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![[1H-Pyrazolo[3, 4-D]Pyrimidin-4-Yl]-Piperidine or -Piperazine Compounds as Serine-Theoronine Kinase Modulators (P70s6k, Atk1 and Atk2) for the Treatment of Immunological, Inflammatory and Proliferative Diseases](/abs-image/US/2008/08/07/US20080188482A1/abs.jpg.150x150.jpg)
1.发明申请[1H-Pyrazolo[3, 4-D]Pyrimidin-4-Yl]-Piperidine or -Piperazine Compounds as Serine-Theoronine Kinase Modulators (P70s6k, Atk1 and Atk2) for the Treatment of Immunological, Inflammatory and Proliferative Diseases 失效[1H-吡唑并[3,4-D]嘧啶-4-基] - 哌啶或哌嗪化合物作为丝氨酸 - 氨基激酶调节剂（P70s6k，Atk1和Atk2）用于治疗免疫学，炎症和增殖性疾病公开(公告)号：US20080188482A1
公开(公告)日：2008-08-07
申请号：US11722291
申请日：2005-12-27
申请人： Ken Rice , Erick Wang Co , Moon Hwan Kim , Lynne Canne Bannen , Joerg Bussenirs , Donna Tra Le , Amy Lew Tsuhako , John Nuss , Yong Wang , Wei Xu , Rhett Ronald Klein
发明人： Ken Rice , Erick Wang Co , Moon Hwan Kim , Lynne Canne Bannen , Joerg Bussenirs , Donna Tra Le , Amy Lew Tsuhako , John Nuss , Yong Wang , Wei Xu , Rhett Ronald Klein
IPC分类号： A61K31/496 , C07D487/02 , C12Q1/48 , A61K31/519
CPC分类号： C07D487/04
摘要： The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
摘要翻译： 本发明提供式（I）化合物和抑制激酶，更特别是p70S6激酶，更优选p70S6，Akt-1和Akt-2激酶的方法。 本发明提供用于调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移，化学侵袭和代谢的化合物。 本发明的化合物抑制，调节和/或调节与上述细胞活性变化相关的激酶受体信号转导途径，本发明包括含有这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病症的方法 。
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公开(公告)号：US08076338B2
公开(公告)日：2011-12-13
申请号：US11568173
申请日：2005-04-22
申请人： Neel K. Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Lynne Canne Bannen , Diva Sze-Ming Chan , Baili Chen , Erick Wang Co , Simona Costanzo , Steven Charles Defina , Larisa Dubenko , Maurizio Franzini , Ping Huang , Vasu Jammalamadaka , Richard George Khoury , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Morrison B. Mac , John M. Nuss , Jason Jevious Parks , Kenneth D. Rice , Tsze H. Tsang , Amy Lew Tsuhako , Yong Wang , Wei Xu
发明人： Neel K. Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Lynne Canne Bannen , Diva Sze-Ming Chan , Baili Chen , Erick Wang Co , Simona Costanzo , Steven Charles Defina , Larisa Dubenko , Maurizio Franzini , Ping Huang , Vasu Jammalamadaka , Richard George Khoury , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Morrison B. Mac , John M. Nuss , Jason Jevious Parks , Kenneth D. Rice , Tsze H. Tsang , Amy Lew Tsuhako , Yong Wang , Wei Xu
IPC分类号： A61K31/501 , A61K31/497 , C07D473/16 , C07D401/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the Formula (I) and (II) wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译： 本发明涉及式（I）和（II）的化合物，其中R，R 21，R 25 -R 33，m，n，X 21-X 23和Q 1在本文中定义。 该化合物调节蛋白激酶酶活性以调节细胞活性，如增殖，分化，程序性细胞死亡，迁移和化学侵袭。 本发明的化合物抑制，调节和/或调节激酶，特别是p70S6和/或Akt激酶。 使用和制备化合物的方法及其药物组合物治疗激酶依赖性疾病和病症也是本发明的一个方面。
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公开(公告)号：US20080076774A1
公开(公告)日：2008-03-27
申请号：US11568173
申请日：2005-04-22
申请人： Neel K. Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Lynne Canne Bannen , Diva Sze-Ming Chan , Baili Chen , Erick Wang Co , Simona Costanzo , Steven Charles Defina , Larisa Dubenko , Maurizio Franzini , Ping Huang , Vasu Jammalamadaka , Richard George Khoury , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Morrison B. Mac , John M. Nuss , Jason Jevious Parks , Kenneth D. Rice , Tsze H. Tsang , Amy Lew Tsuhako , Yong Wang , Wei Xu
