336882-80-5Relevant academic research and scientific papers
SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
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Page/Page column 135, (2011/05/05)
The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
New μ-opioid receptor agonists with phenoxyacetic acid moiety
Sato, Susumu,Komoto, Teruo,Kanamaru, Yoshihiko,Kawamoto, Noriyuki,Okada, Tomomi,Kaiho, Terumitsu,Mogi, Kinichi,Morimoto, Shinichi,Umehara, Norimitsu,Koda, Tadayuki,Miyashita, Akira,Sakamoto, Takao,Niino, Yasuhiro,Oka, Tetsuo
, p. 292 - 297 (2007/10/03)
New μ-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Among the synthesized compounds, [2-[1-[3-(N,N-dimethylcarbamoyl)-3,3-diphenylpropyl]-4-hydroxypiperidin-4-yl] phenoxy]acetic acid (8: SS620) having phenoxyacetic acid and 4-hydroxypiperidine moieties showed the highest agonist potency on the MOR in an isolated guinea-pig ileum preparation, and it also had selectivity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells compared with the same types of δ- and κ-opioid receptors (DOR and KOR). In addition, compound 8 showed a 10 times more potent MOR agonist activity than loperamide. Furthermore, compound 8 showed a peripheral analgesic activity in vivo screening on rat.
4-hydroxy-4-phenylpiperidine derivatives and pharmaceuticals containing the same
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Referential example 3, (2010/01/31)
Described is a 4-hydroxy-4-phenylpiperidine derivative represented by the following formula (1): [wherein, R1and R2are the same or different and each independently represents a hydrogen atom, a lower alkyl, or the like, R3represents a hydrogen atom or a group —(CR4R5)n—Y (in which, R4and R5each represents a hydrogen atom or a lower alkyl group, Y represents a group —COOR6, —CONR7R8, —OR9or —OCOR10(in which R6, R9and R10each independently represents a hydrogen atom, a lower alkyl group, or the like, R7and R8are the same or different and each independently represents a hydrogen atom, a lower alkyl group, or the like), and n stands for 1 to 6)], or salt thereof. The compound exhibits excellent peripheral analgesic action.
