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公开(公告)号：US09174947B2
公开(公告)日：2015-11-03
申请号：US11586751
申请日：2006-10-26
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 , Wie 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 , Wie Xu
IPC分类号： C07D239/88 , A61K31/47 , A61K31/4709 , A61K31/517 , C07D215/22 , C07D215/233 , C07D295/15 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
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, KDR, 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/或调节激酶受体，特别是c-Met，KDR，c-Kit，flt-3和flt-4，与细胞活性变化相关的信号转导途径的喹啉和喹啉 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。 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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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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公开(公告)号：US08476298B2
公开(公告)日：2013-07-02
申请号：US11753503
申请日：2007-05-24
申请人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrisson B. Mac , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wie Xu
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Jeff Chen , Timothy Patrick Forsyth , Tai Phat Huynh , Vasu Jammalamadaka , Richard George Khoury , James William Leahy , Morrisson B. Mac , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wie Xu
IPC分类号： A01N43/42 , A61K31/47 , C07D239/72
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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公开(公告)号：US20120238570A1
公开(公告)日：2012-09-20
申请号：US13487559
申请日：2012-06-04
申请人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
发明人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
IPC分类号： A61K31/517 , A61K31/519 , C07D413/04 , A61P35/00 , C07D239/84 , C07D471/04 , C07D403/12 , A61K31/5377 , C07D239/70
CPC分类号： C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
摘要： The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
摘要翻译： 本发明涉及式I化合物或其单一异构体; 其中除了制备式I化合物的方法之外，化合物任选为其药学上可接受的盐，水合物，溶剂合物或其组合，以及使用式I化合物治疗癌症的方法。
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公开(公告)号：US20110201599A1
公开(公告)日：2011-08-18
申请号：US13002195
申请日：2009-07-02
申请人： Suleyman Bahceci , Bryan Chan , Diva Sze-Ming Chan , Jeff Chen , Timothy Patrick Forsyth , Maurizio Franzini , Vasu Jammalamadaka , Joon Won Jeong , Lisa Renee Jones , Ryan Michael Kelley , Moon Hwan Kim , James W. Leahy , Morrison B. Mac , Robin Tammie Noguchi , Pallavi Rao , Brian Hugh Ridgway , Wei Xu , Yong Wang
发明人： Suleyman Bahceci , Bryan Chan , Diva Sze-Ming Chan , Jeff Chen , Timothy Patrick Forsyth , Maurizio Franzini , Vasu Jammalamadaka , Joon Won Jeong , Lisa Renee Jones , Ryan Michael Kelley , Moon Hwan Kim , James W. Leahy , Morrison B. Mac , Robin Tammie Noguchi , Pallavi Rao , Brian Hugh Ridgway , Wei Xu , Yong Wang
IPC分类号： A61K31/55 , C07D471/04 , C07D401/14 , C07D403/14 , C07D413/00 , C07D413/14 , C12N5/071 , A61K31/437 , A61K31/505 , A61K31/497 , A61K31/5377 , A61P35/00 , A61P35/02 , A61P37/00
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： A compound according to Formula I: or a pharmaceutically-acceptable salt thereof, wherein R1, R3, A, B and D are as defined in the specification; pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译： 根据式I的化合物或其药学上可接受的盐，其中R 1，R 3，A，B和D如说明书中所定义; 其药物组合物及其使用方法。
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公开(公告)号：US20090105299A1
公开(公告)日：2009-04-23
申请号：US11753514
申请日：2007-05-24
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 , Morrisson B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wie 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 , Morrisson B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wie Xu
IPC分类号： A61K31/47 , C07D215/233 , A61P35/00
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，以及使用它们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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公开(公告)号：US08367667B2
公开(公告)日：2013-02-05
申请号：US13214665
申请日：2011-08-22
申请人： Lynne Canne Bannen , Jeff Chen , Lisa Esther Dalrymple , Brenton T Flatt , Timothy Patrick Forsyth , Xiao-Hui Gu , Morrison B Mac , Larry W Mann , Grace Mann , Richard Martin , Raju Mohan , Brett Murphy , Michael Charles Nyman , William C Stevens , Tie-Lin Wang , Yong Wang , Jason H Wu
发明人： Lynne Canne Bannen , Jeff Chen , Lisa Esther Dalrymple , Brenton T Flatt , Timothy Patrick Forsyth , Xiao-Hui Gu , Morrison B Mac , Larry W Mann , Grace Mann , Richard Martin , Raju Mohan , Brett Murphy , Michael Charles Nyman , William C Stevens , Tie-Lin Wang , Yong Wang , Jason H Wu
IPC分类号： A61K31/40 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/506
CPC分类号： C07D207/416 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
摘要翻译： 提供了调节受体活性的化合物，组合物和方法。 特别地提供化合物和组合物用于调节受体的活性和用于治疗，预防或改善与受体活性直接或间接相关的疾病或病症的一种或多种症状。
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公开(公告)号：US08211929B2
公开(公告)日：2012-07-03
申请号：US11722719
申请日：2005-12-28
申请人： Jeff Chen , Lisa Esther Dalrymple Meyr , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , James W. Leahy , Gary Lee Lewis , Grace Mann , Larry W. Mann , Robin Tammie Noguchi , Brian Hugh Ridgway , Joan Cruz Sangalang , Kevin Luke Schnepp , Xian Shi , Craig Stacy Takeuchi , Matthew Alan Williams , John Nuss , Atwood K. Cheung
发明人： Jeff Chen , Lisa Esther Dalrymple Meyr , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , James W. Leahy , Gary Lee Lewis , Grace Mann , Larry W. Mann , Robin Tammie Noguchi , Brian Hugh Ridgway , Joan Cruz Sangalang , Kevin Luke Schnepp , Xian Shi , Craig Stacy Takeuchi , Matthew Alan Williams , John Nuss , Atwood K. Cheung
IPC分类号： A01N43/56 , A61K31/415 , C07D239/02 , C07D231/00
CPC分类号： C07D413/14 , C07D239/48 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/04 , C07D413/12 , C07D417/14 , C07D487/04
摘要： The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The 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 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. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O—R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14. C(O)O—C1-C6 alkyl, or N(R13)—C(O)—C1-C6 alkyl; Y is H, halo, OH, C1-C6 alkyl, C0-C6alkyl-NR,15R16, NR15R,6, C1-C6 alkoxy, —N(R13)—(CH2)n-NR15R16, —C(O)O—C1-C6 alkyl, —O—(CH2)n—NR15R16, —C(O)—C1-C6 alkyl, —C0-C6-alkyl-R21, —O—R21, —C(O)—R21, —O—(CH2)n—R21, —C(O)—NR13R14, —C(O)—N(R13)-aryl, —C(O)—N(R13)(CH2)n—NR15R16, —C(O)—N(R13)—(CH2)n-aryl —C(O)—N(R13)—(CH2)n-heterocyclyl; or X and Y together with the atoms to which they are attached form a 4-7 membered heterocyclyl or heteroaryl group containing one or two heteroatoms independently selected from O, N, and S. Z is H, NR2R3, —S—R2a, or —O—R2a
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公开(公告)号：US20120070368A1
公开(公告)日：2012-03-22
申请号：US13087094
申请日：2011-04-14
申请人： Lynne Canne Bannen , Diva Sze-Ming Chan , Timothy Patrick Forsyth , Richard George Khoury , James William Leahy , Morrison B. Mac , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Yong Wang , Wei Xu , Diane Simeone
发明人： Lynne Canne Bannen , Diva Sze-Ming Chan , Timothy Patrick Forsyth , Richard George Khoury , James William Leahy , Morrison B. Mac , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Yong Wang , Wei Xu , Diane Simeone
CPC分类号： A61K31/47 , A61K31/517 , A61K31/7068 , A61K45/06 , A61N5/10 , A61K2300/00
摘要： Disclosed are methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt thereof, in combination with gemcitabine (GEM), or a pharmaceutically acceptable salt thereof, and optionally one or more additional treatments, wherein:R1 is halo;R2 is halo;R3 is (C1-C6)alkyl;R4 is (C1-C6)alkyl; andQ is CH or N.
摘要翻译： 公开了通过给予式I化合物或其药学上可接受的盐与吉西他滨（GEM）或其药学上可接受的盐以及任选的一种或多种另外的治疗组合治疗癌症的方法，其中：R1是卤素; R2是卤素; R3是（C1-C6）烷基; R4是（C1-C6）烷基; Q为CH或N.
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公开(公告)号：US08067436B2
公开(公告)日：2011-11-29
申请号：US11753514
申请日：2007-05-24
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 , Morrisson B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wie 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 , Morrisson B. Mac , Grace Mann , Larry W. Mann , John M. Nuss , Jason Jevious Parks , Craig Stacy Takeuchi , Yong Wang , Wie Xu
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/517 , A61K31/5377
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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