2509-18-4Relevant academic research and scientific papers
Discovery of orally available spirodiketopiperazine-based CCR5 antagonists
Nishizawa, Rena,Nishiyama, Toshihiko,Hisaichi, Katsuya,Hirai, Keisuke,Habashita, Hiromu,Takaoka, Yoshikazu,Tada, Hideaki,Sagawa, Kenji,Shibayama, Shiro,Maeda, Kenji,Mitsuya, Hiroaki,Nakai, Hisao,Fukushima, Daikichi,Toda, Masaaki
experimental part, p. 5208 - 5223 (2010/09/18)
Using the previously reported novel spirodiketopiperazine scaffold, the design and synthesis of orally available CCR5 antagonists was undertaken. Compounds possessing a carboxylic acid function in the appropriate position showed improved oral exposure (AU
PYRROLIDINE DERIVATIVE OR SALT THEREOF
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Page/Page column 46-47, (2008/06/13)
[PROBLEMS] To provide a compound which can be used for the treatment of a disease associated with a calcium-sensing receptor (CaSR), particularly hyperparathyroidism. [MEANS FOR SOLVING PROBLEMS] It is found that a novel pyrrolidine derivative having an aminomethyl group substituted by an arylaklyl group or the like or a salt thereof has an excellent CaSR agonistic modulation effect and also has an excellent selectivity in the inhibition of CYP2D6 which may cause a drug-drug interaction. Thus, the novel pyrrolidine derivative is useful as a therapeutic agent for a disease associated with CaSR (e.g., hyperparathyroidism, renal osteodystrophy and hypercalcemia).
