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1.发明申请THIAZOLOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE 有权噻唑啉酮和它们作为磷脂酰肌醇-3激酶的抑制剂公开(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。
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2.发明授权Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase 有权噻唑并嘧啶及其作为磷脂酰肌醇-3激酶抑制剂的用途公开(公告)号：US08168633B2
公开(公告)日：2012-05-01
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： A61K31/5377
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 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。
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3.发明授权Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase 有权噻唑并嘧啶及其作为磷脂酰肌醇-3激酶抑制剂的用途公开(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。
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4.发明申请THIAZOLOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE 有权噻唑啉酮和它们作为磷脂酰肌醇-3激酶的抑制剂公开(公告)号：US20100190769A1
公开(公告)日：2010-07-29
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 , A61P35/00 , A61P37/00 , A61P9/00 , A61P31/12 , A61P29/00 , A61P3/00 , A61P5/00 , A61P25/00
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; R is H or C1-C6 alkyl; and R 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; R是H或C 1 -C 6烷基; 并且R是未取代或取代的吲哚基; 并且其药学上可接受的盐是PI3K的抑制剂，并且对于其它Ia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。
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公开(公告)号：US20120238541A1
公开(公告)日：2012-09-20
申请号：US13496287
申请日：2010-09-17
申请人： Mark Peter Bell , Timothy Harrison , Sumita Bhattacharyya , James Samuel Shane Rountree , Frank Burkamp , Stephen Price , Calum MacLeod , Richard Leonard Elliott , Phillip Smith , Toby Jonathan Blench , Colin Roderick O'Dowd , Lixin Zhang , Graham Peter Trevitt , Hazel Joan Dyke
发明人： Mark Peter Bell , Timothy Harrison , Sumita Bhattacharyya , James Samuel Shane Rountree , Frank Burkamp , Stephen Price , Calum MacLeod , Richard Leonard Elliott , Phillip Smith , Toby Jonathan Blench , Colin Roderick O'Dowd , Lixin Zhang , Graham Peter Trevitt , Hazel Joan Dyke
IPC分类号： A61K31/4188 , A61K31/352 , C07D405/10 , A61K31/4155 , A61K31/496 , A61K31/4178 , C07D491/052 , A61K31/436 , A61K31/4162 , C07D491/147 , A61K31/437 , C07D413/10 , A61K31/5377 , A61K31/422 , A61K31/4192 , C07D498/04 , A61K31/5383 , A61K31/397 , C07C225/20 , A61P35/00 , C07D493/04 , A61K31/357 , C07D311/26
CPC分类号： C07D311/26 , C07D407/04 , C07D491/04
摘要： The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
摘要翻译： 本发明涉及作为丝氨酸 - 苏氨酸激酶AKT抑制剂的特定活性的一系列化合物。 还提供了包含其的药物组合物以及用于治疗癌症的方法。
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公开(公告)号：US08546376B2
公开(公告)日：2013-10-01
申请号：US13496287
申请日：2010-09-17
申请人： Mark Peter Bell , Timothy Harrison , Sumita Bhattacharyya , James Samuel Shane Rountree , Frank Burkamp , Stephen Price , Calum MacLeod , Richard Leonard Elliott , Phillip Smith , Toby Jonathan Blench , Colin Roderick O'Dowd , Lixin Zhang , Graham Peter Trevitt , Hazel Joan Dyke
发明人： Mark Peter Bell , Timothy Harrison , Sumita Bhattacharyya , James Samuel Shane Rountree , Frank Burkamp , Stephen Price , Calum MacLeod , Richard Leonard Elliott , Phillip Smith , Toby Jonathan Blench , Colin Roderick O'Dowd , Lixin Zhang , Graham Peter Trevitt , Hazel Joan Dyke
