- Kinase inhibitors (by machine translation)
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The present invention relates to certain 4 - (substituted anilino) -2 - (substituted piperi -1 -yl) pyrimidine -5 - carboxamide compounds useful for the treatment or prevention of diseases or medical conditions mediated by signal transduction of CaMMK1 isotype. For example, such compounds and salts thereof may be used to treat or prevent a variety of different cancers. Diseases (including 2 diabetes) and/or immune-mediated diseases. (by machine translation)
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Paragraph 0492; 0494
(2020/12/31)
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- A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability
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Aurora kinase inhibitors have attracted a great deal of interest as a new class of antimitotic agents. We report a novel class of Aurora inhibitors based on a pentacyclic scaffold. A prototype pentacyclic inhibitor 32 (AKI-001) derived from two early lead
- Rawson, Thomas E.,Rüth, Matthias,Blackwood, Elizabeth,Burdick, Dan,Corson, Laura,Dotson, Jenna,Drummond, Jason,Fields, Carter,Georges, Guy J.,Goller, Bernhard,Halladay, Jason,Hunsaker, Thomas,Kleinheinz, Tracy,Krell, Hans-Willi,Li, Jun,Liang, Jun,Limberg, Anja,McNutt, Angela,Moffat, John,Phillips, Gail,Ran, Yingqing,Safina, Brian,Ultsch, Mark,Walker, Leslie,Wiesmann, Christian,Zhang, Birong,Zhou, Aihe,Zhu, Bing-Yan,Rüger, Petra,Cochran, Andrea G.
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experimental part
p. 4465 - 4475
(2009/07/11)
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- Pentacyclic kinase inhibitors
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The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.
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Page/Page column 39
(2010/11/25)
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- PYRIMIDINE KINASE INHIBITORS
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The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I) wherein ring A, X, Y, Z, R1, R2, R3, R4, m and n are as defined herein.
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Page/Page column 32-33
(2008/06/13)
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- Pyrrolobenzimidazoles for treating heart or circulatory diseases
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Pyrrolobenzimidazoles, processes for the preparation thereof and pharmaceutical compositions thereof for the treatment of coronary insufficiencies, cardiac failure, blood circulatory disturbances and occlusive diseases. The new pyrrolobenzimidazoles are of the formula STR1 wherein R1 is hydrogen, alkyl, alkenyl or cycloalkyl, R2 is hydrogen, alkyl, alkenyl, cyano or a substituted carbonyl or R1 and R2 together represent cycloalkylene or form alkylidene or cycloalkylidene, X is a valency bond, C1 -C4 alkylene or vinylene, T is oxygen or sulphur and Py is pyridyl or substituted pyridyl and including the tautomers thereof and the physiologically acceptable salts thereof.
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