- Dihydropyrimidine Compounds and Their Uses in Preparation of Medicaments for Treating and Preventing Antiviral Diseases
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The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, to a process for preparing the compound of formula (I), and to use of the compound of formula (I) or a pharmaceutically acceptable salt or
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Page/Page column 22
(2010/04/30)
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- DIHYDROPYRIMIDINE COMPOUNDS AND THEIR USES IN PREPARATION OF MEDICAMENTS FOR TREATING AND PREVENTING ANTIVIRAL DISEASES
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The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, to a process for preparing the compound of formula (I), and to use of the compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof as a medicament, in particular as a medicament for the treatment and prevention of type B hepatitis.
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Page/Page column 32-33
(2009/04/23)
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- TRICYCLIC 2,4-DIAMIN0-L,3,5-TRIAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF CANCER AND MYELOPROLIFERATIVE DISORDERS
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The present invention relates to compounds of Formula (I): (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.
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Page/Page column 78
(2010/01/07)
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- Potent N-(1,3-Thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel
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A series of N-(1,3-thiazol-2-yl)pyridin-2-amine KDR kinase inhibitors have been developed that possess optimal properties. Compounds have been discovered that exhibit excellent in vivo potency. The particular challenges of overcoming hERG binding activity and QTc increases in vivo in addition to achieving good pharmacokinetics have been acomplished by discovering a unique class of amine substituents. These compounds have a favorable kinase selectivity profile that can be accentuated with appropriate substitution.
- Bilodeau, Mark T.,Balitza, Adrienne E.,Koester, Timothy J.,Manley, Peter J.,Rodman, Leonard D.,Buser-Doepner, Carolyn,Coll, Kathleen E.,Fernandes, Christine,Gibbs, Jackson B.,Heimbrook, David C.,Huckle, William R.,Kohl, Nancy,Lynch, Joseph J.,Mao, Xianzhi,McFall, Rosemary C.,McLoughlin, Debra,Miller-Stein, Cynthia M.,Rickert, Keith W.,Sepp-Lorenzino, Laura,Shipman, Jennifer M.,Subramanian, Raju,Thomas, Kenneth A.,Wong, Bradley K.,Yu, Sean,Hartman, George D.
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p. 6363 - 6372
(2007/10/03)
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- Active salt forms with tyrosine kinase activity
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The present invention relates to orally active salt forms of the mesylate salt of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, retinal ischemia, macular edema, inflammatory diseases, and the like in mammals.
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Page/Page column 13
(2010/02/05)
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- Polymorphs with tyrosine kinase activity
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The present invention relates to active polymorphs of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, retinal ischemia, macular edema, inflammatory diseases, and the like in mammals.
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Page/Page column 13
(2010/02/05)
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- Salt forms with tyrosine kinase activity
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The present invention relates to salt forms of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, retinal ischemia, macular edema, inflammatory diseases, and the like in mammals.
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Page/Page column 14;15
(2010/02/05)
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- Process for making substituted thiazolyl-amino pyrimidinyl
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The present invention relates to a process for preparing substituted thiazolyl-amino pyrimidinyl piperazines, which are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases.
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Page/Page column 7
(2010/11/30)
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- Tyrosine kinase inhibitors
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The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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- Tyrosine kinase inhibitors
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The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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- Tyrosine kinase inhibitors
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The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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