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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
Applicant: 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
Inventor： 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: A01N43/56 , A61K31/415 , C07D239/02 , C07D231/00
CPC classification number: C07D413/14 , C07D239/48 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/04 , C07D413/12 , C07D417/14 , C07D487/04
Abstract: 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：US08067436B2
公开(公告)日：2011-11-29
申请号：US11753514
申请日：2007-05-24
Applicant: 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
Inventor： 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: A61K31/47 , A61K31/4709 , A61K31/517 , A61K31/5377
CPC classification number: 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
Abstract: 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.
Abstract translation: 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：US20090170896A1
公开(公告)日：2009-07-02
申请号：US12393806
申请日：2009-02-26
Applicant: Lynn 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
Inventor： Lynn 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: A61K31/47 , C07D215/20 , A61P35/00
CPC classification number: 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
Abstract: 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：US09174947B2
公开(公告)日：2015-11-03
申请号：US11586751
申请日：2006-10-26
Applicant: 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
Inventor： 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: C07D239/88 , A61K31/47 , A61K31/4709 , A61K31/517 , C07D215/22 , C07D215/233 , C07D295/15 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
CPC classification number: 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
Abstract: 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.
Abstract translation: 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
Applicant: 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
Inventor： 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: A61K31/47
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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Patent Agency Ranking
公开(公告)号：US08476298B2
公开(公告)日：2013-07-02
申请号：US11753503
申请日：2007-05-24
Applicant: 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
Inventor： 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: A01N43/42 , A61K31/47 , C07D239/72
CPC classification number: 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
Abstract: 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.
Abstract translation: 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
Applicant: 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
Inventor： 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: A61K31/517 , A61K31/519 , C07D413/04 , A61P35/00 , C07D239/84 , C07D471/04 , C07D403/12 , A61K31/5377 , C07D239/70
CPC classification number: C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
Abstract: 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.
Abstract translation: 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：US20090105299A1
公开(公告)日：2009-04-23
申请号：US11753514
申请日：2007-05-24
Applicant: 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
Inventor： 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: A61K31/47 , C07D215/233 , A61P35/00
CPC classification number: 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
Abstract: 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.
Abstract translation: 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：US08222263B2
公开(公告)日：2012-07-17
申请号：US12049225
申请日：2008-03-14
Applicant: 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
Inventor： 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: A61K31/517 , A01N43/54
CPC classification number: C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
Abstract: 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.
Abstract translation: 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：US08088767B2
公开(公告)日：2012-01-03
申请号：US12443103
申请日：2007-09-28
Applicant: Adam Antoni Galan , Jeff Chen , Hongwang Du , Timothy Forsyth , Tai Phat Huynh , Henry William Beecroft Johnson , Patrick Kearney , James W. Leahy , Matthew Sangyup Lee , Grace Mann , Brian Hugh Ridgway , Craig Stacy Takeuchi , Peiwen Zhou
Inventor： Adam Antoni Galan , Jeff Chen , Hongwang Du , Timothy Forsyth , Tai Phat Huynh , Henry William Beecroft Johnson , Patrick Kearney , James W. Leahy , Matthew Sangyup Lee , Grace Mann , Brian Hugh Ridgway , Craig Stacy Takeuchi , Peiwen Zhou
IPC: A61K31/5377 , A61K31/4439 , A61K31/4184 , C07D413/14 , C07D401/14 , C07D403/12
CPC classification number: C07D405/14 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14
Abstract: This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.
Abstract translation: 本发明涉及蛋白酪氨酸激酶及其抑制剂的领域。 特别地，本发明涉及JAK-2抑制剂，用于抑制JAK-2的化合物的药物组合物，抑制细胞中JAK-2的方法，包括使需要JAK-2抑制的细胞与化合物 或包含根据本发明的化合物的药物组合物。 还包括治疗涉及JAK-2的疾病或病症的方法，包括向患者施用包含本发明化合物的药物组合物。
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