- Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)- pyrimidinones and evaluation of their antiviral activity
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A series of 2-amino-5-bromo-4(3 H)-pyrimidinone derivatives bearing different substituents at the C-6 position were synthesized using a highly regioselective lithiation-substitution protocol, and the effect of structural variation at the C-6 position on their antiviral activity in cell culture was evaluated. Although some of the derivatives were found to be active against various virus strains, they were effective only close to their toxicity threshold.
- Singh, Kamaljit,Singh, Kawaljit,Balzarini, Jan
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p. 428 - 433
(2013/10/01)
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- CHEMICAL COMPOUNDS
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The invention is directed to to substituted indazole derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 - R6 and X are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically leukemia and cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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Page/Page column 136-137
(2010/11/04)
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- Application of fragment-based lead generation to the discovery of novel, cyclic amidine β-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency
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Fragment-based lead generation has led to the discovery of a novel series of cyclic amidine-based inhibitors of β-secretase (BACE-1). Initial fragment hits with an isocytosine core having millimolar potency were identified via NMR affinity screening. Stru
- Edwards, Philip D.,Albert, Jeffrey S.,Sylvester, Mark,Aharony, David,Andisik, Donald,Callaghan, Owen,Campbell, James B.,Carr, Robin A.,Chessari, Gianni,Congreve, Miles,Frederickson, Martyn,Folmer, Rutger H. A.,Geschwindner, Stefan,Koether, Gerard,Kolmodin, Karin,Krumrine, Jennifer,Mauger, Russell C.,Murray, Christopher W.,Olsson, Lise-Lotte,Patel, Sahil,Spear, Nate,Tian, Gaochao
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p. 5912 - 5925
(2008/04/12)
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- NOVEL 2-AMINOPYRIMIDINONE DERIVATIVES AND THEIR USE
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This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheim
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Page/Page column 116
(2008/06/13)
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- SUBSTITUTED AMINO-PYRIMIDONES AND USES THEREOF
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This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia,Ib), and their phatmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Abeta related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
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Page/Page column 157
(2008/06/13)
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