- PYRAZOLE DERIVATIVES AS MALT1 INHIBITORS
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Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT 1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, and G, are defined herein.
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Paragraph 1082-1084
(2020/01/04)
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- Extending the scope of the aza-Fischer synthesis of 4- and 6-azaindoles
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Fischer indole cyclization has recently been described as an efficient approach to the synthesis of azaindoles bearing electron-donating groups. We now show that this cascade reaction can be very efficient for the formation of a wider range of 4- and 6-azaindoles by using microwave irradiation. Fischer indole cyclization starting from aminopyridines is a very efficient cascade sequence leading to 4- and 6-azaindoles. The scope of the substituents on the pyridine ring was extended to include halogens and to weakly electron-donating substituents by using microwave irradiation. Copyright
- Thomae, David,Jeanty, Matthieu,Coste, Jerome,Guillaumet, Gerald,Suzenet, Franck
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p. 3328 - 3336
(2013/07/05)
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- Substituted pyrazoles as novel sEH antagonist: Investigation of key binding interactions within the catalytic domain
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A novel series of pyrazole sEH inhibitors is reported. Lead optimization efforts to replace the aniline core are also described. In particular, 2-pyridine, 3-pyridine and pyridazine analogs are potent sEH inhibitors with favorable CYP3A4 inhibitory and microsomal stability profiles.
- Lo, Ho Yin,Man, Chuk C.,Fleck, Roman W.,Farrow, Neil A.,Ingraham, Richard H.,Kukulka, Alison,Proudfoot, John R.,Betageri, Raj,Kirrane, Tom,Patel, Usha,Sharma, Rajiv,Hoermann, Mary Ann,Kabcenell, Alisa,Lombaert, Stéphane De
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scheme or table
p. 6379 - 6383
(2010/12/19)
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- 1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS FOR THE TEATMENT OF CNS DISORDERS
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The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterised by general Formula (I): with R1 being phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X in
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Page/Page column 58
(2009/07/03)
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- STEROIDAL [3, 2-C] PYRAZOLE COMPOUNDS, WITH GLUCOCORTICOID ACTIVITY
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The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 80-81
(2009/05/29)
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- SUBSTITUTED PYRAZOLE COMPOUNDS USEFUL AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
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Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.
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Page/Page column 82
(2008/06/13)
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