IPC分类号： A61K31/4188 , A61K31/352 , A61K31/357 , A61K31/397 , A61K31/4155 , A61K31/4162 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/436 , A61K31/437 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61P35/00 , C07C225/20 , C07D311/26 , C07D405/10 , C07D413/10 , C07D491/052 , C07D491/147 , C07D493/04 , C07D498/04
CPC分类号： C07D311/26 , C07D407/04 , C07D491/04
摘要： The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
摘要翻译： 本发明涉及作为丝氨酸 - 苏氨酸激酶AKT抑制剂的特定活性的一系列化合物。 还提供了包含其的药物组合物以及用于治疗癌症的方法。
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公开(公告)号：US08691826B2
公开(公告)日：2014-04-08
申请号：US13613952
申请日：2012-09-13
申请人： Toby Jonathan Blench , Christine Edwards , Robert Andrew Heald , Janusz Jozef Kulagowski , Jonathan Mark Sutton , Carmelida Capaldi
发明人： Toby Jonathan Blench , Christine Edwards , Robert Andrew Heald , Janusz Jozef Kulagowski , Jonathan Mark Sutton , Carmelida Capaldi
IPC分类号： A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
摘要翻译： 式（I）化合物：可用作人中性粒细胞弹性蛋白酶的抑制剂。
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公开(公告)号：US07208494B2
公开(公告)日：2007-04-24
申请号：US10876954
申请日：2004-06-25
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00
CPC分类号： C07D471/14
摘要： The present invention provides piperazine derivatives of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in the description. They can be used for the treatment of obesity.
摘要翻译： 本发明提供式（I）的哌嗪衍生物及其药学上可接受的盐和酯，其中R 1至R 5具有说明书中给出的含义。 它们可用于治疗肥胖。
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9.发明申请Heterocyclic Compounds and Their Use in the Treatment of Cardiovascular Disease 审中-公开杂环化合物及其在治疗心血管疾病中的应用公开(公告)号：US20090221564A1
公开(公告)日：2009-09-03
申请号：US12224265
申请日：2007-02-20
IPC分类号： A61K31/541 , C07D333/58 , A61K31/381 , C07D409/12 , C07D409/10 , A61K31/4436 , C07D413/10 , A61K31/4245 , A61K31/496 , A61K31/506 , C07D417/12 , A61K31/428 , A61K31/422 , A61K31/4196 , A61K31/433 , A61K31/497 , A61K31/4725 , C07D413/12 , A61K31/5377 , A61K31/445 , A61K31/44 , A61P9/00
CPC分类号： A61K31/381 , C07D333/70 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.
摘要翻译： 提供式（I）的杂环化合物：其中环A，环B，R 1，R 2，R 3，R 4，Y，m，n和q如本文所述。 R1特别是脒基。 本发明还提供特定的苯并噻吩化合物。 本发明的化合物可用作因子IXa的抑制剂和用于心血管疾病和疾病的治疗。 血栓形成。
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10.发明授权1,2,3,4,9,9a-hexahydro-2,4a,5-triaza-fluorene and 1,2,3,4-tetrahydro-2,4a,5-triaza-fluorene derivatives 失效1,2,3,4,9,9a-六氢-2,4a，5-三氮杂芴和1,2,3,4-四氢-2,4a，5-三唑 - 芴衍生物公开(公告)号：US07098337B2
公开(公告)日：2006-08-29
申请号：US10350616
申请日：2003-01-24
申请人： David Reginald Adams , Jonathan Mark Bentley , Toby Jonathan Blench , Paul Hebeisen , Nathaniel Julius Thomas Monck , Hans Richter , Stephan Roever , Jonathan Richard Anthony Roffey , Sven Taylor
发明人： David Reginald Adams , Jonathan Mark Bentley , Toby Jonathan Blench , Paul Hebeisen , Nathaniel Julius Thomas Monck , Hans Richter , Stephan Roever , Jonathan Richard Anthony Roffey , Sven Taylor
IPC分类号： C07D471/14 , A61K31/4985 , A61P3/04
CPC分类号： C07D471/14
摘要： The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，溶剂化物和酯。 这些化合物可用于制备用于治疗或预防中枢神经系统疾病，中枢神经系统损害，心血管疾病，胃肠道疾病，糖尿病，肥胖症和睡眠呼吸暂停的药物组合物。
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