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Items: 1 to 20 of 131

1.

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) [corrected].

Biftu T, Qian X, Chen P, Feng D, Scapin G, Gao YD, Cox J, Roy RS, Eiermann G, He H, Lyons K, Salituro G, Patel S, Petrov A, Xu F, Xu SS, Zhang B, Caldwell C, Wu JK, Lyons K, Weber AE.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5361-6. doi: 10.1016/j.bmcl.2013.07.061. Epub 2013 Aug 5. Erratum in: Bioorg Med Chem Lett. 2014 Jun 1;24(11):2590.

PMID:
23972441
2.

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

Chen P, Feng D, Qian X, Apgar J, Wilkening R, Kuethe JT, Gao YD, Scapin G, Cox J, Doss G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Weber AE, Yan Y, Roy RS, Biftu T.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5767-71. doi: 10.1016/j.bmcl.2015.10.070. Epub 2015 Oct 30.

PMID:
26546218
3.

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

Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE.

J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2.

PMID:
24660890
4.

(3R)-3-amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Nitta A, Fujii H, Sakami S, Nishimura Y, Ohyama T, Satoh M, Nakaki J, Satoh S, Inada C, Kozono H, Kumagai H, Shimamura M, Fukazawa T, Kawai H.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5435-8. doi: 10.1016/j.bmcl.2008.09.042. Epub 2008 Sep 12.

PMID:
18819797
5.

Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors.

Nitta A, Fujii H, Sakami S, Satoh M, Nakaki J, Satoh S, Kumagai H, Kawai H.

Bioorg Med Chem Lett. 2012 Dec 1;22(23):7036-40. doi: 10.1016/j.bmcl.2012.09.099. Epub 2012 Oct 2.

PMID:
23072865
6.

Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Yoshida T, Akahoshi F, Sakashita H, Kitajima H, Nakamura M, Sonda S, Takeuchi M, Tanaka Y, Ueda N, Sekiguchi S, Ishige T, Shima K, Nabeno M, Abe Y, Anabuki J, Soejima A, Yoshida K, Takashina Y, Ishii S, Kiuchi S, Fukuda S, Tsutsumiuchi R, Kosaka K, Murozono T, Nakamaru Y, Utsumi H, Masutomi N, Kishida H, Miyaguchi I, Hayashi Y.

Bioorg Med Chem. 2012 Oct 1;20(19):5705-19. doi: 10.1016/j.bmc.2012.08.012. Epub 2012 Aug 17.

PMID:
22959556
7.

Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.

Sutton JM, Clark DE, Dunsdon SJ, Fenton G, Fillmore A, Harris NV, Higgs C, Hurley CA, Krintel SL, MacKenzie RE, Duttaroy A, Gangl E, Maniara W, Sedrani R, Namoto K, Ostermann N, Gerhartz B, Sirockin F, Trappe J, Hassiepen U, Baeschlin DK.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1464-8. doi: 10.1016/j.bmcl.2011.11.054. Epub 2011 Nov 20. Erratum in: Bioorg Med Chem Lett. 2012 Mar 15;22(6):2359.

PMID:
22177783
8.

The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.

Deng J, Peng L, Zhang G, Lan X, Li C, Chen F, Zhou Y, Lin Z, Chen L, Dai R, Xu H, Yang L, Zhang X, Hu W.

Eur J Med Chem. 2011 Jan;46(1):71-6. doi: 10.1016/j.ejmech.2010.10.016. Epub 2010 Oct 26.

PMID:
21106276
9.

Discovery of β-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors.

Park WS, Kang SK, Jun MA, Shin MS, Kim KY, Rhee SD, Bae MA, Kim MS, Kim KR, Kang NS, Yoo SE, Lee JO, Song DH, Silinski P, Schneider SE, Ahn JH, Kim SS.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1366-70. doi: 10.1016/j.bmcl.2011.01.041. Epub 2011 Jan 14.

PMID:
21306895
10.

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

Lankas GR, Leiting B, Roy RS, Eiermann GJ, Beconi MG, Biftu T, Chan CC, Edmondson S, Feeney WP, He H, Ippolito DE, Kim D, Lyons KA, Ok HO, Patel RA, Petrov AN, Pryor KA, Qian X, Reigle L, Woods A, Wu JK, Zaller D, Zhang X, Zhu L, Weber AE, Thornberry NA.

Diabetes. 2005 Oct;54(10):2988-94.

11.

2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A.

Nishio Y, Kimura H, Sawada N, Sugaru E, Horiguchi M, Ono M, Furuta Y, Sakai M, Masui Y, Otani M, Hashizuka T, Honda Y, Deguchi J, Nakagawa T, Nakahira H.

Bioorg Med Chem. 2011 Sep 15;19(18):5490-9. doi: 10.1016/j.bmc.2011.07.042. Epub 2011 Aug 4.

PMID:
21865048
12.

Discovery of potent dipeptidyl peptidase IV inhibitors through pharmacophore hybridization and hit-to-lead optimization.

Zeng S, Xie H, Zeng LL, Lu X, Zhao X, Zhang GC, Tu ZC, Xu HJ, Yang L, Zhang XQ, Hu W.

Bioorg Med Chem. 2013 Apr 1;21(7):1749-55. doi: 10.1016/j.bmc.2013.01.062. Epub 2013 Feb 8.

PMID:
23434133
13.

Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.

Wang J, Feng Y, Ji X, Deng G, Leng Y, Liu H.

Bioorg Med Chem. 2013 Dec 1;21(23):7418-29. doi: 10.1016/j.bmc.2013.09.048. Epub 2013 Oct 1.

PMID:
24153396
14.

Design, synthesis and biological evaluation of novel aminomethyl-piperidones based DPP-IV inhibitors.

Jadav P, Bahekar R, Shah SR, Patel D, Joharapurkar A, Jain M, Sairam KV, Singh PK.

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1918-22. doi: 10.1016/j.bmcl.2014.03.009. Epub 2014 Mar 12.

PMID:
24675378
15.

Discovery of potent dipeptidyl peptidase IV inhibitors derived from β-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes.

Shan Z, Peng M, Fan H, Lu Q, Lu P, Zhao C, Chen Y.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1731-5. doi: 10.1016/j.bmcl.2011.01.086. Epub 2011 Jan 22.

PMID:
21334204
16.

Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes.

Kim HJ, Kwak WY, Min JP, Lee JY, Yoon TH, Kim HD, Shin CY, Kim MK, Choi SH, Kim HS, Yang EK, Cheong YH, Chae YN, Park KJ, Jang JM, Choi SJ, Son MH, Kim SH, Yoo M, Lee BJ.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3809-12. doi: 10.1016/j.bmcl.2011.04.029. Epub 2011 Apr 13.

PMID:
21570283
17.

Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.

Liu Y, Si M, Tang L, Shangguan S, Wu H, Li J, Wu P, Ma X, Liu T, Hu Y.

Bioorg Med Chem. 2013 Sep 15;21(18):5679-87. doi: 10.1016/j.bmc.2013.07.034. Epub 2013 Jul 25.

PMID:
23938053
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.
20.

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

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