615251-46-2Relevant academic research and scientific papers
Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate
Washburn, William N.,Manfredi, Mark,Devasthale, Pratik,Zhao, Guohua,Ahmad, Saleem,Hernandez, Andres,Robl, Jeffrey A.,Wang, Wei,Mignone, James,Wang, Zhenghua,Ngu, Khehyong,Pelleymounter, Mary Ann,Longhi, Daniel,Zhao, Rulin,Wang, Bei,Huang, Ning,Flynn, Neil,Azzara, Anthony V.,Barrish, Joel C.,Rohrbach, Kenneth,Devenny, James J.,Rooney, Suzanne,Thomas, Michael,Glick, Susan,Godonis, Helen E.,Harvey, Susan J.,Cullen, Mary Jane,Zhang, Hongwei,Caporuscio, Christian,Stetsko, Paul,Grubb, Mary,Maxwell, Brad D.,Yang, Hong,Apedo, Atsu,Gemzik, Brian,Janovitz, Evan B.,Huang, Christine,Zhang, Lisa,Freeden, Chris,Murphy, Brian J.
, p. 7509 - 7522 (2015/01/09)
Identification of MCHR1 antagonists with a preclinical safety profile to support clinical evaluation as antiobesity agents has been a challenge. Our finding that a basic moiety is not required for MCHR1 antagonists to achieve high affinity allowed us to explore structures less prone to off-target activities such as hERG inhibition. We report the SAR evolution of hydroxylated thienopyrimidinone ethers culminating in the identification of 27 (BMS-819881), which entered obesity clinical trials as the phosphate ester prodrug 35 (BMS-830216).
Enantioselective synthesis of iclaprim enantiomers- A versatile approach to 2-substituted chiral chromenes
Tahtaoui, Chouaib,Demailly, Arnold,Guidemann, Carole,Joyeux, Cecile,Schneider, Peter
supporting information; experimental part, p. 3781 - 3785 (2010/09/03)
Figure presented Both enantiomers of the DHFR inhibitor iclaprim (R)-1 and (S)-1 were synthesized from the cyclopropyl homoallyl alcohols (R)-6 and (S)-6, respectively. As key steps these transformations include a Mitsunobu reaction and the formation of the diaminopyrimidine unit prior to a novel cyclization procedure to obtain the desired chromene heterocycle. The moderate enantioselectivity of the products (R)-1 and (S)-1 is related to the Mitsunobu reaction, which unfortunately did not proceed with complete inversion of configuration.
PREPARATION OF 24 ALKYL ANALOGS OF CHOLECALCIFEROL AND NON-RACEMIC COMPOUNDS
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Example 3, (2010/02/07)
Disclosed is a process for the preparation of 24 -alkyl analogs of cholecalcyferol of Formula 1 having a (5E) or (5Z) configuration, wherein X represents a hydrogen atom, a hydroxy group or an OR1 group, wherein R1, R2
