13626-59-0Relevant articles and documents
Structure-activity studies of 6-substituted decahydroisoquinoline-3- carboxylic acid AMPA receptor antagonists. 2. Effects of distal acid bioisosteric substitution, absolute stereochemical preferences, and in vivo activity
Ornstein,Arnold,Allen,Bleisch,Borromeo,Lugar,Leander,Lodge,Schoepp
, p. 2232 - 2244 (1996)
We have explored the excitatory amino acid antagonist activity in a series of decahydroisoquinoline-3-carboxyic acids, and within this series found the potent and selective AMPA antagonist (3SR,4aRS,6RS,8aRS)-6-(2-(1H-tetrazol- 5-yl)ethyl)decahydroisoquin
NEW BIARYL AMIDE DERIVATIVES
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Page/Page column 24, (2012/07/13)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
NEW BIARYL AMIDE DERIVATIVES
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Page/Page column 58-59, (2012/07/14)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
New 2-heterocyclyl-imidazo[2,1- i ]purin-5-one derivatives as potent and selective human A3 adenosine receptor antagonists
Baraldi, Pier Giovanni,Preti, Delia,Zaid, Abdel Naser,Saponaro, Giulia,Tabrizi, Mojgan Aghazadeh,Baraldi, Stefania,Romagnoli, Romeo,Moorman, Allan R.,Varani, Katia,Cosconati, Sandro,Di Maro, Salvatore,Marinelli, Luciana,Novellino, Ettore,Borea, Pier Andrea
body text, p. 5205 - 5220 (2011/10/08)
A series of 4-allyl/benzyl-7,8-dihydro-8-methyl/ethyl-2-[(substituted) isoxazol/pyrazol-3/5-yl]-1H-imidazo[2,1-i]purin-5(4H)-ones has been synthesized and evaluated in radioligand binding assays to determine their affinities at the human A1, A
Practical synthesis of a potent bradykinin B1 antagonist via enantioselective hydrogenation of a pyridyl N-acyl enamide
O'Shea, Paul D.,Gauvreau, Danny,Gosselin, Francis,Hughes, Greg,Nadeau, Christian,Roy, Amelie,Shultz, C. Scott
supporting information; experimental part, p. 4547 - 4553 (2009/09/30)
(Chemical Equation Presented) A practical and efficient synthesis of bradykinin B1 antagonist 1 is described. A convergent strategy was utilized which involved synthesis of three fragments: 3, 6, and 7. Cross coupling of fragments 6 and 7 followed by amidation with 3 enabled efficient synthesis of 1 in 19 steps total, a 35% overall yield from commercially available pyridine 10. The key to the success of the synthesis was the development of a fluorodenitration step to install the fluorine in pyridine 7 and a catalytic enantioselective hydrogenation of N-acyl enamide 9 to set the stereochemistry.
HETEROCYCLIC COMPOUND HAVING TYPE I 11 BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORY ACTIVITY
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Page/Page column 21, (2010/11/30)
Disclosed is a compound useful as a type I 11 β hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally su