771572-85-1Relevant articles and documents
2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists
Ryu, Hyungchul,Seo, Sejin,Cho, Seong-Hee,Kim, Ho Shin,Jung, Aeran,Kang, Dong Wook,Son, Karam,Cui, Minghua,Hong, Sun-Hye,Sharma, Pankaz Kumar,Choi, Sun,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Stockhausen, Hannelore,Schiene, Klaus,Christoph, Thomas,Frormann, Sven,Lee, Jeewoo
, p. 4039 - 4043 (2014/09/16)
A series of 2-alkyl/alkenyl pyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed excellent and stereospecific TRPV1 antagonism with better potency than previous lead 2. Among them, compound 15f demonstrated a strong analgesic profile in a rat neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner. Docking analysis of (S)-15f with our hTRPV1 homology model provided insight into its specific binding mode.
2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4- methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists
Ryu, Hyungchul,Seo, Sejin,Kim, Myeong Seop,Kim, Mi-Yeon,Kim, Ho Shin,Ann, Jihyae,Tran, Phuong-Thao,Hoang, Van-Hai,Byun, Jieun,Cui, Minghua,Son, Karam,Sharma, Pankaz Kumar,Choi, Sun,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Koegel, Babette-Yvonne,Christoph, Thomas,Frormann, Sven,Lee, Jeewoo
, p. 4044 - 4047 (2014/09/03)
A series of 2-aryl pyridine C-region derivatives of 2-(3-fluoro-4- methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed highly potent TRPV1 antagonism toward capsaicin comparable to previous lead 7. Among them, compound 9 demonstrated anti-allodynia in a mouse neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner. Docking analysis of 9 with our hTRPV1 homology model provided insight into its specific binding mode.
Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
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Paragraph 0265; 0269, (2013/04/10)
The invention relates to substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseas
SUBSTITUTED METHANESULFONAMIDE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 40, (2013/04/13)
The invention relates to substituted methanesulfonamide derivatives as vanilloid receptor ligands of formula (I), to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and