167263-16-3Relevant academic research and scientific papers
Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists
Cho, Kaimei,Ando, Makoto,Kobayashi, Kensuke,Miyazoe, Hiroshi,Tsujino, Toshiaki,Ito, Sayaka,Suzuki, Tomoki,Tanaka, Takeshi,Tokita, Shigeru,Sato, Nagaaki
scheme or table, p. 4781 - 4785 (2010/07/06)
A novel series of cyclohexanamine derivatives was designed and synthesized as potent and selective human neuropeptide Y Y1 receptor antagonists. Modification of high-throughput screening hit compound 1 resulted in the identification of compound 3i, which displays potent Y1 activity and good selectivity towards hERG K+ channel and serotonin transporter.
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: Synthesis, SAR, and in vivo assessment
Luci, Diane K.,Ghosh, Shyamali,Smith, Charles E.,Qi, Jenson,Wang, Yuanping,Haertlein, Barbara,Parry, Tom J.,Li, Jian,Almond Jr., Harold R.,Minor, Lisa K.,Damiano, Bruce P.,Kinney, William A.,Maryanoff, Bruce E.,Lawson, Edward C.
, p. 6489 - 6492 (2008/03/13)
Various 4-phenylpiperidine-benzoxazin-3-ones were synthesized and biologically evaluated as urotensin-II (U-II) receptor antagonists. Compound 12i was identified from in vitro evaluation as a low nanomolar antagonist against both rat and human U-II receptors. This compound showed in vivo efficacy in reversing the ear-flush response induced by U-II in rats.
4,4-Disubstitued piperidines, and methods of use thereof
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, (2008/06/13)
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The comp
SUBSTITUTED PYRROLIDIN-3-YL-ALKYL-PIPERIDINES
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, (2008/06/13)
The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
