治疗由与PI3激酶相关的异常细胞生长，功能或行为引起的疾病或障碍的方法，该方法包括向有需要的患者施用作为式（I）的稠合嘧啶的化合物：

3. 发明授权

US07776856B2 Pharmaceutical compounds 有权
标题翻译：药物化合物
公开(公告)号：US07776856B2
公开(公告)日：2010-08-17
申请号：US11665657
申请日：2005-10-25
申请人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
发明人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D495/04
摘要： Fused pyrimidines of formula (I): where A is a thiophene or furan ring and R1-R3 and n are defined in the specification. These compounds have activity as inhibitors of PI3K and may thus be used to treat diseased 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 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是噻吩或呋喃环，R1-R3和n在说明书中定义。这些化合物具有作为PI3K抑制剂的活性，因此可用于治疗与由PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌紊乱相关的异常细胞生长，功能或行为引起的疾病和病症和神经障碍。还描述了合成化合物的方法。

4. 发明授权

US07696204B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US07696204B2
公开(公告)日：2010-04-13
申请号：US12089677
申请日：2006-10-11
申请人： Edward McDonald , Jonathan M Large , Stephen J Shuttleworth
发明人： Edward McDonald , Jonathan M Large , Stephen J Shuttleworth
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Pyrimidines of formula (I): wherein R1 to R4, X and Y are defined in the specification are inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的嘧啶：其中R1至R4，X和Y在本说明书中定义为P13K的抑制剂，因此可用于治疗与P13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病症，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。

5. 发明授权

US07649110B2 Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders 有权
标题翻译：用于治疗代谢紊乱的化合物，药物组合物和方法
公开(公告)号：US07649110B2
公开(公告)日：2010-01-19
申请号：US11067377
申请日：2005-02-25
申请人： Michelle Akerman , Jonathan Houze , Daniel C. H. Lin , Jinqian Liu , Jiwen Liu , Jian Luo , Zhihua Ma , Julio C. Medina , Wei Qiu , Jeffrey D. Reagan , Rajiv Sharma , Michael J. Schmitt , Stephen J. Shuttleworth , Ying Sun , Yingcai Wang , Jian Zhang , Liusheng Zhu
发明人： Michelle Akerman , Jonathan Houze , Daniel C. H. Lin , Jinqian Liu , Jiwen Liu , Jian Luo , Zhihua Ma , Julio C. Medina , Wei Qiu , Jeffrey D. Reagan , Rajiv Sharma , Michael J. Schmitt , Stephen J. Shuttleworth , Ying Sun , Yingcai Wang , Jian Zhang , Liusheng Zhu
IPC分类号： C07C59/40 , C07C65/03
CPC分类号： C07D277/24 , C07D277/30
摘要： The present invention provides compounds useful, for example, for modulating insulin levels in a subject and that have the general formula Q—L1—P—L2—M—X—L3—A wherein the definitions of the variables Q, L1, P, L2, M, X, L3 and A are provided herein. The present invention also provides compositions and methods for use of the compounds, for instance, for treatment of type II diabetes.
摘要翻译：本发明提供了可用于调节受试者胰岛素水平的化合物，其具有通式Q-L1-P-L2-MX-L3-A，其中变量Q，L1，P，L2， M，X，L3和A。本发明还提供了用于治疗II型糖尿病的化合物的组合物和方法。

6. 发明申请

US20090042884A1 Pharmaceutical Compounds 失效
标题翻译：药物化合物
公开(公告)号：US20090042884A1
公开(公告)日：2009-02-12
申请号：US12089677
申请日：2006-10-11
申请人： Edward McDonald , Jonathan M. Large , Stephen J. Shuttleworth
发明人： Edward McDonald , Jonathan M. Large , Stephen J. Shuttleworth
IPC分类号： C07D413/04 , A61K31/5377 , C07D413/14 , A61P35/00 , A61P31/12 , A61P9/00 , A61P29/00 , A61P37/00 , A61P3/00
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Pyrimidines of formula (I): wherein R1 to R4, X and Y are defined in the specification are 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 such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的嘧啶：其中R1至R4，X和Y在本说明书中定义为PI3K的抑制剂，因此可用于治疗与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。

7. 发明授权

US07572783B2 Substituted benzofused heterocycles 有权
标题翻译：取代的苯并杂环
公开(公告)号：US07572783B2
公开(公告)日：2009-08-11
申请号：US11203562
申请日：2005-08-12
申请人： Xi Chen , Xiaoqi Chen , Richard Victor Connors , Kang Dai , Ying Fu , Juan C. Jaen , Yong-Jae Kim , Leping Li , Mike E. Lizarzaburu , Jeffrey T. Mihalic , Stephen J. Shuttleworth
发明人： Xi Chen , Xiaoqi Chen , Richard Victor Connors , Kang Dai , Ying Fu , Juan C. Jaen , Yong-Jae Kim , Leping Li , Mike E. Lizarzaburu , Jeffrey T. Mihalic , Stephen J. Shuttleworth
IPC分类号： A61K31/4709 , A61K31/553 , C07D217/02 , C07D267/02
CPC分类号： C07D417/06 , C07D217/24 , C07D223/16 , C07D243/14 , C07D401/06 , C07D401/12 , C07D487/04 , C07D491/10
摘要： The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for example, for the treatment and prevention of obesity, obesity-related disorders and eating disorders.
摘要翻译：本发明涉及式I化合物，其制备方法和包含它们的药物组合物。化合物和药物组合物可用于例如治疗和预防肥胖，肥胖相关疾病和进食障碍。

8. 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。

9. 发明授权

US07358250B2 Pyrrolo[2,3-d]pyrimidines that modulate ACK1 activity 失效
标题翻译：吡咯并[2,3-d]嘧啶，其调节ACK1活性
公开(公告)号：US07358250B2
公开(公告)日：2008-04-15
申请号：US11169313
申请日：2005-06-29
申请人： Christopher N. Farthing , Paul Faulder , Alexander D. Frenkel , Martin J. Harrison , Xianyun Jiao , Frank Kayser , David J. Kopecky , Jinqian Liu , Sarah E. Lively , Rajiv Sharma , Stephen J. Shuttleworth
发明人： Christopher N. Farthing , Paul Faulder , Alexander D. Frenkel , Martin J. Harrison , Xianyun Jiao , Frank Kayser , David J. Kopecky , Jinqian Liu , Sarah E. Lively , Rajiv Sharma , Stephen J. Shuttleworth
IPC分类号： C07D487/04 , C07D413/10 , A61P35/04 , C07F9/02 , A61K31/519 , A61K31/5355 , A61K31/675
CPC分类号： C07D487/04
摘要： Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general structure: where the values of the substituents are provided herein.
摘要翻译：描述了调节ACK1和LCK的作用的化合物以及用于治疗ACK1和LCK介导的疾病的相关组合物方法。在一个方面，化合物具有一般结构：其中本文提供取代基的值。

10. 发明授权

US07872003B2 Pharmaceutical compounds 有权
标题翻译：药物化合物
公开(公告)号：US07872003B2
公开(公告)日：2011-01-18
申请号：US11893625
申请日：2007-08-16
申请人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
发明人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： C07D495/04
摘要： Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts 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 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R1-R3，A和n具有说明书中描述的任何值; 及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/内分泌失调和神经系统疾病相关的异常细胞生长，功能或行为引起的疾病和障碍疾病还描述了合成化合物的方法。

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