- NEW PROCESSES FOR THE PREPARATION OF VEMURAFENIB
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The present invention relates to novel processes for the manufacture of N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide (I), wherein no protection-deprotection sequences or halogenation steps are required and the use of palladium catalysts is minimized. Formula (I)
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Page/Page column 14
(2018/02/03)
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- PREPARATION OF SUBSTITUTED-4,5-DIHYDROPYRROLO[4,3,2-de][2,6]NAPHTHYRIDIN-3(1H)-ONES
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Disclosed are materials and methods for preparing substituted 4,5-dihydropyrrolo[4,3,2-de][2,6]naphthyridin-3(1H)-ones of formula (1), Compounds of formula (1) inhibit one or more members of the Janus Kinase (JAK) family of cytoplasmic protein tyrosine kinases, and are useful for treating disorders, diseases, and conditions associated with the immune system, inflammation, and abnormal cell growth.
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- Acrosin structure-based design, synthesis and biological activities of 7-azaindol derivatives as new acrosin inhibitors
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A series of 7-azaindol derivatives were designed based on the homologous 3D model of human acrosin. These compounds were synthesized and evaluated for their human acrosin inhibitory activities in vitro. Compounds 7a, 7i, 7j, 7k and 7n showed highly inhibitory activity against human acrosin. The three-dimensional structure-activity relationship was investigated through a CoMFA model, which provided valuable information to further study of potential human acrosin inhibitors.
- Jiang, Jun Hang,Liu, Xue Fei,Zhen, Can Hui,Zhou, You Jun,Zhu, Ju,Lv, Jia Guo,Sheng, Chun Quan
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scheme or table
p. 272 - 275
(2012/01/14)
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- METHODS OF TREATING COGNITIVE IMPAIRMENT AND DEMENTIA
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This invention relates to methods for treating, managing and preventing cognitive impairment associated with various diseases and disorders, age-associated memory impairment, and dementia.
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Page/Page column 70; 71
(2008/12/06)
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- A practical synthesis of 7-azaindolylcarboxy-endo-tropanamide (DF 1012)
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An optimised cost-effective synthesis of the new antitussive drug, DF1012, is herewith reported. The new synthetic route to the key intermediate DF1005 is based on the unusual deprotection step of the 1-tert-butyl-3-cyano-7-azaindole intermediate, which can also be regarded as a convenient way for the industrial production of the expensive 7-azaindole 1. The second key intermediate, endo-tropanamine 6, was obtained in high yield by a novel one-pot stereoselective process using a Pd-catalysed reductive amination procedure.
- Allegretti, Marcello,Anacardio, Roberto,Cesta, M. Candida,Curti, Roberto,Mantovanini, Marco,Nano, Giuseppe,Topai, Alessandra,Zampella, Giuseppe
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p. 209 - 213
(2013/09/05)
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