专利检索 ap:"Larisa Dubenko" 第 1 页

1.

发明授权
Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture 失效
标题翻译：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：US08637499B2

公开(公告)日：2014-01-28

申请号：US13322160

申请日：2010-05-25

申请人： Naing Aay , Arlyn Arcalas , Joerg Bussenius , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Angie Inyoung Kim , Jean-Claire Limun Manalo , Michael Pack , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Owen Joseph Bowles , Jeffry Kimo Curtis

发明人： Naing Aay , Arlyn Arcalas , Joerg Bussenius , Steven Charles DeFina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Angie Inyoung Kim , Jean-Claire Limun Manalo , Michael Pack , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Owen Joseph Bowles , Jeffry Kimo Curtis

IPC分类号： A61P35/00 , A61K31/553 , C07D267/14

CPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04

摘要： The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer in which activity against PI3fC-alph mTOR, or both contributes to its pathology and/or symptomatology include breast cancer mantle cell lymphoma, renal cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, NPM/ALK-transformed anaplastic large cell lymphoma, diffu large B cell lymphoma, rhabdomyosarcoma, ovarian cancer, endometrial cancer, cervic cancer, non small cell lung carcinoma, small cell lung carcinoma, adenocarcinoma, col cancer, rectal cancer, gastric carcinoma, hepatocellular carcinoma, melanoma, pancreat cancer, prostate carcinoma, thyroid carcinoma, anaplastic large cell lymphoma, hemangiom glioblastoma, or head and neck cancer.

摘要翻译： 本发明涉及式（I）的化合物：本发明提供抑制，调节和/或调节P13K和/或mTOR的化合物，其可用于治疗哺乳动物中过度增殖性疾病如癌症。本发明还提供了使用这些化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗方法和含有这些化合物的药物组合物的方法。例如，其中针对PI3fC-alph mTOR或其两者都有助于其病理学和/或症状学的活性的癌症包括乳腺癌套细胞淋巴瘤，肾细胞癌，急性骨髓性白血病，慢性骨髓性白血病，NPM / ALK转化的间变型大细胞淋巴瘤，弥漫性大B细胞淋巴瘤，横纹肌肉瘤，卵巢癌，子宫内膜癌，宫颈癌，非小细胞肺癌，小细胞肺癌，腺癌，胆囊癌，直肠癌，胃癌，肝细胞癌，黑素瘤，胰腺癌，前列腺癌，甲状腺癌，间变性大细胞淋巴瘤，血管瘤胶质母细胞瘤或头颈癌。

2.

发明授权
Azetidines as MEK inhibitors for the treatment of proliferative diseases 有权
标题翻译： 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

申请人： 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

发明人： 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分类号： A61K31/397 , A61K31/50 , A61K31/505 , A61K31/4523 , A61K31/4178

CPC分类号： 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

摘要： 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.

摘要翻译： 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。

3.

发明申请
Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture 失效
标题翻译：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：US20120258953A1

公开(公告)日：2012-10-11

申请号：US13322160

申请日：2010-05-25

申请人： Naing Aay , Arlyn Arcalas , Joerg Bussenius , Charles Steven Defina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Angie Inyoung Kim , Jean-Claire Limun Manalo , Michael Pack , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Owen Joseph Bowles , Jeffry Kimo Curtis

发明人： Naing Aay , Arlyn Arcalas , Joerg Bussenius , Charles Steven Defina , Larisa Dubenko , Jason R. Harris , Eileen E. Jackson-Ugueto , Angie Inyoung Kim , Jean-Claire Limun Manalo , Michael Pack , Csaba J. Peto , Kenneth D. Rice , Tsze H. Tsang , Owen Joseph Bowles , Jeffry Kimo Curtis

IPC分类号： A61K31/553 , A61P35/02 , A61P35/00 , C07D267/14 , C07D225/02

CPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04

摘要： The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer in which activity against PI3fC-alph mTOR, or both contributes to its pathology and/or symptomatology include breast cancer mantle cell lymphoma, renal cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, NPM/ALK-transformed anaplastic large cell lymphoma, diffu large B cell lymphoma, rhabdomyosarcoma, ovarian cancer, endometrial cancer, cervic cancer, non small cell lung carcinoma, small cell lung carcinoma, adenocarcinoma, col cancer, rectal cancer, gastric carcinoma, hepatocellular carcinoma, melanoma, pancreat cancer, prostate carcinoma, thyroid carcinoma, anaplastic large cell lymphoma, hemangiom glioblastoma, or head and neck cancer.

