737765-19-4Relevant academic research and scientific papers
An aminomethylpyrimidine DPP-IV inhibitor with improved properties
Peters, Jens-Uwe,Hunziker, Daniel,Fischer, Holger,Kansy, Manfred,Weber, Silja,Kritter, Stephane,Mueller, Aranka,Wallier, Angelina,Ricklin, Fabienne,Boehringer, Markus,Poli, Sonia Maria,Csato, Miklos,Loeffler, Bernd-Michael
, p. 3575 - 3578 (2007/10/03)
A recently identified DPP-IV inhibitor (1) was found to induce phospholipidosis and to inhibit CYP3A4. A small series of less lipophilic and less amphiphilic analogues was synthesized in an effort to overcome these issues. One compound from this series was equipotent to 1, did not induce phospholipidosis and showed a reduced CYP3A4 inhibition.
Lead generation: Sowing the seeds for future success
Bleicher, Konrad H.,Nettekoven, Matthias,Peters, Jens-Uwe,Wyler, Rene
, p. 588 - 600 (2007/10/03)
Lead generation and the associated hit-to-lead process are key strategic elements in modern pharmaceutical research, and most companies have implemented this concept. Efficient lead generation is one of the main attempts to reduce the high attrition rates observed along the drug discovery process by focussing on the early developmental phases. The level of integration of the lead generation activities within the discovery organization, the flexibility in assessing and implementing new chemistries and new technologies, the high-quality standards set for the identification of the best possible chemical lead series will ultimately determine the future success in discovering new medicines.
