Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Diane E. Grotz"'
Autor:
Gopal Krishna, Elpida Sapidou, Chin-Chung Lin, Inhou Chu, Cliff Chen, Laura Norton, A. D. Soares, Yau Yi Lau, Yumibe Nathan P, Diane E. Grotz
Publikováno v:
Pharmaceutical Research. 19:1606-1610
Purpose. The in vivo hepatic extraction ratio of cynomolgus monkeys was correlated with the corresponding in vitro extraction ratios that were determined in monkey microsomal incubations.
Autor:
Dennis V. Nazareno, Guowei Zhou, Herbert Binch, William J. Greenlee, Mary Cohen-Williams, Jayaram R. Tagat, Diane E. Grotz, Jean E. Lachowicz, James J. Kaminski, Joseph A. Kozlowski, Gordon Crosby, Stuart W. McCombie, Vicki L. Coffin, Kathleen Cox, Vilma Ruperto, Craig D. Boyle, Samuel Chackalamannil, Ruth A. Duffy, Hubert B. Josien, Yuguang Wang, John W. Clader, William Billard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2311-2314
The potential toxicological liabilities of the M(2) muscarinic antagonist 1 were addressed by replacing the methylenedioxyphenyl moiety with a p-methoxyphenyl group, resulting in M(2) selective compounds such as 3. Several halogenated naphthamide der
Autor:
Diane E. Grotz, Kimberly Dunn-Meynell, Eva Duchoslav, Kathleen Cox, Chin-Chung Lin, Chris Elicone, Charles C. Liu, Cynthia A. Palmer, Cymbelene Nardo, Walter A. Korfmacher
Publikováno v:
Rapid Communications in Mass Spectrometry. 13:901-907
There is a continuing need for increased throughput in the evaluation of new drug entities in terms of their pharmacokinetic parameters. One useful parameter that can be measured in vitro using liver microsomal preparations is metabolic stability. In
Autor:
Yan Yi, Lau, Gopal, Krishna, Nathan P, Yumibe, Diane E, Grotz, Elpida, Sapidou, Laura, Norton, Inhou, Chu, Cliff, Chen, A D, Soares, Chin-Chung, Lin
Publikováno v:
Pharmaceutical research. 19(11)
The in vivo hepatic extraction ratio of cynomolgus monkeys was correlated with the corresponding in vitro extraction ratios that were determined in monkey microsomal incubations.For compounds that are eliminated mainly through liver phase I metabolis
Autor:
Samuel Chackalamannil, Ruth A. Duffy, Yuguang Wang, Herbert Binch, Zhiyong Hu, William Billard, Mary Cohen-Williams, Kathleen Cox, William J. Greenlee, Diane E. Grotz, Vilma Ruperto, Gordon Crosby, Craig D. Boyle, Vicki L. Coffin, John W. Clader, James J. Kaminski, Jean E. Lachowicz
Publikováno v:
Journal of medicinal chemistry. 45(25)
In search of a backup M(2) muscarinic receptor antagonist to the previously reported compound 1, we discovered compound (+)-14, which showed superior oral efficacy in animal models. The improvement of oral efficacy was achieved by modulating both the
Autor:
Kathleen Cox, Vilma Ruperto, Stuart W. McCombie, Claire M. Lankin, Gordon Crosby, Vice Susan F, Vicki L. Coffin, Diane E. Grotz, Mary-Cohen Williams, Craig D. Boyle, Jean E. Lachowicz, Herbert Binch, Samuel Chackalamannil, Ruth A. Duffy, Jennifer Campion, William Billard
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(23)
We previously reported the initial discovery of a novel class of stabilized benzylidene ketal M 2 receptor antagonists. This paper discusses new analogues consisting of benzamide modifications which not only improved M 2 receptor affinity and selecti