- N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridin yl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine for use in the treatment of antimitotic agent resistant cancer
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The present invention relates to methods of using the compound, N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine or a pharmaceutically acceptable salt thereof, to treat cancers, including solid tumors, which have become resistant to treatment with chemotherapeutic agents, including anti-mitotic agents such as taxanes, and/or other anti-cancer agents, including aurora kinase inhibiting agents. The invention also includes methods of treating cancers refractory to such treatments by administering a pharmaceutical composition, comprising the compound to a cancer subject.
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Paragraph 0032; 0033
(2018/12/13)
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- CRYSTALLINE FORMS OF N-(4-((3-(2-AMINO-4-PYRIMIDINYL) - 2-PYRIDINYL)OXY)PHENYL)-4-(4-METHYL-2-THIENYL)-1 -PHTHALAZINAMINE PHARMACEUTICALLY ACCEPTABLE SALTS AND USES THEREOF
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The present invention relates to crystalline forms and co-crystal forms of pharmaceutically acceptable salts of the compound, N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine (AMG 900, and pharmaceutical compositions comprising said crystalline and co-crystal forms thereof. The invention further provides uses of the crystalline foms and compositions, to treat cancer, including various types of solid tumors and hematologic cancer including myeloma and leukemia.
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Page/Page column 17
(2015/06/18)
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- Discovery of N -(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines
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Efforts to improve upon the physical properties and metabolic stability of Aurora kinase inhibitor 14a revealed that potency against multidrug-resistant cell lines was compromised by increased polarity. Despite its high in vitro metabolic intrinsic cleara
- Geuns-Meyer, Stephanie,Cee, Victor J.,Deak, Holly L.,Du, Bingfan,Hodous, Brian L.,Nguyen, Hanh Nho,Olivieri, Philip R.,Schenkel, Laurie B.,Vaida, Karina R.,Andrews, Paul,Bak, Annette,Be, Xuhai,Beltran, Pedro J.,Bush, Tammy L.,Chaves, Mary K.,Chung, Grace,Dai, Yang,Eden, Patrick,Hanestad, Kelly,Huang, Liyue,Lin, Min-Hwa Jasmine,Tang, Jin,Ziegler, Beth,Radinsky, Robert,Kendall, Richard,Patel, Vinod F.,Payton, Marc
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p. 5189 - 5207
(2015/08/03)
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- Use of AMG 900 for the Treatment of Cancer
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The present invention relates to methods of using AMG 900, a small molecule pan aurora kinase inhibitor, for the treatment of cancer, including solid tumors, hematologically derived tumors and the like. The invention further provides pharmaceutical compositions, dosage ranges and treatment regimens for administering AMG 900 to treat cancer.
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Paragraph 0046
(2014/01/07)
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- PROTEIN KINASE MODULATORS AND METHOD OF USE
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The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.
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Page/Page column 143
(2010/02/14)
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