Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors
摘要:
Previous efforts have led to the identification of a potent, selective, and nonphlorizin based SGLT2 inhibitor 1. This Letter describes efforts to further optimize the potency, microsomal stability, solubility and pharmacokinetic properties of this series of SGLT2 inhibitors. From these efforts, compounds 28 and 32 have improved solubility and pharmacokinetic properties compared to compound 1 (C) 2011 Elsevier Ltd. All rights reserved.
Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors
摘要:
Previous efforts have led to the identification of a potent, selective, and nonphlorizin based SGLT2 inhibitor 1. This Letter describes efforts to further optimize the potency, microsomal stability, solubility and pharmacokinetic properties of this series of SGLT2 inhibitors. From these efforts, compounds 28 and 32 have improved solubility and pharmacokinetic properties compared to compound 1 (C) 2011 Elsevier Ltd. All rights reserved.
QUINUCLIDINE DERIVATIVES BINDING TO MUCARINIC M3 RECEPTORS
申请人:Collingwood Stephen Paul
公开号:US20100041887A1
公开(公告)日:2010-02-18
Compounds of formula I
in salt or zwitterionic form wherein, wherein R
1
, R
2
, R
3
, and R
4
have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
Quinuclidine derivatives binding to mucarinic m3 receptors
申请人:Collingwood Paul Stephen
公开号:US20070060563A1
公开(公告)日:2007-03-15
Compounds of formula I
in salt or zwitterionic form wherein, wherein R
1
, R
2
, R
3
, and R
4
have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
Previous efforts have led to the identification of a potent, selective, and nonphlorizin based SGLT2 inhibitor 1. This Letter describes efforts to further optimize the potency, microsomal stability, solubility and pharmacokinetic properties of this series of SGLT2 inhibitors. From these efforts, compounds 28 and 32 have improved solubility and pharmacokinetic properties compared to compound 1 (C) 2011 Elsevier Ltd. All rights reserved.