- Design, synthesis and biological evaluation of glycolamide, glycinamide, and β-amino carbonyl 1,2,4-triazole derivatives as DPP-4 inhibitors
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Through modification of the skeleton of Sitagliptin and Vildagliptin, we successfully synthesized and built-up four series of 1,2,4-triazole derivatives, containing N,O-disubstituted glycolamide, N,N′-disubstituted glycinamide, β-amino ester, and β-amino
- Fuh, Mao-Tsu,Tseng, Ching-Chun,Li, Sin-Min,Tsai, Shuo-En,Chuang, Tsung-Jui,Lu, Chih-Hao,Yang, Ya-Chen,Tsai, Henry J.,Wong, Fung Fuh
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supporting information
(2021/06/21)
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- NOVEL COMPOUNDS
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This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
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Paragraph 0214; 0215; 0216; 0217; 0218
(2013/06/28)
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- PIPERAZINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLU5 RECEPTORS
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This invention relates to compounds of formula (I) their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
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Page/Page column 51; 52
(2013/07/05)
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- Optimization of non-ATP competitive CDK/cyclin groove inhibitors through REPLACE-mediated fragment assembly
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A major challenge in drug discovery is to develop and improve methods for targeting protein-protein interactions. Further exemplification of the REPLACE (REplacement with Partial Ligand Alternatives through Computational Enrichment) strategy for generatin
- Liu, Shu,Premnath, Padmavathy Nandha,Bolger, Joshua K.,Perkins, Tracy L.,Kirkland, Lindsay O.,Kontopidis, George,McInnes, Campbell
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p. 1573 - 1582
(2013/04/10)
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