- Tumor inhibitor MLN4924 synthetic method (by machine translation)
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The invention discloses tumor inhibitor MLN4924 synthetic method, which belongs to the field of chemical synthesis, the method to compound A and compound E as the starting material, by mitsunobu reaction, amination reaction, deprotected base and sulphur esterification four-step reaction can synthesize the target product MLN4924, has the advantage of short synthetic route, and the raw material source is wide, low cost, mild reaction conditions, the operation is safe, friendly to the environment, high yield, can be up to 40% more than, is suitable for industrial large-scale production. (by machine translation)
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Paragraph 0039; 0042
(2017/07/22)
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- Process Development and GMP Production of a Potent NAE Inhibitor Pevonedistat
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A practical synthesis of a novel NEDD8-activating enzyme (NAE) inhibitor pevonedistat (MLN4924) is described. Key steps include an enantioselective synthesis of an amino-diol cyclopentane intermediate containing three chiral centers and a novel, regiosele
- Armitage, Ian,Elliott, Eric L.,Hicks, Frederick,Langston, Marianne,McCarron, Ashley,McCubbin, Quentin J.,Obrien, Erin,Stirling, Matt,Zhu, Lei
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p. 1299 - 1307
(2015/09/28)
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- HYDROCHLORIDE SALT OF ((1S,2S,4R)-4-{4-[(1S)-2,3-DIHYDRO-1H-INDEN-1-YLAMINO]-7H-PYRROLO [2,3-D]PYRIMIDIN-7-YL}-2-HYDROXYCYCLOPENTYL)METHYL SULFAMATE
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Disclosed is a compound of formula (I); crystalline forms thereof, and solvates thereof; pharmaceutical compositions comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and a pharmaceutically acceptable carrier or diluent; and the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting an El activating enzyme, particularly NAE, including, e.g., cancer.
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Page/Page column 36
(2010/12/17)
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- Inhibitors of E1 activating enzymes
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This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
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Page/Page column 52
(2010/11/28)
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- INHIBITORS OF E1 ACTIVATING ENZYMES
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This invention relates to compounds that inhibit El activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
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Page/Page column 138
(2008/06/13)
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