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公开(公告)号：US08012956B2
公开(公告)日：2011-09-06
申请号：US12290159
申请日：2008-10-27
Applicant: Kenneth D. Rice , Naing Aay , Neel Kumar Anand , Arlyn Arcalas , Tae-Gon Baik , Charles M. Blazey , Owen Joseph Bowles , Chris A. Buhr , Joerg Bussenius , Simona Costanzo , Jeffrey Kimo Curtis , Steven Charles Defina , Larisa Dubenko , Abigail R. Kennedy , Angie Inyoung Kim , Katherine Lara , Sunghoon Ma , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Longcheng Wang
Inventor： Kenneth D. Rice , Naing Aay , Neel Kumar Anand , Arlyn Arcalas , Tae-Gon Baik , Charles M. Blazey , Owen Joseph Bowles , Chris A. Buhr , Joerg Bussenius , Simona Costanzo , Jeffrey Kimo Curtis , Steven Charles Defina , Larisa Dubenko , Abigail R. Kennedy , Angie Inyoung Kim , Katherine Lara , Sunghoon Ma , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Longcheng Wang
IPC: A61K31/46 , A61K31/5377 , A61K31/496 , A61K31/497 , C07D451/04
CPC classification number: C07D451/02
Abstract: A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
Abstract translation: 根据式I或II的化合物：其中R1，R1b，R2，L1和L2和L2b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：US20100305093A1
公开(公告)日：2010-12-02
申请号：US12756374
申请日：2010-04-08
Applicant: Neel Kumar Anand , Arlyn Arcalas , Charles M. Blazey , Chris A. Buhr , Jonah Cannoy , Sergey Ephsteyn , Henry William Beecroft Johnson , Anagha Joshi , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Sunghoon Ma , Morrison B. Mac , John M. Nuss , Craig Stacy Takeuchi , Longcheng Wang , Yong Wang
Inventor： Neel Kumar Anand , Arlyn Arcalas , Charles M. Blazey , Chris A. Buhr , Jonah Cannoy , Sergey Ephsteyn , Henry William Beecroft Johnson , Anagha Joshi , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Sunghoon Ma , Morrison B. Mac , John M. Nuss , Craig Stacy Takeuchi , Longcheng Wang , Yong Wang
IPC: A61K31/553 , C07D405/10 , A61P35/00 , A61P37/00 , A61P35/02 , A61P27/00
CPC classification number: C07D267/14 , C07D413/04
Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐或溶剂合物，以及制备和使用该化合物的方法。
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3.发明申请Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases 有权Azetidines作为MEK抑制剂治疗增殖性疾病公开(公告)号：US20100249096A1
公开(公告)日：2010-09-30
申请号：US12774544
申请日：2010-05-05
Applicant: Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
Inventor： Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
IPC: A61K31/397 , C07D205/04 , C07D401/04 , C07D403/04 , C07D413/06 , C07D403/06 , C07D401/14 , A61K31/496 , A61K31/4523 , A61K31/5377 , A61K31/4025 , A61P35/00
CPC classification number: C07D205/04 , C07D205/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐和溶剂化物。 这些化合物是MEK抑制剂，可用于治疗增殖性疾病如癌症。 还公开了含有这些化合物的药物组合物以及使用本发明化合物和组合物治疗癌症的方法。
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4.发明授权Azetidines as MEK inhibitors for the treatment of proliferative diseases 有权Azetidines作为治疗增殖性疾病的MEK抑制剂公开(公告)号：US07803839B2
公开(公告)日：2010-09-28
申请号：US11995928
申请日：2006-10-05
Applicant: Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
Inventor： Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
IPC: A61K31/27 , C07D205/00
CPC classification number: C07D205/04 , C07D205/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐和溶剂化物。 这些化合物是MEK抑制剂，可用于治疗增殖性疾病如癌症。 还公开了含有这些化合物的药物组合物以及使用本发明化合物和组合物治疗癌症的方法。
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公开(公告)号：US20090163471A1
公开(公告)日：2009-06-25
申请号：US12290159
申请日：2008-10-27
Applicant: Kenneth D. Rice , Naing Aay , Neel Kumar Anand , Arlyn Arcalas , Tae-Gon Baik , Charles M. Blazey , Owen Joseph Bowles , Chris A. Buhr , Joerg Bussenius , Simona Costanzo , Jeffrey Kimo Curtis , Steven Charles Defina , Larisa Dubenko , Abigail R. Kennedy , Angie Inyoung Kim , Katherine Lara , Sunghoon Ma , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Longcheng Wang
Inventor： Kenneth D. Rice , Naing Aay , Neel Kumar Anand , Arlyn Arcalas , Tae-Gon Baik , Charles M. Blazey , Owen Joseph Bowles , Chris A. Buhr , Joerg Bussenius , Simona Costanzo , Jeffrey Kimo Curtis , Steven Charles Defina , Larisa Dubenko , Abigail R. Kennedy , Angie Inyoung Kim , Katherine Lara , Sunghoon Ma , Jean-Claire Limun Manalo , Csaba J. Peto , Tsze H. Tsang , Longcheng Wang
IPC: A61K31/46 , C07D451/04 , A61K31/5377 , A61K31/496 , A61K31/497
CPC classification number: C07D451/02
Abstract: A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
Abstract translation: 根据式I或II的化合物：其中R1，R1b，R2，L1和L2和L2b如说明书中所定义，其药物组合物及其使用方法。
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Patent Agency Ranking
公开(公告)号：US20110071145A1
公开(公告)日：2011-03-24
申请号：US12903031
申请日：2010-10-12
Applicant: Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Steven Charles Defina , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Anagha Abhijit Joshi
Inventor： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Larisa Dubenko , Abigail R. Kennedy , Steven Charles Defina , Angie I. Kim , Jean-Claire L. Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Anagha Abhijit Joshi
IPC: A61K31/4184 , A61P35/00 , A61P19/02 , A61P9/10 , A61P1/00 , A61P9/00 , A61K31/538 , A61K31/498 , A61K31/416 , A61K31/4439 , A61K31/5377 , A61K31/454 , A61K31/496
CPC classification number: C07D413/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X 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 Raf. 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.