发明人： Neel K. Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Lynne Canne Bannen , Diva Sze-Ming Chan , Baili Chen , Erick Wang Co , Simona Costanzo , Steven Charles Defina , Larisa Dubenko , Maurizio Franzini , Ping Huang , Vasu Jammalamadaka , Richard George Khoury , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Morrison B. Mac , John M. Nuss , Jason Jevious Parks , Kenneth D. Rice , Tsze H. Tsang , Amy Lew Tsuhako , Yong Wang , Wei Xu
IPC分类号： A61K31/497 , A61K31/501 , A61P43/00 , C07D403/14 , C07D473/00 , C12N5/06 , C12Q1/48
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the Formula (I) and (II) wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译： 本发明涉及式（I）和（II）的化合物，其中R 1，R 21，R 25，R 33，m ，n，X 21 -X 23和Q 1在本文中定义。 该化合物调节蛋白激酶酶活性以调节细胞活性，如增殖，分化，程序性细胞死亡，迁移和化学侵袭。 本发明的化合物抑制，调节和/或调节激酶，特别是p70S6和/或Akt激酶。 使用和制备化合物的方法及其药物组合物治疗激酶依赖性疾病和病症也是本发明的一个方面。
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![[1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases](/abs-image/US/2011/08/09/US07994172B2/abs.jpg.150x150.jpg)
4.发明授权[1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases 失效[1H-吡唑并[3,4-D]嘧啶-4-基] - 哌啶或哌嗪化合物，作为用于治疗免疫学，炎症和增殖性疾病的丝氨酸 - 氨氮激酶调节剂（P70s6k，Atk1和Atk2）公开(公告)号：US07994172B2
公开(公告)日：2011-08-09
申请号：US11722291
申请日：2005-12-27
申请人： Ken Rice , Erick Wang Co , Moon Hwan Kim , Lynn Canne Bannen , Joerg Bussenius , Donna Tra Le , Amy Lew Tsuhako , John Nuss , Yong Wang , Wei Xu , Rhett Ronald Klein
发明人： Ken Rice , Erick Wang Co , Moon Hwan Kim , Lynn Canne Bannen , Joerg Bussenius , Donna Tra Le , Amy Lew Tsuhako , John Nuss , Yong Wang , Wei Xu , Rhett Ronald Klein
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
摘要翻译： 本发明提供式（I）化合物和抑制激酶，更特别是p70S6激酶，更优选p70S6，Akt-1和Akt-2激酶的方法。 本发明提供用于调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移，化学侵袭和代谢的化合物。 本发明的化合物抑制，调节和/或调节与上述细胞活性变化相关的激酶受体信号转导途径，本发明包括含有这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病症的方法 。
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5.发明授权Substituted 3-(diarylmethylene)indolin-2-ones and methods of their use 失效取代的3-（二芳基亚甲基）二氢吲哚-2-酮及其使用方法公开(公告)号：US07626031B2
公开(公告)日：2009-12-01
申请号：US10533555
申请日：2003-11-14
申请人： Wei Xu , Erick Wang Co , John M. Nuss , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Amy Lew Tsuhako , Jason Jevious Parks , Zhaoyang Wen , Wei Cheng
发明人： Wei Xu , Erick Wang Co , John M. Nuss , Moon Hwan Kim , Rhett Ronald Klein , Donna Tra Le , Amy Lew Tsuhako , Jason Jevious Parks , Zhaoyang Wen , Wei Cheng
IPC分类号： C07D401/00 , A61K31/445
CPC分类号： C07D403/14 , C07D401/14 , C07D413/14 , C07D451/04
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides oxindole derivatives which inhibit, regulate and/or modulate kinase receptor, particularly VEGF receptor 2 (Flk-1/KDR), FGFR1, and PDGFR (alpha and beta), signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
摘要翻译： 本发明提供调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物。 更具体地，本发明提供抑制，调节和/或调节激酶受体，特别是VEGF受体2（Flk-1 / KDR），FGFR1和PDGFR（α和β）的信号转导途径的羟吲哚衍生物，其与细胞的变化相关 如上所述的活性，含有这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病症的方法。
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公开(公告)号：US20130144056A1
公开(公告)日：2013-06-06
申请号：US13541503
申请日：2012-07-03
申请人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew Tsuhako , Morrison B. Mac , Shumeye Mamo , Zhaoyang Wen , Wei Xu , Richard George Khoury
发明人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew Tsuhako , Morrison B. Mac , Shumeye Mamo , Zhaoyang Wen , Wei Xu , Richard George Khoury
IPC分类号： C07D241/04 , C07D403/06 , C07D401/06 , C07D413/06
CPC分类号： C07D241/04 , C07C309/87 , C07D213/70 , C07D401/06 , C07D401/12 , C07D403/06 , C07D413/06
摘要： The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.
