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Items: 1 to 20 of 265

1.

Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG.

J Med Chem. 2005 Jul 28;48(15):5025-37.

PMID:
16033281
2.

7-But-2-ynyl-9-(6-methoxy-pyridin-3-yl)-6-piperazin-1-yl-7,9-dihydro-purin-8-one is a novel competitive and selective inhibitor of dipeptidyl peptidase IV with an antihyperglycemic activity.

Yamazaki K, Yasuda N, Inoue T, Nagakura T, Kira K, Shinoda M, Saeki T, Tanaka I.

J Pharmacol Exp Ther. 2006 Dec;319(3):1253-7. Epub 2006 Sep 15.

3.

1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.

Villhauer EB, Brinkman JA, Naderi GB, Burkey BF, Dunning BE, Prasad K, Mangold BL, Russell ME, Hughes TE.

J Med Chem. 2003 Jun 19;46(13):2774-89.

PMID:
12801240
4.

Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.

Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG.

J Med Chem. 2004 May 6;47(10):2587-98.

PMID:
15115400
5.

Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.

Pei Z, Li X, Longenecker K, von Geldern TW, Wiedeman PE, Lubben TH, Zinker BA, Stewart K, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Long M, Wells H, Kempf-Grote AJ, Madar DJ, McDermott TS, Bhagavatula L, Fickes MG, Pireh D, Solomon LR, Lake MR, Edalji R, Fry EH, Sham HL, Trevillyan JM.

J Med Chem. 2006 Jun 15;49(12):3520-35. Erratum in: J Med Chem. 2006 Aug 24;49(17):5387.

PMID:
16759095
6.
7.

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

Edmondson SD, Mastracchio A, Mathvink RJ, He J, Harper B, Park YJ, Beconi M, Di Salvo J, Eiermann GJ, He H, Leiting B, Leone JF, Levorse DA, Lyons K, Patel RA, Patel SB, Petrov A, Scapin G, Shang J, Roy RS, Smith A, Wu JK, Xu S, Zhu B, Thornberry NA, Weber AE.

J Med Chem. 2006 Jun 15;49(12):3614-27.

PMID:
16759103
8.

Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor.

Gupta RC, Chhipa L, Mandhare AB, Zambad SP, Chauthaiwale V, Nadkarni SS, Dutt C.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5021-5. doi: 10.1016/j.bmcl.2009.07.058. Epub 2009 Jul 12.

PMID:
19643608
9.

Saxagliptin, a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Gallwitz B.

IDrugs. 2008 Dec;11(12):906-17. Review. Erratum in: IDrugs. 2009 Mar;12(3):200.

PMID:
19051153
10.

1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.

Villhauer EB, Brinkman JA, Naderi GB, Dunning BE, Mangold BL, Mone MD, Russell ME, Weldon SC, Hughes TE.

J Med Chem. 2002 Jun 6;45(12):2362-5.

PMID:
12036346
11.

Potent and selective proline derived dipeptidyl peptidase IV inhibitors.

Edmondson SD, Mastracchio A, Beconi M, Colwell LF Jr, Habulihaz B, He H, Kumar S, Leiting B, Lyons KA, Mao A, Marsilio F, Patel RA, Wu JK, Zhu L, Thornberry NA, Weber AE, Parmee ER.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5151-5.

PMID:
15380217
12.

cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization.

Wright SW, Ammirati MJ, Andrews KM, Brodeur AM, Danley DE, Doran SD, Lillquist JS, McClure LD, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soeller WC, Soglia CB, Treadway JL, VanVolkenburg MA, Wang H, Wilder DC, Olson TV.

J Med Chem. 2006 Jun 1;49(11):3068-76.

PMID:
16722626
13.

Antihyperglycemic effects of ASP8497 in streptozotocin-nicotinamide induced diabetic rats: comparison with other dipeptidyl peptidase-IV inhibitors.

Tahara A, Matsuyama-Yokono A, Nakano R, Someya Y, Hayakawa M, Shibasaki M.

Pharmacol Rep. 2009 Sep-Oct;61(5):899-908.

14.

Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors.

Fukushima H, Hiratate A, Takahashi M, Mikami A, Saito-Hori M, Munetomo E, Kitano K, Chonan S, Saito H, Suzuki A, Takaoka Y, Yamamoto K.

Bioorg Med Chem. 2008 Apr 1;16(7):4093-106. doi: 10.1016/j.bmc.2008.01.016. Epub 2008 Jan 16.

PMID:
18243000
15.

(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.

Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, Hickey GJ, Kowalchick JE, Leiting B, Lyons K, Marsilio F, McCann ME, Patel RA, Petrov A, Scapin G, Patel SB, Roy RS, Wu JK, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE.

J Med Chem. 2005 Jan 13;48(1):141-51.

PMID:
15634008
16.

DPP-4 inhibitors and their potential role in the management of type 2 diabetes.

Barnett A.

Int J Clin Pract. 2006 Nov;60(11):1454-70. Review.

PMID:
17073841
17.

Inhibition of dipeptidyl peptidase IV by novel inhibitors with pyrazolidine scaffold.

Cheon HG, Kim SS, Kim KR, Rhee SD, Yang SD, Ahn JH, Park SD, Lee JM, Jung WH, Lee HS, Kim HY.

Biochem Pharmacol. 2005 Jul 1;70(1):22-9.

PMID:
15893294
18.

RBx-0597, a potent, selective and slow-binding inhibitor of dipeptidyl peptidase-IV for the treatment of type 2 diabetes.

Singh S, Roy S, Sethi S, Benjamin B, Sundaram S, Khanna V, Kandalkar SR, Pal C, Kant R, Patra AK, Rayasam G, Mittra S, Saini KS, Paliwal J, Chugh A, Ahmed S, Sattigeri J, Cliff I, Ray A, Bansal VS, Bhatnagar PK, Davis JA.

Eur J Pharmacol. 2011 Feb 10;652(1-3):157-63. doi: 10.1016/j.ejphar.2010.06.001. Epub 2010 Jun 9. Erratum in: Eur J Pharmacol. 2011 Mar 25;655(1-3):121. multiple author names added.

PMID:
20540938
19.

Saxagliptin: a new drug for the treatment of type 2 diabetes.

Thareja S, Aggarwal S, Malla P, Haksar D, Bhardwaj TR, Kumar M.

Mini Rev Med Chem. 2010 Jul;10(8):759-65. Review.

PMID:
20402634
20.

ASP4000, a slow-binding dipeptidyl peptidase 4 inhibitor, has antihyperglycemic activity of long duration in Zucker fatty rats.

Tanaka-Amino K, Matsumoto K, Hatakeyama Y, Takakura S, Mutoh S.

Acta Diabetol. 2010 Mar;47(1):43-8. doi: 10.1007/s00592-009-0096-5. Epub 2009 Feb 24.

PMID:
19238312

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