Lanqi Jia
Boehringer Ingelheim
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Publication
Featured researches published by Lanqi Jia.
ACS Medicinal Chemistry Letters | 2011
Lanqi Jia; Robert D. Simpson; Jing Yuan; Zhenrong Xu; Wei Zhao; Salvacion Cacatian; Colin M. Tice; Joan Guo; Alexey V. Ishchenko; Suresh B. Singh; Zhongren Wu; Brian M. McKeever; Yuri Bukhtiyarov; Judith A. Johnson; Christopher P. Doe; Richard K. Harrison; Gerard M. McGeehan; Lawrence W. Dillard; John J. Baldwin; David A. Claremon
Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the cyclohexylmethyl group occupying the S1 pocket with a (R)-(tetrahydropyran-3-yl)methyl group and utilization of a different attachment point led to the identification of clinical candidate 9. This compound demonstrated excellent selectivity over related and unrelated off-targets, >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans.
Bioorganic & Medicinal Chemistry Letters | 2010
Zhenrong Xu; Salvacion Cacatian; Jing Yuan; Robert D. Simpson; Lanqi Jia; Wei Zhao; Colin M. Tice; Patrick T. Flaherty; Joan Guo; Alexey V. Ishchenko; Suresh B. Singh; Zhongren Wu; Brian M. McKeever; Boyd B. Scott; Yuri Bukhtiyarov; Jennifer Berbaum; Jennifer M. Mason; Reshma Panemangalore; Maria Grazia Cappiello; Ross Bentley; Christopher P. Doe; Richard K. Harrison; Gerard M. McGeehan; Lawrence W. Dillard; John J. Baldwin; David A. Claremon
Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC(50) of 0.83nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10mg/kg resulted in >20h reduction of blood pressure in a double transgenic rat model of hypertension.
Bioorganic & Medicinal Chemistry Letters | 2011
Jing Yuan; Robert D. Simpson; Wei Zhao; Colin M. Tice; Zhenrong Xu; Salvacion Cacatian; Lanqi Jia; Patrick T. Flaherty; Joan Guo; Alexey V. Ishchenko; Zhongren Wu; Brian M. McKeever; Boyd B. Scott; Yuri Bukhtiyarov; Jennifer Berbaum; Reshma Panemangalore; Ross Bentley; Christopher P. Doe; Richard K. Harrison; Gerard M. McGeehan; Suresh B. Singh; Lawrence W. Dillard; John J. Baldwin; David A. Claremon
Structure-based design led to the discovery of a novel class of renin inhibitors in which an unprecedented phenyl ring filling the S1 site is attached to the phenyl ring filling the S3 pocket. Optimization for several parameters including potency in the presence of human plasma, selectivity against CYP3A4 inhibition and improved rat oral bioavailability led to the identification of 8d which demonstrated antihypertensive efficacy in a transgenic rat model of human hypertension.
Archive | 2013
Lawrence W. Dillard; Jing Yuan; Katerina Leftheris; Shankar Venkatraman; Guosheng Wu; Lanqi Jia; Zhenrong Xu; Salvacion Cacatian; Angel Morales-Ramos; Suresh B. Singh; Yajun Zheng
Archive | 2014
David A. Claremon; Lawrence W. Dillard; Chengguo Dong; Yi Fan; Lanqi Jia; Stephen D. Lotesta; Andrew P. Marcus; Suresh B. Singh; Colin M. Tice; Jing Yuan; Wei Zhao; Yajun Zheng; Linghang Zhuang
Archive | 2015
Salvacion Cacatian; David A. Claremon; Lanqi Jia; Angel Morales-Ramos; Suresh B. Singh; Shankar Venkatraman; Zhenrong Xu; Yajun Zheng
Archive | 2009
David A. Claremon; Robert D. Simpson; Lanqi Jia
Archive | 2017
David A. Claremon; Lawrence W. Dillard; Yi Fan; Lanqi Jia; Suresh B. Singh; Colin M. Tice; Zhenrong Xu; Jing Yuan; Linghang Zhuang
Archive | 2016
David A. Claremon; Lawrence W. Dillard; Chengguo Dong; Yi Fan; Lanqi Jia; Stephen D. Lotesta; Andrew P. Marcus; Suresh B. Singh; Colin M. Tice; Jing Yuan; Wei Zhao; Yajun Zheng; Linghang Zhuang
Archive | 2013
Yuri Bukhtiyarov; Salvacion Cacatian; Lawrence Wayne Dillard; Cornelia Dorner-Ciossek; Klaus Fuchs; Lanqi Jia; Deepak S. Lala; Angel Morales-Ramos; Jonathan T. Reeves; Suresh B. Singh; Shankar Venkatraman; Zhenrong Xu; Jing Yuan; Yi Zhao; Yajun Zheng; Georg Rast