- PIKFYVE KINASE INHIBITORS
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The present invention relates to compounds useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.
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Page/Page column 178
(2021/08/20)
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- Development of an efficient, scalable route for the preparation of a novel insulin-like growth factor-1 receptor modulator
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A chromatography-free and efficient synthesis of insulin-like growth factor-1 receptor (IGF-1R) modulator is reported. Herein we describe an improved synthesis for the target compound, which features facile introduction of a novel pyrrolidinyl-pyrimidyl isoxazole 8, via in situ sulfone displacement by fluorine. The overall process consists of six chemical steps and five isolations, with introduction of the expensive triheterocyclic unit 8 towards the end of the synthesis.
- Kumar, C.H. Vinod,Kavitake, Santosh,Kumar, Sythana Suresh,Cornwall, Philip,Ashok, Mithun,Bhagat, Sagar,Manjunatha, Sulur G.,Nambiar, Sudhir
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p. 1416 - 1421
(2012/10/29)
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- Novel Compounds
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The present invention relates to the new compounds of general formula I wherein A, U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers thereof, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.
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Page/Page column 67
(2012/04/18)
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- Aminopyrimidinone Cdc7 Kinase Inhibitors
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We have investigated the SAR of a series of pyrimidinone-containing Cdc7 kinase inhibitors. A wide range of amine substitutions give potent compounds with activities (Ki) less than 1 nM. Kinase selectivity is reasonable and cytotoxicity corresponds to inhibition of MCM2 phosphorylation.
- Woods, Keith W.,Lai, Chunqiu,Miyashiro, Julie M.,Tong, Yunsong,Florjancic, Alan S.,Han, Edward K.,Soni, Niru,Shi, Yan,Lasko, Loren,Leverson, Joel D.,Johnson, Eric F.,Shoemaker, Alexander R.,Penning, Thomas D.
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supporting information; scheme or table
p. 1940 - 1943
(2012/04/17)
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- ANTIPROLIFERATIVE PYRIMIDYL, FUSED PYRIMIDYL AND PYRIMIDYL HYDRAZONES
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The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.
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Page/Page column 49-50
(2010/11/27)
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