Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.
A series of amide derived beta(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is used to lay the SAR foundation for second generation beta(3)-AR agonists for the treatment of overactive bladder.
Goble
Stephen D
SD
Merck Research Laboratories, Rahway, NJ 07065, USA. stephen_goble@merck.com
Wang
Liping
L
Howell
K Lulu
KL
Bansal
Alka
A
Berger
Richard
R
Brockunier
Linda
L
DiSalvo
Jerry
J
Feighner
Scott
S
Harper
Bart
B
He
Jiafang
J
Hurley
Amanda
A
Hreniuk
Donna
D
Parmee
Emma
E
Robbins
Michael
M
Salituro
Gino
G
Sanfiz
Anthony
A
Streckfuss
Eric
E
Watkins
Eloisa
E
Weber
Ann E
AE
Struthers
Mary
M
Edmondson
Scott D
SD
D000081:Acetamides / Q000493:pharmacokinetics / Q000494:pharmacology*; D058667:Adrenergic beta-3 Receptor Agonists; D000319:Adrenergic beta-Antagonists / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D001549:Benzamides / Q000493:pharmacokinetics / Q000494:pharmacology*; D012377:Rodentia; D013329:Structure-Activity Relationship
D000081:Acetamides; D058667:Adrenergic beta-3 Receptor Agonists; D000319:Adrenergic beta-Antagonists; D001549:Benzamides