1476028-20-2Relevant articles and documents
Dihydropyrimidine compounds and their use in medicine (by machine translation)
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Paragraph 0353; 0355; 0357; 0358, (2018/03/25)
The invention relates to a dihydropyrimidine compounds and their use as medicaments, in particular for the treatment and prevention of hepatitis b use of the medicament. In particular, the invention relates to the general formula (I) or (Ia) compound of formula or its enantiomer, non-enantiomeric isomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt, wherein the variables are defined in the specification. The invention also relates to the general formula (I) or (Ia) compound of formula or its enantiomer, non-enantiomeric isomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt as the pharmaceutical use, especially for the treatment and prevention of hepatitis b use of the medicament. (by machine translation)
Synthesis of 3-oxadiazolyl/triazolyl morpholines: Novel scaffolds for drug discovery
Tereshchenko, Alexander D.,Myronchuk, Julia S.,Leitchenko, Lena D.,Knysh, Irina V.,Tokmakova, Ganna O.,Litsis, Olena O.,Tolmachev, Andrey,Liubchak, Konstantin,Mykhailiuk, Pavel
, p. 750 - 757 (2017/01/16)
Synthesis of isomeric 3-oxadiazolyl/triazolyl morpholines was performed based on a common intermediate on the gram scale. The target compounds were designed as novel scaffolds for the medicinal chemistry. The key reaction was an electrochemical CH-oxidati
CHEMICAL COMPOUNDS
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Page/Page column 144-145, (2010/11/04)
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.
CHEMICAL COMPOUNDS
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Page/Page column 214, (2010/07/10)
The invention is directed to 6-(4-pyι?midinyl)-1 H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1 - R4 are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically 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.
BETA CARBOLINES AND USES THEREOF
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Page/Page column 46-47, (2009/06/27)
This invention provides beta-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, G, and x are as described in the specification. The compounds are useful for treating cancer and inflammatory disorders.
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors
Pace, Paola,Di Francesco, M. Emilia,Gardelli, Cristina,Harper, Steven,Muraglia, Ester,Nizi, Emanuela,Orvieto, Federica,Petrocchi, Alessia,Poma, Marco,Rowley, Michael,Scarpelli, Rita,Laufer, Ralph,Paz, Odalys Gonzalez,Monteagudo, Edith,Bonelli, Fabio,Hazuda, Daria,Stillmock, Kara A.,Summa, Vincenzo
, p. 2225 - 2239 (2007/10/03)
Human immunodeficiency virus type-1 (HIV-1) integrase, one of the three constitutive viral enzymes required for replication, is a rational target for chemotherapeutic intervention in the treatment of AIDS that has also recently been confirmed in the clinical setting. We report here on the design and synthesis of N-benzyl-5,6-dihydroxypyrimidine-4-carboxamides as a class of agents which exhibits potent inhibition of the HIV-integrase-catalyzed strand transfer process. In the current study, structural modifications on these molecules were made in order to examine effects on HIV-integrase inhibitory potencies. One of the most interesting compounds for this series is 2-[1-(dimethylamino)-1-methylethyl]-N-(4-fluorobenzyl)-5,6-dihydroxypyrimidine- 4-carboxamide 38, with a CIC95 of 78 nM in the cell-based assay in the presence of serum proteins. The compound has favorable pharmacokinetic properties in preclinical species (rats, dogs, and monkeys) and shows no liabilities in several counterscreening assays, highlighting its potential as a clinically useful antiviral agent.
4,5-Dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species
Summa, Vincenzo,Petrocchi, Alessia,Matassa, Victor G.,Gardelli, Cristina,Muraglia, Ester,Rowley, Michael,Paz, Odalys Gonzalez,Laufer, Ralph,Monteagudo, Edith,Pace, Paola
, p. 6646 - 6649 (2007/10/03)
The dihydroxypyrimidine carboxamide 4a was discovered as a potent and selective HIV integrase strand transfer inhibitor. The optimization of physicochemical properties, pharmacokinetic profiles, and potency led to the identification of 13 in the dihydroxypyrimidine series and 18 in the N-methylpyrimidinone series having low nanomolar activity in the cellular HIV spread assay in the presence of 50% normal human serum and very good pharmacokinetics in preclinical species.
POLYHETEROCYCLIC COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS
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Page/Page column 43, (2010/02/13)
The present invention relates to new compounds of formula (I), wherein P, Q, X1, X2, X3, X4, X5, X6, R1, R2, R3, m, n, and p are as defined as in formula (I), or salts, or hydrates thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.