摘要翻译： 本发明涉及式（I）的化合物：本发明提供抑制，调节和/或调节P13K和/或mTOR的化合物，其可用于治疗哺乳动物中过度增殖性疾病如癌症。本发明还提供了使用这些化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗方法和含有这些化合物的药物组合物的方法。例如，其中针对PI3fC-alph mTOR或其两者都有助于其病理学和/或症状学的活性的癌症包括乳腺癌套细胞淋巴瘤，肾细胞癌，急性骨髓性白血病，慢性骨髓性白血病，NPM / ALK转化的间变型大细胞淋巴瘤，弥漫性大B细胞淋巴瘤，横纹肌肉瘤，卵巢癌，子宫内膜癌，宫颈癌，非小细胞肺癌，小细胞肺癌，腺癌，胆囊癌，直肠癌，胃癌，肝细胞癌，黑素瘤，胰腺癌，前列腺癌，甲状腺癌，间变性大细胞淋巴瘤，血管瘤胶质母细胞瘤或头颈癌。

4.

发明申请
Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases 有权
标题翻译： 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

申请人： 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

发明人： 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分类号： A61K31/397 , C07D413/06 , C07D401/04 , A61P35/00 , C07D471/04 , C07D403/04 , C07D401/06 , A61K31/5377 , C07D205/04 , C07D403/06

CPC分类号： 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

摘要： 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.

摘要翻译： 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。

5.

发明授权
Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture 失效
标题翻译：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：US08648066B2

公开(公告)日：2014-02-11

申请号：US12784254

申请日：2010-05-20

申请人： 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

发明人： 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分类号： A61P35/00 , A61K31/553 , C07D267/14

CPC分类号： C07D413/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/08 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00

摘要： 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.

摘要翻译： 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。

6.

发明授权
Protein kinase modulators and methods of use 失效
标题翻译：蛋白激酶调节剂和使用方法

公开(公告)号：US07704995B2

公开(公告)日：2010-04-27

申请号：US10513081

申请日：2003-05-02

申请人： Chris A. Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Wang Co , Sergey Epshteyn , Abigail R Kennedy , Baili Chen , Larisa Dubenko , Neel Kumar Anand , Tsze H. Tsang , John M. Nuss , Csaba J Peto , Kenneth D. Rice , Mohamed Abdulkader Ibrahim , Kevin Luke Schnepp , Xian Shi , James William Leahy , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Grace Mann , Larry Wayne Mann , Craig Stacy Takeuchi , Peter Lamb , David J. Matthews , Nicole Miller

发明人： Chris A. Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Wang Co , Sergey Epshteyn , Abigail R Kennedy , Baili Chen , Larisa Dubenko , Neel Kumar Anand , Tsze H. Tsang , John M. Nuss , Csaba J Peto , Kenneth D. Rice , Mohamed Abdulkader Ibrahim , Kevin Luke Schnepp , Xian Shi , James William Leahy , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Grace Mann , Larry Wayne Mann , Craig Stacy Takeuchi , Peter Lamb , David J. Matthews , Nicole Miller

IPC分类号： C07D279/16 , C07D279/12 , C07D417/12 , C07D265/36 , C07D413/12 , C07D403/12 , C07D401/12 , C07D405/12 , C07D409/12 , C07D411/12 , C07D419/12 , C07D241/18 , C07D241/20 , A61K31/55 , A61K31/497 , A61K31/5355 , A61K31/541 , C07D305/12 , C07D307/79 , A61K31/44 , A61P35/00

CPC分类号： C07D241/26 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12

摘要： This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.

摘要翻译： 本发明涉及用于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，以及含有这些化合物的药物组合物。更具体地，本发明涉及抑制，调节和/或调节激酶，特别是检查点激酶，甚至更特别是检查点激酶1或Chk1的化合物。治疗或预防性地使用化合物和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，并且包括通过以下方法治疗癌症以及与不期望的血管生成和/或细胞增殖相关的其它疾病状态，施用有效量的这些化合物。

7.

发明申请
Kinase Modulators and Methods of Use 失效
标题翻译：激酶调节剂和使用方法

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。