摘要翻译： 本发明提供了用于抑制ADAM-10蛋白质的化合物，具有选择性对MMP-1。 这些化合物可用于体外研究ADAM-10（及其抑制）在生物过程中的作用。 本发明还包括药物组合物，其包含一种或多种本发明的ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗癌症，关节炎和与血管发生相关的疾病。 相应地，本发明还包括治疗癌症，关节炎和与血管生成有关的疾病形式的方法，其中ADAM-10起关键作用。
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公开(公告)号：US20090143386A1
公开(公告)日：2009-06-04
申请号：US12322422
申请日：2009-02-02
申请人： S. David Brown , Lynne Canne-Bannen , Erick Wang Co , Vasu Jammalamadaka , Rickard George Khoury , Moon Hwan Kim , Donna T. Le , Amy Lew Tsuhako , Morrison B. Mac , Shumeye Mamo , John M. Nuss , Michael P. Prisbylla , Wei Xu
发明人： S. David Brown , Lynne Canne-Bannen , Erick Wang Co , Vasu Jammalamadaka , Rickard George Khoury , Moon Hwan Kim , Donna T. Le , Amy Lew Tsuhako , Morrison B. Mac , Shumeye Mamo , John M. Nuss , Michael P. Prisbylla , Wei Xu
IPC分类号： A61K31/5375 , C07C311/00 , A61K31/215 , A61K31/445 , A61K31/4965 , C07D241/04 , C07D211/30 , C07D295/00
CPC分类号： C07D409/04 , C07C311/29 , C07C2601/14 , C07D207/09 , C07D211/34 , C07D213/56 , C07D213/65 , C07D213/70 , C07D233/48 , C07D233/64 , C07D295/13 , C07D295/15 , C07D295/185 , C07D295/215 , C07D311/70
摘要： The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.
摘要翻译： 本发明提供了可用于抑制ADAM-10蛋白质的化合物。 这些化合物可用于体外研究ADAM-10（及其抑制）在生物过程中的作用。 本发明还包括药物组合物，其包含一种或多种本发明的ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗癌症，关节炎和与血管发生相关的疾病。 相应地，本发明还包括治疗癌症，关节炎和与血管生成有关的疾病形式的方法，其中ADAM-10起关键作用。 本发明还提供从其制备双芳基醚磺酰氯和ADAM-10调节剂的方法。
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公开(公告)号：US07498358B2
公开(公告)日：2009-03-03
申请号：US10498338
申请日：2002-12-13
申请人： S. David Brown , Lynne Canne-Bannen , Erick Wang Co , Vasu Jammalamadaka , Rickard George Khoury , Moon Hwan Kim , Donna T. Le , Amy Lew Tsuhako , Morrison B. Mac , Shumeye Mamo , John M. Nuss , Michael P. Prisbylla , Wei Xu
发明人： S. David Brown , Lynne Canne-Bannen , Erick Wang Co , Vasu Jammalamadaka , Rickard George Khoury , Moon Hwan Kim , Donna T. Le , Amy Lew Tsuhako , Morrison B. Mac , Shumeye Mamo , John M. Nuss , Michael P. Prisbylla , Wei Xu
IPC分类号： C07C311/19 , C07C311/29 , C07C259/06 , C07C259/08 , C07D213/32 , C07D213/68 , A61K31/16 , A61K31/44 , A61P19/02 , A61P35/00 , A61P9/10
CPC分类号： C07D409/04 , C07C311/29 , C07C2601/14 , C07D207/09 , C07D211/34 , C07D213/56 , C07D213/65 , C07D213/70 , C07D233/48 , C07D233/64 , C07D295/13 , C07D295/15 , C07D295/185 , C07D295/215 , C07D311/70
摘要： The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.
摘要翻译： 本发明提供了可用于抑制ADAM-10蛋白质的化合物。 这些化合物可用于体外研究ADAM-10（及其抑制）在生物过程中的作用。 本发明还包括药物组合物，其包含一种或多种本发明的ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗癌症，关节炎和与血管发生相关的疾病。 相应地，本发明还包括治疗癌症，关节炎和与血管生成有关的疾病形式的方法，其中ADAM-10起关键作用。 本发明还提供从其制备双芳基醚磺酰氯和ADAM-10调节剂的方法。
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公开(公告)号：US07951972B2
公开(公告)日：2011-05-31
申请号：US12322422
申请日：2009-02-02
申请人： S. David Brown , Lynne Canne-Bannen , Erick Wang Co , Vasu Jammalamadaka , Rickard George Khoury , Moon Hwan Kim , Donna T. Le , Amy Lew Tsuhako , Morrison B. Mac , Shumeye Mamo , John M. Nuss , Michael P. Prisbylla , Wei Xu
发明人： S. David Brown , Lynne Canne-Bannen , Erick Wang Co , Vasu Jammalamadaka , Rickard George Khoury , Moon Hwan Kim , Donna T. Le , Amy Lew Tsuhako , Morrison B. Mac , Shumeye Mamo , John M. Nuss , Michael P. Prisbylla , Wei Xu
IPC分类号： C07C311/19 , C07C311/29 , C07C259/06 , C07C259/08 , C07D213/32 , C07D213/68 , A61K31/16 , A61K31/44 , A61P19/02 , A61P35/00 , A61P9/10
CPC分类号： C07D409/04 , C07C311/29 , C07C2601/14 , C07D207/09 , C07D211/34 , C07D213/56 , C07D213/65 , C07D213/70 , C07D233/48 , C07D233/64 , C07D295/13 , C07D295/15 , C07D295/185 , C07D295/215 , C07D311/70
摘要： The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.
摘要翻译： 本发明提供了可用于抑制ADAM-10蛋白质的化合物。 这些化合物可用于体外研究ADAM-10（及其抑制）在生物过程中的作用。 本发明还包括药物组合物，其包含一种或多种本发明的ADAM-10抑制剂与药学上可接受的载体的组合。 这样的组合物可用于治疗癌症，关节炎和与血管发生相关的疾病。 相应地，本发明还包括治疗癌症，关节炎和与血管生成有关的疾病形式的方法，其中ADAM-10起关键作用。 本发明还提供从其制备双芳基醚磺酰氯和ADAM-10调节剂的方法。
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公开(公告)号：US20110021525A1
公开(公告)日：2011-01-27
申请号：US12839925
申请日：2010-07-20
申请人： Wei Cheng , Erick Wang Co , Moon Hwan Kim , Rhett Ronald Klein , Donna T. Le , Amy Lew Tsuhako , John M. Nuss , Wei Xu
发明人： Wei Cheng , Erick Wang Co , Moon Hwan Kim , Rhett Ronald Klein , Donna T. Le , Amy Lew Tsuhako , John M. Nuss , Wei Xu
IPC分类号： A61K31/5377 , A61K31/505 , A61P35/00 , A61P37/06 , A61P19/02 , A61P17/06 , A61P9/10 , A61P3/10 , A61P3/04 , A61P29/00 , A61P27/02 , A61P35/04 , C12N5/00 , A61K31/506
CPC分类号： C07D239/58 , C07D213/85 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/56 , C07D401/12 , C07D403/12 , C07D405/04 , C07D409/12 , C07D417/12 , C07D487/04 , C07D491/04
摘要： The invention provides compounds and methods for inhibition of kinases, more specifically p70S6 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.
摘要翻译： 本发明提供用于抑制激酶，更特别是p70S6激酶的化合物和方法。 本发明提供用于调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移，化学侵袭和代谢的化合物。 本发明的化合物抑制，调节和/或调节与上述细胞活性变化相关的激酶受体信号转导途径，本发明包括含有这些化合物的组合物，以及使用它们治疗激酶依赖性疾病和病症的方法 。
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