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Kathryn A. Lyons
Researcher at Merck & Co.
Publications - 56
Citations - 3121
Kathryn A. Lyons is an academic researcher from Merck & Co.. The author has contributed to research in topics: Sodium channel blocker & Dipeptidyl peptidase. The author has an hindex of 24, co-authored 56 publications receiving 2977 citations.
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Journal ArticleDOI
(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Dooseop Kim,Liping Wang,Maria G. Beconi,George J. Eiermann,Michael H. Fisher,Huaibing He,Gerard J. Hickey,Jennifer E. Kowalchick,Barbara Leiting,Kathryn A. Lyons,Frank Marsilio,Margaret E. McCann,Reshma A. Patel,Aleksandr Petrov,Giovanna Scapin,Sangita B. Patel,Ranabir Sinha Roy,Joseph K. Wu,Matthew J. Wyvratt,Bei B. Zhang,Lan Zhu,Nancy A. Thornberry,Ann E. Weber +22 more
TL;DR: A novel series of beta-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes and MK-0431, the phosphate salt of compound 1, was selected for development.
Journal ArticleDOI
Dipeptidyl Peptidase IV Inhibition for the Treatment of Type 2 Diabetes: Potential Importance of Selectivity Over Dipeptidyl Peptidases 8 and 9
George R. Lankas,Barbara Leiting,Ranabir Sinha Roy,George J. Eiermann,Maria G. Beconi,Tesfaye Biftu,Chi-Chung Chan,Scott D. Edmondson,William P. Feeney,Huaibing He,Dawn E. Ippolito,Dooseop Kim,Kathryn A. Lyons,Hyun O. Ok,Reshma A. Patel,Aleksandr Petrov,Kelly Ann Pryor,Xiaoxia Qian,Leah Bitalac Reigle,Andrea Woods,Joseph K. Wu,Dennis M. Zaller,Xiaoping Zhang,Lan Zhu,Ann E. Weber,Nancy A. Thornberry +25 more
TL;DR: Assessment of selectivity of potential clinical candidates may be important to an optimal safety profile for this new class of antihyperglycemic agents, according to the results of toxicity and tolerability studies.
Journal ArticleDOI
Analgesic Effects of a Substituted N-Triazole Oxindole (TROX-1), a State-Dependent, Voltage-Gated Calcium Channel 2 Blocker
Catherine Abbadie,Owen B. McManus,Shu-Yu Sun,Randal M. Bugianesi,Ge Dai,Rodolfo Haedo,James B Herrington,Gregory J. Kaczorowski,McHardy M. Smith,Andrew M. Swensen,Vivien A. Warren,Brande S. Williams,Stephen P. Arneric,Cyrus Eduljee,Terrance P. Snutch,Elizabeth Tringham,Nina Jochnowitz,Annie Liang,D. Euan MacIntyre,Erin McGowan,Shruti Mistry,Valerie V. White,Scott B. Hoyt,Clare London,Kathryn A. Lyons,Patricia B. Bunting,Sylvia Volksdorf,Joseph L. Duffy +27 more
TL;DR: TROX-1 demonstrates that an orally available state-dependent Cav2 channel blocker may achieve a therapeutic window suitable for the treatment of chronic pain.
Journal ArticleDOI
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors
Scott D. Edmondson,Lan Wei,Jinyou Xu,Jackie Shang,Shiyao Xu,Jianmei Pang,Ashok Chaudhary,Dennis C. Dean,Huaibing He,Barbara Leiting,Kathryn A. Lyons,Reshma A. Patel,Sangita B. Patel,Giovanna Scapin,Joseph K. Wu,Maria G. Beconi,Nancy A. Thornberry,Ann E. Weber +17 more
TL;DR: A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors.
Journal ArticleDOI
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors
Linda Brockunier,Jiafang He,Lawrence F. Colwell,Bahanu Habulihaz,Huaibing He,Barbara Leiting,Kathryn A. Lyons,Frank Marsilio,Reshma A. Patel,Yohannes Teffera,Joseph K. Wu,Nancy A. Thornberry,Ann E. Weber,Emma R. Parmee +13 more
TL;DR: Simplification of the molecule and incorporation of multiple fluorine atoms on the phenyl ring has provided low molecular weight analogs such as compound 32, which is a 19nM DP-IV inhibitor with >4000-fold selectivity over QPP.