Abstract translation: 本发明涉及式I化合物，其中G，A，X 1，X 2，X 3，Z，E，Y和X如本文所定义。 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Raf。 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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7.发明申请Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture 失效苯并西泮作为PI3K / mTOR的抑制剂及其使用和制造方法公开(公告)号：US20100298290A1
公开(公告)日：2010-11-25
申请号：US12784254
申请日：2010-05-20
Applicant: Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Chris Allen Buhr , Joerg Bussenius , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Anagha Joshi , Angie Inyoung Kim , Amy Lew Tsuhako , Sunghoon Ma , Jean-Claire Limun Manalo , Stephanie Ng , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Cristiana A. Zaharia
Inventor： Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Chris Allen Buhr , Joerg Bussenius , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Anagha Joshi , Angie Inyoung Kim , Amy Lew Tsuhako , Sunghoon Ma , Jean-Claire Limun Manalo , Stephanie Ng , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Cristiana A. Zaharia
IPC: A61K31/553 , C07D413/14 , A61P35/00 , A61P35/04
CPC classification number: C07D413/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/08 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐或溶剂合物，以及制备和使用该化合物的方法。
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8.发明申请Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases 有权Azetidines作为MEK抑制剂治疗增殖性疾病公开(公告)号：US20090156576A1
公开(公告)日：2009-06-18
申请号：US11995928
申请日：2006-10-05
Applicant: Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
Inventor： Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
IPC: A61K31/397 , C07D205/04 , C07D401/14 , C07D403/06 , C07D471/04 , C07D413/06
CPC classification number: C07D205/04 , C07D205/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐和溶剂化物。 这些化合物是MEK抑制剂，可用于治疗增殖性疾病如癌症。 还公开了含有这些化合物的药物组合物以及使用本发明化合物和组合物治疗癌症的方法。
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9.发明授权Azetidines as MEK inhibitors for the treatment of proliferative diseases 有权Azetidines作为治疗增殖性疾病的MEK抑制剂公开(公告)号：US08362002B2
公开(公告)日：2013-01-29
申请号：US13048832
申请日：2011-03-15
Applicant: Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
Inventor： Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
IPC: A61K31/397 , A61K31/50 , A61K31/505 , A61K31/4523 , A61K31/4178
CPC classification number: C07D205/04 , C07D205/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐和溶剂化物。 这些化合物是MEK抑制剂，可用于治疗增殖性疾病如癌症。 还公开了含有这些化合物的药物组合物以及使用本发明化合物和组合物治疗癌症的方法。
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10.发明申请Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases 有权Azetidines作为MEK抑制剂治疗增殖性疾病公开(公告)号：US20110263558A1
公开(公告)日：2011-10-27
申请号：US13048832
申请日：2011-03-15
Applicant: Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
Inventor： Naing Aay , Neel Kumar Anand , Charles M. Blazey , Owen Joseph Bowles , Joerg Bussenius , Simona Costanzo , Jeffry Kimo Curtis , Steven Charles DeFina , Larisa Dubenko , Anagha Abhijit Joshi , Abigail R. Kennedy , Angie Inyoung Kim , Elena S. Koltun , Jean-Claire Limun Manalo , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang
IPC: A61K31/397 , C07D413/06 , C07D401/04 , A61P35/00 , C07D471/04 , C07D403/04 , C07D401/06 , A61K31/5377 , C07D205/04 , C07D403/06
CPC classification number: C07D205/04 , C07D205/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐和溶剂化物。 这些化合物是MEK抑制剂，可用于治疗增殖性疾病，例如癌症。 还公开了含有这些化合物的药物组合物以及使用本发明化合物和组合物治疗癌症的方法。
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