cas 1134-82-3, 2-BENZYL-5-METHYL-2H-PYRAZOL-3-YLAMINE

Articles about 1134-82-3Total 8 be found

Discovery, synthesis and characterization of a series of (1-alkyl-3-methyl-1H-pyrazol-5-yl)-2-(5-aryl-2H-tetrazol-2-yl)acetamides as novel GIRK1/2 potassium channel activators
The present study describes the discovery and characterization of a series of 5-aryl-2H-tetrazol-3-ylacetamides as G protein-gated inwardly-rectifying potassium (GIRK) channels activators. Working from an initial hit discovered during a high-throughput screening campaign, we identified a tetrazole scaffold that shifts away from the previously reported urea-based scaffolds while remaining effective GIRK1/2 channel activators. In addition, we evaluated the compounds in Tier 1 DMPK assays and have identified a (3-methyl-1H-pyrazol-1-yl)tetrahydrothiophene-1,1-dioxide head group that imparts interesting and unexpected microsomal stability compared to previously-reported pyrazole head groups.
Sharma, Swagat,Kozek, Krystian A.,Abney, Kristopher K.,Kumar, Sushil,Gautam, Nagsen,Alnouti, Yazen,David Weaver,Hopkins, Corey R.
p. 791 - 796
(2019/02/06)

Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators
The G protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) are a family of inward-rectifying potassium channels, and there is significant evidence supporting the roles of GIRKs in a number of physiological processes and as potential targets for numerous indications. Previously reported urea containing molecules as GIRK1/2 preferring activators have had significant pharmacokinetic (PK) liabilities. Here we report a novel series of 1H-pyrazolo-5-yl-2-phenylacetamides in an effort to improve upon the PK properties. This series of compounds display nanomolar potency as GIRK1/2 activators with improved brain distribution (rodent Kp > 0.6).
Wieting, Joshua M.,Vadukoot, Anish K.,Sharma, Swagat,Abney, Kristopher K.,Bridges, Thomas M.,Daniels, J. Scott,Morrison, Ryan D.,Wickman, Kevin,Weaver, C. David,Hopkins, Corey R.
p. 1873 - 1879
(2017/09/25)

SMALL MOLECULE INHIBITORS OF MCL-1 AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having pyrazolopyridine structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
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Paragraph 0142

(2015/10/28)

The Boulton-Katritzky rearrangement of isocarboxazid
(Chemical Equation Presented) Isocarboxazid rearranges on heating to 5-acetonyl-2-benzyl-4-hydroxy-1,2,3-triazole in DMF at 150°C, in the ionic liquid, [bmin]HSO4- at 100°C or as a melt at 105°C. This is the first reported example of the Boulton-Katritzky rearrangement of an acyl hydrazide.
Van Arnum, Susan D.,Niemczykapi, Henry J.
experimental part
p. 909 - 913
(2010/01/11)

INHIBITORS OF AKT ACTIVITY
Invented are novel substituted pyridine compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 9; 35-36

(2009/04/25)

Composition for dyeing keratin fibers which contain at least one diaminopyrazole, dyeing process, novel diaminopyrazoles and process for their preparation
The invention relates to novel compositions for the oxidation dyeing of keratin fibers, comprising at least one specific diaminopyrazole derivative, to the dyeing process using this composition, to novel diaminopyrazole derivatives and to a process for their preparation.
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Page column 19

(2008/06/13)

Rearrangement of N-(Alkylamino)azoles in Acid Media: A New Entry to C-Amino-N-substituted Azoles
A ring-opening / ring-closure mechanism for the thermal rearrangement of 1-(alkylamino)pyrazoles into 5-amino-1-alkylpyrazoles in acid medium has been established. 1-(Benzylamino)pyrazoles show a different reactivity, affording bis(5-amino-1-benzyl-4-pyrazolyl)phenylmethanes.The reaction was extended to 1-(alkylamino)indazoles but failed in the case of 1-(alkylamino)-1,2,4-triazoles.
Salazar, Loreto,Espada, Modesta,Avendano, Carmen,Claramunt, Rosa Maria,Sanz, Dionisia,Elguero, Jose
p. 1563 - 1567
(2007/10/02)

Aminopyrazoles. IV. Pyrazol-3- and 5-amines from 2,3-dihaloalkanenitriles or 3-Chloroacrylonitriles and Hydrazines
2,3-Dihalopropanenitriles and substituted 3-chloropropenenitriles react with hydrazines in basic solution to form either pyrazol-3-amines 4 or pyrazol-5-amines 5 or a mixture of both isomers.
Ege, Guenter,Franz, Hermann
p. 1267 - 1273
(2007/10/02)