503610-15-9Relevant academic research and scientific papers
Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists
Ladouceur, Gaetan H.,Cook, James H.,Hertzog, Donald L.,Jones,Hundertmark, Thomas,Korpusik, Mary,Lease, Timothy G.,Livingston, James N.,MacDougall, Margit L.,Osterhout, Martin H.,Phelan, Kathleen,Romero, Romulo H.,Schoen, William R.,Shao, Chunning,Smith, Roger A.
, p. 3421 - 3424 (2007/10/03)
Optimized substituent patterns in 4-aryl-pyridine glucagon receptor antagonists were merged to produce highly potent derivatives containing both a 3-[(1R)-hydroxyethyl] and a 2′-hydroxy group. Due to restricted rotation of the phenyl-pyridine bond, these analogues exist as four isomers. A diastereoselective methylcopper reaction was developed to facilitate the synthesis, and single isomers were isolated with activities in the range IC50=10-25 nM.
Substituted biphenyls
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, (2008/06/13)
Substituted biphenyls having glucagon receptor antagonistic activity. Claimed compounds have the formula wherein R1aand R1bindependently represent (C1-C6) alkyl; R2represents (C1-C10) alkyl or substituted (C1-C10) alkyl wherein the substituents are independently from 1 to 3 of —SR7; R7represents phenyl, or substituted phenyl wherein the substituents are independently 1-5 of halogen, trifluoromethyl, (C1-C6) alkyl, (C1-C6) alkoxy, nitro, cyano, or hydroxyl; R3represents substituted (C1-C6) alkyl wherein the substituents are 1-2 hydroxyl groups; G represents a substituent selected from the group consisting of halogen, (C1-C6) alkyl, and OR4wherein R4is H or (C1-C6) alkyl; and y is 0 or an integer of 1-3. Pharmaceutical compositions containing such compounds and methods of treatment of glucagon-mediated conditions by administering such compounds are also claimed.
