公开(公告)号：US20120184523A1

公开(公告)日：2012-07-19

申请号：US13427093

申请日：2012-03-22

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 Takbuchi ,  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 Takbuchi ,  Yong Wang ,  Wei Xu

IPC: 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 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.

公开(公告)号：US08013156B2

公开(公告)日：2011-09-06

申请号：US10549300

申请日：2004-03-19

Applicant: 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

Inventor： 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: C07D401/14 ,  C07D403/14 ,  A61K31/4425 ,  A61K31/495 ,  A61K31/506 ,  A61P19/02 ,  A61P35/00

CPC classification number: A61K31/496 ,  C07D213/75 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14

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. 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.

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。 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。

公开(公告)号：US20100105953A1

公开(公告)日：2010-04-29

申请号：US12605118

申请日：2009-10-23

Applicant: 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

Inventor： 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: C07C315/00

CPC classification number: C07D241/04 ,  C07C309/87 ,  C07D213/70 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D413/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07579473B2

公开(公告)日：2009-08-25

申请号：US12393806

申请日：2009-02-26

Applicant: Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Timothy Patrick Forsyth ,  Richard George Khoury ,  James William Leahy ,  Morrisson B. Mac ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Yong Wang ,  Wie Xu

Inventor： Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Timothy Patrick Forsyth ,  Richard George Khoury ,  James William Leahy ,  Morrisson B. Mac ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Yong Wang ,  Wie Xu

IPC: C07D215/38 ,  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。

公开(公告)号：US20090203577A1

公开(公告)日：2009-08-13

申请号：US12096961

申请日：2006-12-12

Applicant: Tae-Gon Baik ,  Chris A. Buhr ,  Brett B. Busch ,  Diva Sze-Ming Chan ,  Brenton T. Flatt ,  Xiao-Hui Gu ,  Vasu Jammalamadaka ,  Richard George Khoury ,  Katherine Lara ,  Sunghoon Ma ,  Richard Martin ,  Raju Mohan ,  John M. Nuss ,  Jason Jevious Parks ,  Jason H. Wu ,  Bryan K. S. Yeung ,  Wei Xu ,  Tie-Lin Wang ,  Longcheng Wang

Inventor： Tae-Gon Baik ,  Chris A. Buhr ,  Brett B. Busch ,  Diva Sze-Ming Chan ,  Brenton T. Flatt ,  Xiao-Hui Gu ,  Vasu Jammalamadaka ,  Richard George Khoury ,  Katherine Lara ,  Sunghoon Ma ,  Richard Martin ,  Raju Mohan ,  John M. Nuss ,  Jason Jevious Parks ,  Jason H. Wu ,  Bryan K. S. Yeung ,  Wei Xu ,  Tie-Lin Wang ,  Longcheng Wang

IPC: A61K31/55 ,  C07D487/04 ,  A61P3/00 ,  A61K38/22 ,  A61K38/28

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds of formula I, which exhibit affinity for the farnesoid X receptor.

Abstract translation: 本发明涉及对法呢酯X受体表现出亲和性的式I化合物。

公开(公告)号：US08178532B2

公开(公告)日：2012-05-15

申请号：US11753462

申请日：2007-05-24

Applicant: Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Timothy Patrick Forsyth ,  Richard George Khoury ,  James William Leahy ,  Morrisson B. Mac ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Yong Wang ,  Wie Xu

Inventor： Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Timothy Patrick Forsyth ,  Richard George Khoury ,  James William Leahy ,  Morrisson B. Mac ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Yong Wang ,  Wie Xu

IPC: A61K31/535 ,  C07D413/00

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，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。

公开(公告)号：US20120071653A1

公开(公告)日：2012-03-22

申请号：US13167128

申请日：2011-06-23

Applicant: 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

Inventor： 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: C07D241/04 ,  C07D413/06

CPC classification number: C07D241/04 ,  C07C309/87 ,  C07D213/70 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D413/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20120022065A1

公开(公告)日：2012-01-26

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: A61K31/5377 ,  A61K31/4709 ,  C07D239/94 ,  A61K31/517 ,  A61P35/00 ,  C07D413/14 ,  A61K31/497 ,  A61K31/513 ,  C12Q1/48 ,  C12N5/071 ,  C07D215/233 ,  C07D401/12

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。

公开(公告)号：US07989661B2

公开(公告)日：2011-08-02

申请号：US12605118

申请日：2009-10-23

Applicant: 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

Inventor： 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: C07C309/09

CPC classification number: C07D241/04 ,  C07C309/87 ,  C07D213/70 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D413/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07977345B2

公开(公告)日：2011-07-12

申请号：US11571140

申请日：2005-07-01

Applicant: Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Lisa Esther Dalrymple ,  Vasu Jammalamadaka ,  Richard George Khoury ,  James William Leahy ,  Morrisson B. Mac ,  Grace Mann ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Yong Wang ,  Wie Xu

Inventor： Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Lisa Esther Dalrymple ,  Vasu Jammalamadaka ,  Richard George Khoury ,  James William Leahy ,  Morrisson B. Mac ,  Grace Mann ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Yong Wang ,  Wie Xu

IPC: C07D487/04 ,  A61K31/519 ,  A61K31/522

CPC classification number: C07D487/04 ,  C07D209/52 ,  C07D471/04 ,  C07D473/30 ,  C07D473/32 ,  C07D493/04 ,  C07D493/14 ,  C07D493/20 ,  C07D498/04

Abstract: A compound for modulating kinase activity according to Formula I, or a pharmaceutically acceptable salt thereof, Wherein J1, J2, J3, R2, J4, Z, Ar and R3 are as defined in the specification, compositions thereof, and methods of use thereof.

Abstract translation: 用于调节根据式I的激酶活性的化合物或其药学上可接受的盐，其中J1，J2，J3，R2，J4，Z，Ar和R3如说明书，其组合物及其使用方法中所定义。