- Selective NK-3 receptor antagonist, preparation and application thereof
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The invention provides a selective NK-3 receptor antagonist, preparation and application thereof, particularly a compound represented by the following formula (I). The compound of the invention has unexpected activity to modulate cytokines and/or interferon, and is useful in the treatment of CNS and peripheral diseases or disorders.
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Paragraph 0074-0078
(2020/11/09)
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- An Efficient Two-Step Preparation of α-, β-, γ- or δ-Amino Acids from 2-Pyrazinones, 2-Hydroxypyrimidines or 2-Pyridones Respectively
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A practical and efficient two-step procedure is reported for the preparation of a variety of α-, β-, γ- and δ-amino acids from 2-pyridone, 2-pyrazinone or 2-hydroxypyrimidine and derivatives. The procedure is amenable to scale-up and in most cases no chromatographic purification of the product is required. This approach is useful, especially in the synthesis of amino acids or deuterated amino acids that are not obtained by other methods.
- Zacharie, Boulos,Abbott, Shaun D.,Baigent, Christopher B.,Doyle, Christopher,Yalagala, Ravi Shekar
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p. 6486 - 6493
(2018/11/23)
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- Enantioselective synthesis of α-secondary and α-tertiary piperazin-2- Ones and piperazines by catalytic asymmetric allylic alkylation
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The asymmetric palladium-catalyzed decarboxylative allylic alkylation of differentially N-protected piperazin-2- ones allows the synthesis of a variety of highly enantioenriched tertiary piperazine-2-ones. Deprotection and reduction affords the corresponding tertiary piperazines, which can be employed for the synthesis of medicinally important analogues. The introduction of these chiral tertiary piperazines resulted in imatinib analogues which exhibited comparable antiproliferative activity to that of their corresponding imatinib counterparts.
- Korch, Katerina M.,Eidamshaus, Christian,Behenna, Douglas C.,Stoltz, Brian M.,Nam, Sangkil,Horne, David
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supporting information
p. 179 - 183
(2015/02/05)
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- Phthalazine, aza- and diaza-phthalazine compounds and methods of use
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The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
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Page/Page column 51; 52
(2008/06/13)
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- Studies in Potential Filaricides: Part 20 - Synthesis of 1,4-Disubstituted Piperazines as Diethylcarbamazine Analogs
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A series of substituted 2,4-dimethylpiperazines (10-15), 1-benzyl-2-methylpiperazines (16-19), 1-substituted 3-methylpiperazines (20-25,27) and 1,4-disubstituted piperazines (28-34) have been synthesized starting from 1-benzyl-2-methylpiperazine (9) and 1
- Charles, Elisabeth S.,Sharma, Satyavan
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p. 752 - 756
(2007/10/02)
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