公开(公告)号：US08592459B2

公开(公告)日：2013-11-26

申请号：US12759578

申请日：2010-04-13

申请人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

发明人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

IPC分类号： A61K31/4439 ,  C07D401/12

CPC分类号： C07D401/14 ,  Y02P20/55

摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

公开(公告)号：US07732465B2

公开(公告)日：2010-06-08

申请号：US12315779

申请日：2008-12-05

申请人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

发明人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

IPC分类号： A61K31/4439

CPC分类号： C07D401/14 ,  Y02P20/55

摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

摘要翻译： 提供了新的取代的苯并咪唑化合物，组合物和抑制与人或动物受试者的肿瘤发生相关的激酶活性的方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。

公开(公告)号：US20090170904A1

公开(公告)日：2009-07-02

申请号：US12315779

申请日：2008-12-05

申请人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

发明人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

IPC分类号： A61K31/4439 ,  A61P35/00

CPC分类号： C07D401/14 ,  Y02P20/55

摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

公开(公告)号：US20100234394A1

公开(公告)日：2010-09-16

申请号：US12759578

申请日：2010-04-13

申请人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

发明人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

IPC分类号： A61K31/496 ,  C07D401/14 ,  A61K31/4439 ,  A61K31/444 ,  A61P35/00

CPC分类号： C07D401/14 ,  Y02P20/55

摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

摘要翻译： 提供了新的取代的苯并咪唑化合物，组合物和抑制与人或动物受试者中的肿瘤发生相关的激酶活性的方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。

公开(公告)号：US07482367B2

公开(公告)日：2009-01-27

申请号：US11513959

申请日：2006-08-30

申请人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

发明人： Mina E. Aikawa ,  Payman Amiri ,  Jeffrey H. Dove ,  Barry Haskell Levine ,  Christopher McBride ,  Teresa E. Pick ,  Daniel J. Poon ,  Savithri Ramurthy ,  Paul A. Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

IPC分类号： A61K31/4439 ,  C07D401/14

CPC分类号： C07D401/14 ,  Y02P20/55

摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

摘要翻译： 提供了新的取代的苯并咪唑化合物，组合物和抑制与人或动物受试者中的肿瘤发生相关的激酶活性的方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。

公开(公告)号：US20070161680A1

公开(公告)日：2007-07-12

申请号：US11513959

申请日：2006-08-30

申请人： Mina Alkawa ,  Payman Amiri ,  Jeffrey Dove ,  Barry Levine ,  Christopher McBride ,  Teresa Pick ,  Daniel Poon ,  Savithri Ramurthy ,  Paul Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

发明人： Mina Alkawa ,  Payman Amiri ,  Jeffrey Dove ,  Barry Levine ,  Christopher McBride ,  Teresa Pick ,  Daniel Poon ,  Savithri Ramurthy ,  Paul Renhowe ,  Cynthia Shafer ,  Darrin Stuart ,  Sharadha Subramanian

IPC分类号： A61K31/4439 ,  C07D403/14

CPC分类号： C07D401/14 ,  Y02P20/55

摘要： New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

摘要翻译： 提供了新的取代的苯并咪唑化合物，组合物和抑制与人或动物受试者的肿瘤发生相关的激酶活性的方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药剂组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。

公开(公告)号：US20140057904A1

公开(公告)日：2014-02-27

申请号：US14066734

申请日：2013-10-30

申请人： Carlos Garcia-Echeverria ,  Sauveur-Michel Maira ,  Darrin Stuart ,  Susan Wee ,  Christine Fritsch ,  Tobi Nagel

发明人： Carlos Garcia-Echeverria ,  Sauveur-Michel Maira ,  Darrin Stuart ,  Susan Wee ,  Christine Fritsch ,  Tobi Nagel

IPC分类号： A61K31/5377 ,  A61K45/06 ,  A61K31/437 ,  A61K31/166 ,  A61K31/4439

CPC分类号： A61K31/4745 ,  A61K31/166 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

摘要： The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.

摘要翻译： 本发明涉及药物组合，其包含（a）磷酸肌醇3-激酶抑制剂化合物和（b）调节Ras / Raf / Mek途径用于治疗增殖性疾病，特别是实体瘤疾病的化合物; 包含这种组合的药物组合物; 使用这种组合来制备用于治疗增殖性疾病的药物; 包括作为用于同时，分开或顺序使用的组合制剂的组合的商业包装或产品; 以及治疗温血动物，特别是人的方法。

公开(公告)号：US20110105521A1

公开(公告)日：2011-05-05

申请号：US13003581

申请日：2009-07-10

申请人： Carlos Garcia-Echeverria ,  Sauveur-Michel Maira ,  Darrin Stuart ,  Susan Wee ,  Christine Fritsch ,  Tobi Nagel

发明人： Carlos Garcia-Echeverria ,  Sauveur-Michel Maira ,  Darrin Stuart ,  Susan Wee ,  Christine Fritsch ,  Tobi Nagel

IPC分类号： A61K31/496 ,  A61K31/4745 ,  A61P35/00 ,  A61P35/02

CPC分类号： A61K31/4745 ,  A61K31/166 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

摘要： The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.

摘要翻译： 本发明涉及药物组合，其包含（a）磷酸肌醇3-激酶抑制剂化合物和（b）调节Ras / Raf / Mek途径用于治疗增殖性疾病，特别是实体瘤疾病的化合物; 包含这种组合的药物组合物; 使用这种组合来制备用于治疗增殖性疾病的药物; 包括作为用于同时，分开或顺序使用的组合制剂的组合的商业包装或产品; 以及治疗温血动物，特别是人的方法。

公开(公告)号：US20110092546A1

公开(公告)日：2011-04-21

申请号：US12997770

申请日：2009-06-11

申请人： Darrin Stuart

发明人： Darrin Stuart

IPC分类号： A61K31/4439 ,  A61P35/00

CPC分类号： A61K31/4439

摘要： The present invention relates to the use of BENZIMIDAZOLE DERIVATIVES for the preparation of a drug for the treatment of neurofibromatosis.

摘要翻译： 本发明涉及苯扎咪唑衍生物在制备用于治疗神经纤维瘤病的药物中的用途。

公开(公告)号：US20150265616A1

公开(公告)日：2015-09-24

申请号：US14419256

申请日：2013-08-05

申请人： Giordano Caponigro ,  Darrin Stuart ,  Laure Moutouh-De Parseval

发明人： Giordano Caponigro ,  Darrin Stuart ,  Laure Moutouh-De Parseval

IPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/517 ,  A61K39/395

CPC分类号： A61K31/506 ,  A61K31/4439 ,  A61K31/517 ,  A61K39/39558 ,  A61K2300/00

摘要： A pharmaceutical combination comprising (a) a B-Raf inhibitor, (b) a EGFR inhibitor and, optionally, (c) a PI3K inhibitor; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.

摘要翻译： 一种药物组合，其包含（a）B-Raf抑制剂，（b）EGFR抑制剂和任选的（c）PI3K抑制剂; 这种组合在增殖性疾病治疗中的应用; 以及治疗患有增殖性疾病的受试者的方法，包括施用治疗有效量的这种组合。