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2 results on '"Juerg Lehmann"'

1. Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series

Author

Khawja A. Usmani, Dawei Yue, Zhi-Liang Chu, Abu J.M. Sadeque, Chris Carroll, Chuan Chen, Hsin-Hui Shu, Sanju Narayanan, Hussein Al-Sharmma, Dominic P. Behan, Robert M. Jones, Graeme Semple, James N. Leonard, David J. Unett, Daniel J. Buzard, Michael Morgan, Juerg Lehmann, Imelda Calderon, Shiu-Feng Tung, Woo Hyun Yoon, Xiuwen Zhu, Sangdon Han, Andrew M. Kawasaki, Amy Siu-Ting Wong, and Sun Hee Kim

Subjects
Blood Glucose, Male, medicine.medical_specialty, Clinical Biochemistry, Administration, Oral, Pharmaceutical Science, Pharmacology, Biochemistry, Rats sprague dawley, Receptors, G-Protein-Coupled, Rats, Sprague-Dawley, Mice, Structure-Activity Relationship, chemistry.chemical_compound, Cyclohexanes, Internal medicine, Drug Discovery, medicine, Animals, Humans, Hypoglycemic Agents, Structure–activity relationship, Gpr119 agonist, Molecular Biology, Glycemic, Organic Chemistry, Rats, Zucker, Endocrinology, Diabetes Mellitus, Type 2, chemistry, Molecular Medicine, Lead compound
Abstract

The design and optimization of a novel trans-1,4-dioxycyclohexane GPR119 agonist series is described. A lead compound 21 was found to be a potent and efficacious GPR119 agonist across species, and possessed overall favorable pharmaceutical properties. Compound 21 demonstrated robust acute and chronic regulatory effects on glycemic parameters in the diabetic or non-diabetic rodent models.

Published
2015
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2. Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease

Author

Joel Gatlin, Kevin Whelan, Michael Morgan, Juerg Lehmann, Lixia Fu, Yinghong Gao, Moody Jeanne, Minh Le, Hussien A. Al-Shamma, Jeremy Barden, Khawja A. Usmani, Jeff Edwards, Chuan Chen, Jayant Thatte, Dipanjan Sengupta, Xiuwen Zhu, Abu J.M. Sadeque, Imelda Calderon, Michelle Solomon, Lars Thoresen, Tawfik Gharbaoui, Robert M. Jones, Ling Liu, Luis Lopez, Daniel J. Buzard, Brett Ullman, Krishnan Ashwin M, Sheryll Espinola, Charles Xing, Sangdon Han, and Andrew M. Kawasaki

Subjects
Autoimmune disease, chemistry.chemical_classification, Chemistry, Sphingosine-1-phosphate receptor, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, medicine.disease, Biochemistry, In vitro, Sprague dawley, In vivo, Drug Discovery, medicine, Molecular Medicine, Structure–activity relationship, lipids (amino acids, peptides, and proteins), Receptor, Molecular Biology, Tricyclic
Abstract

Two series of fused tricyclic indoles were identified as potent and selective S1P(1) agonists. In vivo these agonists produced a significant reduction in circulating lymphocytes which translated into robust efficacy in several rodent models of autoimmune disease. Importantly, these agonists were devoid of any activity at the S1P(3) receptor in vitro, and correspondingly did not produce S1P(3) mediated bradycardia in telemeterized rat.

Published
2012
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