852324-85-7Relevant academic research and scientific papers
Urotensin-II receptor antagonists: Synthesis and SAR of N-cyclic azaalkyl benzamides
Jin, Jian,An, Ming,Sapienza, Anthony,Aiyar, Nambi,Naselsky, Diane,Sarau, Henry M.,Foley, James J.,Salyers, Kevin L.,Knight, Steven D.,Keenan, Richard M.,Rivero, Ralph A.,Dhanak, Dashyant,Douglas, Stephen A.
scheme or table, p. 3950 - 3954 (2009/05/07)
SAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N-cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with a Ki of 4 nM. The synthesis and structure-activity relationships (SAR) of N-cyclic azaalkyl benzamides are described.
Discovery of novel and long acting muscarinic acetylcholine receptor antagonists
Jin, Jian,Wang, Yonghui,Shi, Dongchuan,Wang, Feng,Davis, Roderick S.,Jin, Qi,Fu, Wei,Foley, James J.,Webb, Edward F.,Dehaas, Chris J.,Berlanga, Manuela,Burman, Miriam,Sarau, Henry M.,Morrow, Dwight M.,Rao, Parvathi,Kallal, Lorena A.,Moore, Michael L.,Rivero, Ralph A.,Palovich, Michael,Salmon, Michael,Belmonte, Kristen E.,Busch-Petersen, Jakob
scheme or table, p. 4866 - 4869 (2009/08/09)
High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory
NOVEL M3 MUSCARINIC ACETYCHOLINE RECEPTOR ANTAGONISTS
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Page/Page column 27, (2008/06/13)
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
MELANOCORTIN RECEPTOR AGONISTS
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Page/Page column 56, (2010/02/11)
The present invention relates a compound of formula 1, and pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.
Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists
Jin, Jian,Dhanak, Dashyant,Knight, Steven D.,Widdowson, Katherine,Aiyar, Nambi,Naselsky, Diane,Sarau, Henry M.,Foley, James J.,Schmidt, Dulcie B.,Bennett, Carl D.,Wang, Bing,Warren, Gregory L.,Moore, Michael L.,Keenan, Richard M.,Rivero, Ralph A.,Douglas, Stephen A.
, p. 3229 - 3232 (2007/10/03)
High throughput screening of the corporate compound collection led to the discovery of a novel series of substituted aminoalkoxybenzyl pyrrolidines as human urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that led to the identification of a truncated sub-series, represented by SB-436811 (1a), are described.
