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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：US20100105953A1
公开(公告)日：2010-04-29
申请号：US12605118
申请日：2009-10-23
申请人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew , 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 , Morrison B. Mac , Shumeye Mamo , Zhaoyang Wen , Wei Xu , Richard George Khoury
IPC分类号： C07C315/00
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：US20120071653A1
公开(公告)日：2012-03-22
申请号：US13167128
申请日：2011-06-23
申请人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew , 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 , Morrison B. Mac , Shumeye Mamo , Zhaoyang Wen , Wei Xu , Richard George Khoury
IPC分类号： C07D241/04 , 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：US07989661B2
公开(公告)日：2011-08-02
申请号：US12605118
申请日：2009-10-23
申请人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew , 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 , Morrison B. Mac , Shumeye Mamo , Zhaoyang Wen , Wei Xu , Richard George Khoury
IPC分类号： C07C309/09
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：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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公开(公告)号：US07629341B2
公开(公告)日：2009-12-08
申请号：US10518110
申请日：2003-06-11
申请人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew , Shumeye Mamo , Zhaoyang Wen , Wei Xu
发明人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew , Shumeye Mamo , Zhaoyang Wen , Wei Xu
IPC分类号： C07D213/10 , C07D401/06 , C07D401/12 , C07D241/04 , A61K31/495 , A61K31/496 , A61K31/5377
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：US20120184523A1
公开(公告)日：2012-07-19
申请号：US13427093
申请日：2012-03-22
申请人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takbuchi , Yong Wang , Wei Xu
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takbuchi , Yong Wang , Wei Xu
IPC分类号： A61K31/4709 , A61K31/517 , C07D215/233 , C07D401/12 , A61K31/47 , C07D239/94 , C07D417/12 , C07D401/10 , C07D413/12 , A61K31/5377 , C07D215/46 , C07D417/14 , A61K31/501 , A61K31/496 , A61K31/513 , C12N9/99 , C12Q1/48 , C12Q1/66 , A61P35/00 , A61P29/00 , A61P37/00 , A61P37/06 , A61P25/00 , A61P17/06 , A61P9/00 , A61P9/10 , A61P1/00 , A61P19/02 , A61P27/02 , C07D403/10
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
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 quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, 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. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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公开(公告)号：US08013156B2
公开(公告)日：2011-09-06
申请号：US10549300
申请日：2004-03-19
申请人： Lynne Canne Bannen , S. David Brown , Wei Cheng , Vasu Jammalamadaka , John M. Nuss , Morrison B. Mac , Jason Jevious Parks , Matthew A. Williams , Wei Xu , Atwood Kim Cheung , Lisa Esther Dalrymple , Sergey Epshteyn , Mohamed Abdulkader Ibrahim , James William Leahy , Gary Lee Lewis , Robin Tammie Noguchi , Larry Wayne Mann , Brian Hugh Ridgway , Joan C. Sangalang , Kevin Luke Schnepp , Xian Shi , Richard George Khoury
发明人： Lynne Canne Bannen , S. David Brown , Wei Cheng , Vasu Jammalamadaka , John M. Nuss , Morrison B. Mac , Jason Jevious Parks , Matthew A. Williams , Wei Xu , Atwood Kim Cheung , Lisa Esther Dalrymple , Sergey Epshteyn , Mohamed Abdulkader Ibrahim , James William Leahy , Gary Lee Lewis , Robin Tammie Noguchi , Larry Wayne Mann , Brian Hugh Ridgway , Joan C. Sangalang , Kevin Luke Schnepp , Xian Shi , Richard George Khoury
IPC分类号： C07D401/14 , C07D403/14 , A61K31/4425 , A61K31/495 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： A61K31/496 , C07D213/75 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D417/14
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. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using 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。 本发明的化合物抑制，调节和/或调节激酶，特别是Tie-2。 使用化合物及其药物组合物治疗激酶依赖性疾病和病症的方法也是本发明的一个方面。
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公开(公告)号：US08497284B2
公开(公告)日：2013-07-30
申请号：US13249815
申请日：2011-09-30
申请人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrison B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wei Xu
IPC分类号： A61K31/47
CPC分类号： C07D215/233 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D215/22 , C07D215/36 , C07D215/38 , C07D215/46 , C07D239/88 , C07D239/94 , C07D295/15 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C12Q1/485 , G01N2500/04 , Y02A50/393
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 quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, 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. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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/或调节与细胞活性变化相关的激酶受体，特别是c-Met，KDF，c-Kit，flt-3和flt-4信号转导途径的喹唑啉和喹啉 如上所述，含有这些化合物的组合物，及其用于治疗激酶依赖性疾病和病症的方法。 本发明还提供了制备上述化合物的方法和含有这些化合物的组合物。
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