cas 929000-58-8, 1-(2-Bromophenylsulfonyl)pyrrolidine | Articles data ｜lookchem

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929000-58-8

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AMINO-SUBSTITUTED HETEROCYCLIC DERIVATIVES AS SODIUM CHANNEL INHIBITORS
The present invention relates to novel aminoindazolyl derivative compounds of Formula(I), the use of said compounds in treating diseases mediated by modulation of voltage-gated sodium channels in particular Nav1.7 AND to compositions containing said derivatives.
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Page/Page column 71

(2016/11/17)

Palladium-catalysed dehydrogenative sp3 C-H bonds functionalisation into alkenes: A direct access to N-alkenylbenzenesulfonamides
The palladium-catalysed dehydrogenation of sp3 carbon-hydrogen bonds of N-alkylbenzenesulfonamides allows a simple access to N-alkenylbenzenesulfonamides. The reaction proceeds with easily accessible catalysts, with pivalate as a base, and allo
Bheeter, Charles B.,Jin, Rongwei,Bera, Jitendra K.,Dixneuf, Pierre H.,Doucet, Henri
p. 119 - 124
(2014/03/21)

Design and discovery of a selective small molecule κ opioid antagonist (2-methyl- n -((2′-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl) methyl)propan-1-amine, PF-4455242)
By use of parallel chemistry coupled with physicochemical property design, a series of selective κ opioid antagonists have been discovered. The parallel chemistry strategy utilized key monomer building blocks to rapidly expand the desired SAR space. The potency and selectivity of the in vitro κ antagonism were confirmed in the tail-flick analgesia model. This model was used to build an exposure-response relationship between the ? Ki and the free brain drug levels. This strategy identified 2-methyl-N-((2′- (pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242, which entered phase 1 clinical testing and has demonstrated target engagement in healthy volunteers.
Verhoest, Patrick R.,Sawant Basak, Aarti,Parikh, Vinod,Hayward, Matthew,Kauffman, Gregory W.,Paradis, Vanessa,McHardy, Stanton F.,McLean, Stafford,Grimwood, Sarah,Schmidt, Anne W.,Vanase-Frawley, Michelle,Freeman, Jodi,Van Deusen, Jeffrey,Cox, Loretta,Wong, Diane,Liras, Spiros
experimental part
p. 5868 - 5877
(2011/10/08)

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Chemical Properties

Boiling Point: 393.4±44.0 °C(Predicted)
Density: 1.583±0.06 g/cm3(Predicted)
Storage Temp.:2-8°C
PKA: -5.61±0.20(Predicted)
PSA: 45.76000
LogP: 3.25230

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