- SUBSTITUTED BICYCLIC COMPOUNDS USEFUL AS T CELL ACTIVATORS
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Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR6 or N; Y is CR3 or N; R1, R2, R3, R4, R5, R6, R7, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGKα) and diacylglycerol kinase zeta (DGKζ), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
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Paragraph 0396; 0439; 0440
(2021/06/26)
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- SUBSTITUTED NAPHTHYRIDINONE COMPOUNDS USEFUL AS T CELL ACTIVATORS
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Disclosed are compounds of Formula (I) or a salt thereof, wherein: R1, R2, R3, R4, R5, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGKα) and diacylglycerol kinase zeta (DGKζ), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
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Page/Page column 154; 155
(2020/01/24)
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- PDE9 inhibitor and uses thereof
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The invention belongs to the technical field of medicines, particularly relates to a PDE9 inhibitor compound shown as a formula (I) or pharmaceutically acceptable salt, isomer, a deuterated compound,metabolite and prodrug thereof, and further relates to pharmaceutical preparations, pharmaceutical compositions and application of the compounds. X1, X2, X3, X4, R1, R2, ring A, L and m are defined inthe specification. The compounds can be used for preparing medicines for treating or preventing related diseases mediated by PDE9.
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Paragraph 0380; 0381; 0382; 0383
(2020/08/12)
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- PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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Page/Page column 55
(2016/07/05)
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- MACROCYCLIC KINASE INHIBITORS
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Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.
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Page/Page column 47
(2012/06/16)
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- SUBSTITUTED ARYL PYRIMIDINONE DERIVATIVES
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Substituted aryl pyrimidinone derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
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Page/Page column 42
(2009/10/22)
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- 9-Cyano-1-azapaullone (Cazpaullone), a Glycogen Synthase Kinase-3 (GSK-3) inhibitor activating pancreatic β cell protection and replication
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Recently, the serine/threonine kinase glycogen synthase kinase-3 (GSK-3) emerged as a regulator of pancreatic β cell growth and survival. On the basis of the previous observation that GSK-3 inhibitors like 1-azakenpaullone promote β cell protection and re
- Stukenbrock, Hendrik,Mussmann, Rainer,Geese, Marcus,Ferandin, Yoan,Lozach, Olivier,Lemcke, Thomas,Kegel, Simone,Lomow, Alexander,Burk, Ulrike,Dohrmann, Cord,Meijer, Laurent,Austen, Matthias,Kunick, Conrad
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p. 2196 - 2207
(2008/12/22)
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- 2-PHENOXY PYRIMIDINONE ANALOGUES
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2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment
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Page/Page column 44
(2008/06/13)
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- HALOALKYL-SUBSTITUTED PYRIMIDINONE DERIVATIVES
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Haloalkyl-substituted pyrimidinone derivatives are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful
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Page/Page column 46
(2008/06/13)
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- CIS-CYCLOHEXYL SUBSTITUTED PYRIMIDINONE DERIVATIVES
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Cis-cyclohexyl substituted pyrimidinone derivatives are provided, of Formula (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful
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Page/Page column 44
(2008/12/06)
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- Pyridine-2-carboxyamide derivatives
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The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.
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Page/Page column 31
(2008/06/13)
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- BICYCLIC PYRIMIDIN-4-(3H)-ONES AND ANALOGUES AND DERIVATIVES THEREOF WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1)
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Compounds of formula (I); which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
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Page/Page column 39
(2010/02/12)
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- 3-Hydroxy-4-oxo-3,4-dihydro-5-azabenzo-1,2,3-triazene
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The known but long-neglected compound HODhat was shown to be in certain situations a useful peptide coupling additive. Uronium and phosphonium salts with HODhat built into the system were also useful stand-alone coupling reagents. Comparisons with related additives and coupling reagents showed that the new systems were sometimes more and sometimes less effective than previously described systems in the case of stepwise and segment couplings. Applications to assembly of the model decapeptide ACP showed that HDATU was far more effective than HDTU and more effective than HATU under some conditions.
- Carpino, Louis A.,Xia, Jusong,El-Faham, Ayman
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- The ortho effect in pyridines. Part XI(1). Substituent effects on basicity of 2- and 4-substituted 3-aminopyridines
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The substituent effects on the pKa values corresponding to the first protonation site of thirty 2- and 4-substituted 3-aminopyridines have been studied.It was found that the relative localized and delocalized effects are apparently sensitive to the variation of substituent position in the pyridine ring.An interaction of the 2-substituent with the protonation centre has mainly inductive character, whereas, the pKa values of 4-substituted 3-aminopyridines are highly affected by through-resonance.The steric effect was found to be insignificant.Keywords: substituent effects / 2- and 4-substituted 3-aminopyridines / basicity
- Rasala, D.
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- HOMOLYTIC ETHOXYCARBONYLATION OF AMINOPYRIDINES
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Pyridinecarboxylic acid ethyl esters are formed in the reaction of ethoxycarbonyl radicals with aminopyridines.
- Min, R. S.,Aksenov, V. S.
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p. 885 - 886
(2007/10/02)
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