36210-76-1Relevant academic research and scientific papers
Catalytic Enantioselective Addition of Pyrazol-5-ones to Trisubstituted Nitroalkenes with an N-Sulfinylurea Organocatalyst
Phelan, James P.,Ellman, Jonathan A.
, p. 1713 - 1718 (2016)
The first example of enantioselective nitronate protonation following Michael addition of a carbon nucleophile to an α,β,β-trisubstituted nitroalkene is reported. An N-sulfinylurea catalyst was employed to catalyze the addition of a variety of 3-substitut
THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY
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Page/Page column 39, (2008/06/13)
To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R 1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R 2 is methyl; R 3 is a hydrogen atom; and R 4 is a group: -CONR 5 R 6 (in which any one of R 5 and R 6 is a hydrogen atom)].
New series of antiprion compounds: Pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation
Kimata, Ayako,Nakagawa, Hidehiko,Ohyama, Ryo,Fukuuchi, Tomoko,Ohta, Shigeru,Suzuki, Takayoshi,Miyata, Naoki
, p. 5053 - 5056 (2008/03/13)
To find effective antiprion compounds, we synthesized and evaluated various pyrazolone derivatives. Seven of 19 compounds showed inhibition of PrP-res accumulation and the remarkably active compound 13 showed an IC50 value of 3 nM in both ScN2a and F3 cell lines. Findings from studies on physicochemical and biochemical properties suggest that the action mechanism of these compounds does not correlate with any antioxidant activities, any of hydroxyl radical scavenging activities, or any SOD-like activities.
Hydroxyl radical scavenging by edaravone derivatives: Efficient scavenging by 3-methyl-1-(pyridin-2-yl)-5-pyrazolone with an intramolecular base
Nakagawa, Hidehiko,Ohyama, Ryo,Kimata, Ayako,Suzuki, Takayoshi,Miyata, Naoki
, p. 5939 - 5942 (2007/10/03)
We synthesized various 3-methyl-1-phenyl-5-pyrazolone (edaravone) derivatives and evaluated their oxidation potential and hydroxyl radical scavenging activity. It was found 3-methyl-1-(pyridin-2-yl)-5-pyrazolone had a much higher ability to scavenge the radical than did edaravone itself. Its efficient radical scavenging activity was assumed to be due to the increase of its anion form, an active form, by a hydrogen-bonded intramolecular base.
PYRIDINYLPYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE 7 INHIBITORS
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Page 24, (2008/06/13)
To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyridinylpyrazolopyrimidinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl or cycloheptyl group, R2 is methyl; R3 is a group: -NR5R6 or -S(O)0-2R8; hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; and R4 is methoxy or ethoxy group.
PYRAZOLOPYRIMIDINONE DERIVATIVES HAVING PDE7?INHIBITORY ACTIVITY
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Page 18; 19, (2010/02/08)
Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): and the following general formula (IA') or (IB'): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds have the action of selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, they are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.
THROMBOPOIETIN MIMETICS
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Page 30, (2010/02/04)
Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof
