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Dipeptidyl peptidase IV inhibitors for the treatment of diabetes

Weber, Ann E

Journal of medicinal chemistry, 12 August 2004, Vol.47(17), pp.4135-41 [Peer Reviewed Journal]

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Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selective β3 adrenergic receptor agonists for the treatment of overactive bladder

Moyes, Christopher R ; Berger, Richard ; Goble, Stephen D ; Harper, Bart ; Shen, Dong-Ming ; Wang, Liping ; Bansal, Alka ; Brown, Patricia N ; Chen, Airu S ; Dingley, Karen H ; Di Salvo, Jerry ; Fitzmaurice, Aileen ; Gichuru, Loise N ; Hurley, Amanda L ; Jochnowitz, Nina ; Miller, Randall R ; Mistry, Shruty ; Nagabukuro, Hiroshi ; Salituro, Gino M ; Sanfiz

Journal of medicinal chemistry, 27 February 2014, Vol.57(4), pp.1437-53 [Peer Reviewed Journal]

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Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes

Biftu, Tesfaye ; Sinha-Roy, Ranabir ; Chen, Ping ; Qian, Xiaoxia ; Feng, Dennis ; Kuethe, Jeffrey T ; Scapin, Giovanna ; Gao, Ying Duo ; Yan, Youwei ; Krueger, Davida ; Bak, Annette ; Eiermann, George ; He, Jiafang ; Cox, Jason ; Hicks, Jacqueline ; Lyons, Kathy ; He, Huaibing ; Salituro, Gino ; Tong, Sharon ; Patel

Journal of medicinal chemistry, 24 April 2014, Vol.57(8), pp.3205-12 [Peer Reviewed Journal]

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Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder

Edmondson, Scott D ; Zhu, Cheng ; Kar, Nam Fung ; Di Salvo, Jerry ; Nagabukuro, Hiroshi ; Sacre-Salem, Beatrice ; Dingley, Karen ; Berger, Richard ; Goble, Stephen D ; Morriello, Gregori ; Harper, Bart ; Moyes, Christopher R ; Shen, Dong-Ming ; Wang, Liping ; Ball, Richard ; Fitzmaurice, Aileen ; Frenkl, Tara ; Gichuru, Loise N ; Ha, Sookhee ; Hurley

Journal of medicinal chemistry, 28 January 2016, Vol.59(2), pp.609-23 [Peer Reviewed Journal]

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Synthesis and evaluation of [(1 R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1 R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors

Chen, Ping ; Caldwell, Charles G ; Ashton, Wallace ; Wu, Joseph K ; He, Huaibing ; Lyons, Kathryn A ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(6), pp.1880-1886 [Peer Reviewed Journal]

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Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists

Wang, Liping ; Hubert, James A ; Lee, Susan J ; Pan, Jie ; Qian, Su ; Reitman, Marc L ; Strack, Alison M ; Weingarth, Drew T ; Macneil, Douglas J ; Weber, Ann E ; Edmondson, Scott D

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(10), pp.2911-2915 [Peer Reviewed Journal]

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The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors

Cox, Jason M ; Chu, Hong D ; Kuethe, Jeffrey T ; Gao, Ying-Duo ; Scapin, Giovanna ; Eiermann, George ; He, Huaibing ; Li, Xiaohua ; Lyons, Kathryn A ; Metzger, Joseph ; Petrov, Aleksandr ; Wu, Joseph K ; Xu, Shiyao ; Sinha-Roy, Ranabir ; Weber, Ann E ; Biftu, Tesfaye

Bioorganic & Medicinal Chemistry Letters, 01 June 2016, Vol.26(11), pp.2622-2626 [Peer Reviewed Journal]

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Discovery of benzamides as potent human β3 adrenergic receptor agonists

Zhu, Cheng ; Kar, Nam F ; Li, Bing ; Costa, Melissa ; Dingley, Karen H ; Di Salvo, Jerry ; Ha, Sookhee N ; Hurley, Amanda L ; Li, Xiaofang ; Miller, Randy R ; Salituro, Gino M ; Struthers, Mary ; Weber, Ann E ; Hale, Jeffrey J ; Edmondson, Scott D

Bioorganic & Medicinal Chemistry Letters, 01 January 2016, Vol.26(1), pp.55-59 [Peer Reviewed Journal]

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Asymmetric synthesis of anti-β-hydroxy-α-amino acids

Evans, David A ; Sjogren, Eric B ; Weber, Ann E ; Conn, Robin E

Tetrahedron Letters, 1987, Vol.28(1), pp.39-42 [Peer Reviewed Journal]

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Structure–activity-relationship of amide and sulfonamide analogs of omarigliptin

Chen, Ping ; Feng, Dennis ; Qian, Xiaoxia ; Apgar, James ; Wilkening, Robert ; Kuethe, Jeffrey T ; Gao, Ying-Duo ; Scapin, Giovanna ; Cox, Jason ; Doss, George ; Eiermann, George ; He, Huaibing ; Li, Xiaohua ; Lyons, Kathryn A ; Metzger, Joseph ; Petrov, Aleksandr ; Wu, Joseph K ; Xu, Shiyao ; Weber, Ann E ; Yan, Youwei

Bioorganic & Medicinal Chemistry Letters, 15 December 2015, Vol.25(24), pp.5767-5771 [Peer Reviewed Journal]

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Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine (23)

Biftu, Tesfaye ; Qian, Xiaoxia ; Chen, Ping ; Feng, Dennis ; Scapin, Giovanna ; Gao, Ying-Duo ; Cox, Jason ; Sinha Roy, Ranabir ; Eiermann, George ; He, Huabing ; Lyons, Kathy ; Salituro, Gino ; Patel, Sangita ; Petrov, Alexander ; Xu, Feng ; Xu, Shiyao Sherrie ; Zhang, Bei ; Caldwell, Charles ; Wu, Joseph K ; Lyons, Kathy

Bioorganic & Medicinal Chemistry Letters, 01 October 2013, Vol.23(19), pp.5361-5366 [Peer Reviewed Journal]

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A comparative study of the binding properties, dipeptidyl peptidase‐4 (DPP‐4) inhibitory activity and glucose‐lowering efficacy of the DPP‐4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice

Berger, Joel P. ; Sinharoy, Ranabir ; Pocai, Alessandro ; Kelly, Theresa M. ; Scapin, Giovanna ; Gao, Ying‐Duo ; Pryor, Kelly Ann D. ; Wu, Joseph K. ; Eiermann, George J. ; Xu, Shiyao S. ; Zhang, Xiaoping ; Tatosian, Daniel A. ; Weber, Ann E. ; Thornberry, Nancy A. ; Carr, Richard D.

Endocrinology, Diabetes & Metabolism, January 2018, Vol.1(1), pp.n/a-n/a [Peer Reviewed Journal]

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Corrigendum to “Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(4,6-dihydropyrrolo[3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23)” [Bioorg. Med. Chem. Lett. 23 (2013) 5361–5366]

Biftu, Tesfaye ; Qian, Xiaoxia ; Chen, Ping ; Feng, Dennis ; Scapin, Giovanna ; Gao, Ying-Duo ; Cox, Jason ; Roy, Ranabir Sinha ; Eiermann, George ; He, Huabing ; Lyons, Kathy ; Salituro, Gino ; Patel, Sangita ; Petrov, Alexander ; Xu, Feng ; Xu, Shiyao Sherrie ; Zhang, Bei ; Caldwell, Charles ; Wu, Joseph K ; Lyons, Kathy

Bioorganic & Medicinal Chemistry Letters, 01 June 2014, Vol.24(11), pp.2590-2590 [Peer Reviewed Journal]

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Concise syntheses and HCV NS5B polymerase inhibition of (2′R)-3 and (2′S)-2′-ethynyluridine-10 and related nucleosides

Bennett, Frank ; Buevich, Alexei V ; Huang, Hsueh-Cheng ; Girijavallabhan, Vinay ; Kerekes, Angela D ; Huang, Yuhua ; Malikzay, Asra ; Smith, Elizabeth ; Ferrari, Eric ; Senior, Mary ; Osterman, Rebecca ; Wang, Lingyan ; Wang, Jun ; Pu, Haiyan ; Truong, Quang T ; Tawa, Paul ; Bogen, Stephane L ; Davies, Ian W ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 01 December 2017, Vol.27(23), pp.5349-5352 [Peer Reviewed Journal]

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Macrocyclic renin inhibitors: Synthesis of a subnanomolar, orally active cysteine derived inhibitor

Yang, Lihu ; Weber, Ann E ; Greenlee, William J ; Patchett, Arthur A

Tetrahedron Letters, 1993, Vol.34(44), pp.7035-7038 [Peer Reviewed Journal]

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16
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Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition

Liu, Weiguo ; Shao, Pengcheng P ; Liang, Gui-Bai ; Bawiec, John ; He, Jiafang ; Aster, Susan D ; Wu, Margaret ; Chicchi, Garry ; Wang, John ; Tsao, Kwei-Lan ; Shang, Jin ; Salituro, Gino ; Zhou, Yun-Ping ; Li, Cai ; Akiyama, Taro E ; Metzger, Daniel E ; Murphy, Beth Ann ; Howard, Andrew D ; Weber, Ann E ; Duffy

ACS medicinal chemistry letters, 08 November 2018, Vol.9(11), pp.1082-1087 [Peer Reviewed Journal]

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Heterocyclic acetamide and benzamide derivatives as potent and selective β 3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles

Goble, Stephen D ; Wang, Liping ; Howell, K. Lulu ; Bansal, Alka ; Berger, Richard ; Brockunier, Linda ; Disalvo, Jerry ; Feighner, Scott ; Harper, Bart ; He, Jiafang ; Hurley, Amanda ; Hreniuk, Donna ; Parmee, Emma ; Robbins, Michael ; Salituro, Gino ; Sanfiz, Anthony ; Streckfuss, Eric ; Watkins, Eloisa ; Weber, Ann E ; Struthers, Mary

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(6), pp.1895-1899 [Peer Reviewed Journal]

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18
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Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines

Kim, Dooseop ; Kowalchick, Jennifer E ; Brockunier, Linda L ; Parmee, Emma R ; Eiermann, George J ; Fisher, Michael H ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn ; Scapin, Giovanna ; Patel, Sangita B ; Petrov, Aleksandr ; Pryor, Kellyann D ; Roy, Ranabir Sinha ; Wu, Joseph K ; Zhang, Xiaoping ; Wyvratt, Matthew J ; Zhang, Bei B ; Zhu, Lan ; Thornberry

Journal of medicinal chemistry, 14 February 2008, Vol.51(3), pp.589-602 [Peer Reviewed Journal]

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19
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Novel Quinoline-Based P2-P4 Macrocyclic Derivatives As Pan-Genotypic HCV NS3/4a Protease Inhibitors

Shah, Unmesh ; Jayne, Charles ; Chackalamannil, Samuel ; Velázquez, Francisco ; Guo, Zhuyan ; Buevich, Alexei ; Howe, John A ; Chase, Robert ; Soriano, Aileen ; Agrawal, Sony ; Rudd, Michael T ; Mccauley, John A ; Liverton, Nigel J ; Romano, Joseph ; Bush, Kimberly ; Coleman, Paul J ; Grisé-Bard, Christiane ; Brochu

ACS medicinal chemistry letters, 13 March 2014, Vol.5(3), pp.264-9 [Peer Reviewed Journal]

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(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-1,2,4triazolo1,5-a-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Edmondson, Scott D ; Mastracchio, Anthony ; Mathvink, Robert J ; He, Jiafang ; Harper, Bart ; Park, You-Jung ; Beconi, Maria ; Di Salvo, Jerry ; Eiermann, George J ; He, Huaibing ; Leiting, Barbara ; Leone, Joseph F ; Levorse, Dorothy A ; Lyons, Kathryn ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Aleksandr ; Scapin, Giovanna ; Shang, Jackie ; Roy

Journal of medicinal chemistry, 15 June 2006, Vol.49(12), pp.3614-27 [Peer Reviewed Journal]

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(2R)-4-oxo-4-3-(trifluoromethyl)-5,6-dihydro1,2,4triazolo4,3-apyrazin-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

Kim, Dooseop ; Wang, Liping ; Beconi, Maria ; Eiermann, George J ; Fisher, Michael H ; He, Huaibing ; Hickey, Gerard J ; Kowalchick, Jennifer E ; Leiting, Barbara ; Lyons, Kathryn ; Marsilio, Frank ; Mccann, Margaret E ; Patel, Reshma A ; Petrov, Aleksandr ; Scapin, Giovanna ; Patel, Sangita B ; Roy, Ranabir Sinha ; Wu, Joseph K ; Wyvratt, Matthew J ; Zhang

Journal of medicinal chemistry, 13 January 2005, Vol.48(1), pp.141-51 [Peer Reviewed Journal]

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22
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Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9

Lankas, George R ; Leiting, Barbara ; Roy, Ranabir Sinha ; Eiermann, George J ; Beconi, Maria G ; Biftu, Tesfaye ; Chan, Chi-Chung ; Edmondson, Scott ; Feeney, William P ; He, Huaibing ; Ippolito, Dawn E ; Kim, Dooseop ; Lyons, Kathryn A ; Ok, Hyun O ; Patel, Reshma A ; Petrov, Aleksandr N ; Pryor, Kelly Ann ; Qian, Xiaoxia ; Reigle, Leah ; Woods

Diabetes, October 2005, Vol.54(10), pp.2988-94 [Peer Reviewed Journal]

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Discovery of a Potent, Orally Bioavailable β 3 Adrenergic Receptor Agonist, ( R )- N -[4-[2-[[2-Hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide
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Discovery of a Potent, Orally Bioavailable β 3 Adrenergic Receptor Agonist, ( R )- N -[4-[2-[[2-Hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide

Mathvink, Robert J. ; Tolman, J. Samuel ; Chitty, Dawn ; Candelore, Mari R. ; Cascieri, Margaret A. ; Colwell, Lawrence F. ; Deng, Liping ; Feeney, William P. ; Forrest, Michael J. ; Hom, Gary J. ; Macintyre, D. Euan ; Miller, Randall R. ; Stearns, Ralph A. ; Tota, Laurie ; Wyvratt, Matthew J. ; Fisher, Michael H. ; Weber, Ann E.

Journal of Medicinal Chemistry, 10/2000, Vol.43(21), pp.3832-3836 [Peer Reviewed Journal]

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L-750355, a human ß3-adrenoceptor agonist; in vitro pharmacology and profile of activity in vivo in the rhesus monkey

Forrest, Michael J ; Hom, Gary ; Bach, Tom ; Candelore, Mari Rios ; Cascieri, Margaret A ; Strader, Catherine ; Tota, Laurie ; Fisher, Michael H ; Szumiloski, John ; Ok, Hyun O ; Weber, Ann E ; Wyvratt, Matthew ; Vicario, Pasquale ; Marko, Olga ; Deng, Liping ; Cioffe, Christine ; Hegarty-Friscino, Bonnie ; Macintyre, Euan

European Journal of Pharmacology, 2000, Vol.407(1), pp.175-181 [Peer Reviewed Journal]

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Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors

Edmondson, Scott D ; Mastracchio, Anthony ; Cox, Jason M ; Eiermann, George J ; He, Huaibing ; Lyons, Kathryn A ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Aleksandr ; Scapin, Giovanna ; Wu, Joseph K ; Xu, Shiyao ; Zhu, Bing ; Thornberry, Nancy A ; Roy, Ranabir Sinha ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 01 August 2009, Vol.19(15), pp.4097-4101 [Peer Reviewed Journal]

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Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design

Liang, Gui-Bai ; Qian, Xiaoxia ; Biftu, Tesfaye ; Singh, Suresh ; Gao, Ying-Duo ; Scapin, Giovanna ; Patel, Sangita ; Leiting, Barbara ; Patel, Reshma ; Wu, Joseph ; Zhang, Xiaoping ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(13), pp.3706-3710 [Peer Reviewed Journal]

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Design, synthesis, and biological evaluation of triazolopiperazine-based β-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors

Kowalchick, Jennifer E ; Leiting, Barbara ; Pryor, Kellyann D ; Marsilio, Frank ; Wu, Joseph K ; He, Huaibing ; Lyons, Kathryn A ; Eiermann, George J ; Petrov, Aleksandr ; Scapin, Giovanna ; Patel, Reshma A ; Thornberry, Nancy A ; Weber, Ann E ; Kim, Dooseop

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(21), pp.5934-5939 [Peer Reviewed Journal]

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Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes

Chen, Ping ; Caldwell, Charles G ; Mathvink, Robert J ; Leiting, Barbara ; Marsilio, Frank ; Patel, Reshma A ; Wu, Joseph K ; He, Huaibing ; Lyons, Kathryn A ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(21), pp.5853-5857 [Peer Reviewed Journal]

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Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors

Cox, Jason M ; Harper, Bart ; Mastracchio, Anthony ; Leiting, Barbara ; Sinha Roy, Ranabir ; Patel, Reshma A ; Wu, Joseph K ; Lyons, Kathryn A ; He, Huaibing ; Xu, Shiyao ; Zhu, Bing ; Thornberry, Nancy A ; Weber, Ann E ; Edmondson, Scott D

Bioorganic & Medicinal Chemistry Letters, 15 August 2007, Vol.17(16), pp.4579-4583 [Peer Reviewed Journal]

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Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors

Gao, Ying-Duo ; Feng, Dennis ; Sheridan, Robert P ; Scapin, Giovanna ; Patel, Sangita B ; Wu, Joseph K ; Zhang, Xiaoping ; Sinha-Roy, Ranabir ; Thornberry, Nancy A ; Weber, Ann E ; Biftu, Tesfaye

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(14), pp.3877-3879 [Peer Reviewed Journal]

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Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes

Liang, Gui-Bai ; Qian, Xiaoxia ; Feng, Dennis ; Biftu, Tesfaye ; Eiermann, George ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathy ; Petrov, Aleksandr ; Sinha-Roy, Ranabir ; Zhang, Bei ; Wu, Joseph ; Zhang, Xiaoping ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(7), pp.1903-1907 [Peer Reviewed Journal]

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Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole

Ashton, Wallace T ; Sisco, Rosemary M ; Dong, Hong ; Lyons, Kathryn A ; He, Huaibing ; Doss, George A ; Leiting, Barbara ; Patel, Reshma A ; Wu, Joseph K ; Marsilio, Frank ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2005, Vol.15(9), pp.2253-2258 [Peer Reviewed Journal]

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Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors

Xu, Jinyou ; Wei, Lan ; Mathvink, Robert ; He, Jiafang ; Park, You-Jung ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Marsilio, Frank ; Patel, Reshma A ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 16 May 2005, Vol.15(10), pp.2533-2536 [Peer Reviewed Journal]

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Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors

Ashton, Wallace T ; Dong, Hong ; Sisco, Rosemary M ; Doss, George A ; Leiting, Barbara ; Patel, Reshma A ; Wu, Joseph K ; Marsilio, Frank ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 23 February 2004, Vol.14(4), pp.859-863 [Peer Reviewed Journal]

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Human β3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties

Brockunier, Linda L ; Candelore, Mari R ; Cascieri, Margaret A ; Liu, Yong ; Tota, Laurie ; Wyvratt, Matthew J ; Fisher, Michael H ; Weber, Ann E ; Parmee, Emma R

Bioorganic & Medicinal Chemistry Letters, 02 February 2001, Vol.11(3), pp.379-382 [Peer Reviewed Journal]

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