925922-62-9Relevant academic research and scientific papers
FUSED RING COMPOUND HAVING UREA STRUCTURE
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Page/Page column 238, (2020/01/31)
The present invention relates to a novel fused ring compound having urea structure that exhibits excellent NAMPT activating effect, and a method using the same for treating / preventing metabolic disorder, cardiovascular and kidney disease, mitochondrial disease, neurodegenerative disease, ocular disease, and muscle wasting disorder. The present invention provides a compound represented by following formula (I) or a pharmacologically acceptable salt: Formula (I) wherein A, B, R, R2 and R3 represent the same meanings as in the claims.
Synthesis and structure-activity relationships of 2-acylamino-4,6-diphenylpyridine derivatives as novel antagonists of GPR54
Kobayashi, Toshitake,Sasaki, Satoshi,Tomita, Naoki,Fukui, Seiji,Kuroda, Noritaka,Nakayama, Masaharu,Kiba, Atsushi,Takatsu, Yoshihiro,Ohtaki, Tetsuya,Itoh, Fumio,Baba, Atsuo
experimental part, p. 3841 - 3859 (2010/08/06)
GPR54 is a G protein-coupled receptor (GPCR) which was formerly an orphan receptor. Recent functional study of GPR54 revealed that the receptor has an essential role to modulate sex-hormones including GnRH. Though antagonists of GPR54 are expected to be novel drugs for sex-hormone dependent diseases such as prostate cancer or endometriosis, small molecule GPR54 antagonists have not been reported. We have synthesized a series of 2-acylamino-4,6-diphenylpyridines to identify potent GPR54 antagonists. Detailed structure-activity relationship studies led to compound 9l with an IC50 value of 3.7 nM in a GPR54 binding assay, and apparent antagonistic activity in a cellular functional assay.
PYRIDYLPHENOL COMPOUND AND USE THEREOF
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Page/Page column 70-71, (2008/12/05)
The present invention provides a compound which has metastin receptor antagonist activity and is useful for preventing and treating hormone-dependent cancer, benign prostatomegaly, endometriosis, precocious puberty, uterine myoma or the like. More specifically, the present invention provides a compound, represented by the formula: or a salt thereof, a prodrug thereof, and a pharmaceutical agent containing the same; wherein Ring A represents a 5- to 8-membered homocyclic or heterocyclic group optionally having a substituent other than formula -X-R1 wherein X represents a bond or a spacer, and R1 represents optionally substituted amino or an optionally substituted nitrogen-containing heterocyclic group; Ring B represents an optionally substituted benzene ring; R2 represents an optionally substituted homocyclic or heterocyclic group; and R3 and R4 independently represent a hydrogen atom, cyano, acyl or an optionally substituted hydrocarbon group.
