- Visible Light-Promoted Photocatalytic C-5 Carboxylation of 8-Aminoquinoline Amides and Sulfonamides via a Single Electron Transfer Pathway
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An efficient photocatalytic method was developed for the remote C5-H bond carboxylation of 8-aminoquinoline amide and sulfonamide derivatives. This methodology uses in situ generated ?CBr3 radical as a carboxylation agent with alcohol and is further extended to a variety of arenes and heteroarenes to synthesize the desired carboxylated product in moderate-to-good yields. The reaction proceeding through a single electron transfer pathway was established by a control experiment, and a butylated hydroxytoluene-trapped aryl radical cation intermediate in high-resolution mass spectrometry was identified.
- Sen, Chiranjit,Sahoo, Tapan,Singh, Harshvardhan,Suresh, Eringathodi,Ghosh, Subhash Chandra
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p. 9869 - 9896
(2019/08/20)
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- THERAPEUTIC COMPOUNDS AND COMPOSITIONS
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Compounds of general formula (I) and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
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Page/Page column 180
(2014/09/29)
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- THERAPEUTIC COMPOUNDS AND COMPOSITIONS
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Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
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Paragraph 0743; 0744
(2014/09/30)
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- THERAPEUTIC COMPOUNDS AND COMPOSITIONS
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Compounds of general formula (I) and compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
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Page/Page column 193; 194
(2014/09/29)
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- Novel Sulfonaminoquinoline Hepcidin Antagonists
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The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
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Page/Page column 128
(2012/09/05)
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- 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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The present invention relates to 1,4 Oxazines of formula (I): having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the pre
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Page/Page column 73
(2012/08/07)
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- 1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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The present invention relates to 1,4 Oxazines of formula I having BACE 1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the prese
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Page/Page column 39
(2012/07/28)
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- TRIPLE SUBSTITUTED PHENANTHROLINE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE OR HAEMATOLOGICAL DISEASES OR CONDITIONS, OR CANCER
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The present invention relates to a new family of triple substituted phenantroline derivatives of formula (I), which are useful for the treatment or profilaxis of a neurodegenerative or haematological disease or condition or cancer, their use as a medicament, especially for treating a neurodegenerative or haematological disease or condition or cancer, and a pharmaceutical composition comprising the compounds.
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Page/Page column 18-19
(2010/06/22)
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- Preparation of 6-fluoro-8-quinolinol and related 6-fluoroquinolines
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6-Fluoro-8-quinolinol was prepared from 2-amino-5-fluorophenol by a Skraup synthesis. No synergism was observed between 5-fluoro- and 6-fluoro-8-quinolinols or between 6-fluoro- and 7-fluoro-8-quinolinols against any of the six fungi in our test system (Aspergillus niger, A. oryzae, Myrothecium verrucaria, Trichoderma viride, Mucor cirinelloides, and Trichophyton mentagrophytes) in Sabouraud dextrose broth. Unlike the fluoro-8-quinolinols, the 8-quinolinols comparably substituted with chlorine or bromine did form synergistic mixtures. This is attributed to steric factors.
- Gershon, Herman,Clarke, Donald D.,Gershon, Muriel
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p. 1437 - 1442
(2007/10/03)
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- PHARMACEUTICAL COMPOUNDS
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A pharmaceutical compound of the formula in which R1 is hydrogen, C1-4 alkyl, C1-4 alkoxy or halo, and R2 is hydrogen, C1-4 alkyl or C1-4 alkoxy; or a salt thereof.
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