Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3- methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)
The design of a new clinical candidate histamine-H3 receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by re
Semple, Graeme,Santora, Vincent J.,Smith, Jeffrey M.,Covel, Jonathan A.,Hayashi, Rena,Gallardo, Charlemagne,Ibarra, Jason B.,Schultz, Jeffrey A.,Park, Douglas M.,Estrada, Scott A.,Hofilena, Brian J.,Smith, Brian M.,Ren, Albert,Suarez, Marissa,Frazer, John,Edwards, Jeffrey E.,Hart, Ryan,Hauser, Erin K.,Lorea, Jodie,Grottick, Andrew J.
p. 71 - 75
(2012/02/16)
PHENETANOLAMINE DERIVATIVES
Compounds of formula (I) and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective β2-adrenoreceptor agonist is indicated, for example asthma or chronic o
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Page/Page column 50
(2010/02/11)
11,21-BISPHENYL-19-NORPREGNANE DERIVATIVES
The invention relates to a 11,21-bisphenyl-19-norpregnane derivative of formula I STR1 wherein R 1 is selected from H, halogen, (1-6C) alkoxy, and NR 5 R 6, R 5 and R 6 being independently hydrogen or (1-6C)alkyl or R 5 and R 6 together are (3-6C) alkylen
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(2008/06/13)
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