✦ LIBER ✦

Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore

✍ Scribed by Yukihiro Nishio; Hidenori Kimura; Shinya Tosaki; Eiji Sugaru; Mutsuko Sakai; Masakuni Horiguchi; Yumi Masui; Michiko Ono; Tsutomu Nakagawa; Hiroyuki Nakahira

Book ID: 104005053
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 607 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.10.101

No coin nor oath required. For personal study only.

✦ Synopsis

Structures containing the (R)-3-amino-3-methyl piperidine unit as a new pharmacophore moiety have been shown to possess moderate inhibitory activity for DPP-4 with good pharmacokinetics profile. One of these compounds was found to have good oral bioavailability and PK/PD profile in ZF-rat.

📜 SIMILAR VOLUMES

(R)-8-(3-Amino-piperidin-1-yl)-7-but-2-y

(R)-8-(3-Amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a Novel Xanthine-Based Dipeptidyl Peptidase 4 Inhibitor, Has a Superior Potency and Longer Duration of Action Compared with Other Dipeptidyl Peptidase-4 Inhibitors

✍ Thomas, L.; Eckhardt, M.; Langkopf, E.; Tadayyon, M.; Himmelsbach, F.; Mark, M. 📂 Article 📅 2008 🏛 American Society for Pharmacology and Experimental 🌐 English ⚖ 644 KB

(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorop

(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl] -3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a Selective Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes.

✍ Tesfaye Biftu; et al. et al. 📂 Article 📅 2007 🏛 John Wiley and Sons ⚖ 13 KB 👁 1 views

2-({6-[(3R)-3-amino-3-methylpiperidine-1

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

✍ Yukihiro Nishio; Hidenori Kimura; Naoyuki Sawada; Eiji Sugaru; Masakuni Horiguch 📂 Article 📅 2011 🏛 Elsevier Science 🌐 English ⚖ 509 KB

Discovery of ((4 R ,5 S )-5-Amino-4-(2,4

Discovery of ((4 R ,5 S )-5-Amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8 H )-yl)methanone (ABT-341), a Highly Potent, Selective, Orally Efficacious, and Safe Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

✍ Pei, Zhonghua; Li, Xiaofeng; von Geldern, Thomas W.; Madar, David J.; Longenecke 📂 Article 📅 2006 🏛 American Chemical Society 🌐 English ⚖ 190 KB

Piperazine-Based CCR5 Antagonists as HIV

Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-{2-methoxy-1( R )-4-(trifluoromethyl)phenyl}ethyl-3( S )-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist

✍ Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao 📂 Article 📅 2004 🏛 American Chemical Society 🌐 English ⚖ 78 KB