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Dive into the research topics where Lanqi Jia is active.

Publication


Featured researches published by Lanqi Jia.


ACS Medicinal Chemistry Letters | 2011

Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.

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

Optimization of orally bioavailable alkyl amine renin inhibitors.

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

Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket

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

Inhibitors of beta-secretase

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

THIAZOLOPYRROLIDINE INHIBITORS OF ROR-GAMMA

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

Purine derivatives as cd73 inhibitors for the treatment of cancer

Salvacion Cacatian; David A. Claremon; Lanqi Jia; Angel Morales-Ramos; Suresh B. Singh; Shankar Venkatraman; Zhenrong Xu; Yajun Zheng


Archive | 2009

Salts Of Methyl 2-((R))-(3-Chlorophenyl)((R)-1-((S)-2-(Methylamino)-3((R)-tetrahydro-2H-Pyran-3-YL)Propylcarbamoyl)Piperidin-3-YL)Methoxy)Ethylcarbamate

David A. Claremon; Robert D. Simpson; Lanqi Jia


Archive | 2017

Modulators of ror-gamma

David A. Claremon; Lawrence W. Dillard; Yi Fan; Lanqi Jia; Suresh B. Singh; Colin M. Tice; Zhenrong Xu; Jing Yuan; Linghang Zhuang


Archive | 2016

ISOINDOLINE INHIBITORS OF ROR-GAMMA

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

Inhibitors of β-secretase

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

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Wei Zhao

Boehringer Ingelheim

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