557798-56-8Relevant academic research and scientific papers
PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
-
Paragraph 0347; 0350-0351, (2020/02/16)
Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists
Suzuki, Takao,Moriya, Minoru,Sakamoto, Toshihiro,Suga, Takuya,Kishino, Hiroyuki,Takahashi, Hidekazu,Ishikawa, Makoto,Nagai, Keita,Imai, Yumiko,Sekino, Etsuko,Ito, Masahiko,Iwaasa, Hisashi,Ishihara, Akane,Tokita, Shigeru,Kanatani, Akio,Sato, Nagaaki,Fukami, Takehiro
scheme or table, p. 3072 - 3077 (2010/02/28)
Optimization of high-throughput screening hit 1a led to the identification of a novel spiro-piperidine class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Compound 3c was identified as a highly potent and selective MCH-1R antagonist, which has an IC50 value of 0.09 nM at hMCH-1R. The synthesis and structure-activity relationships of the novel spiro-piperidine MCH-1R antagonists are described.
Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R)
Ito, Masahiko,Sakamoto, Toshihiro,Suzuki, Takao,Egashira, Shinichiro,Moriya, Minoru,Ishihara, Akane,Iwaasa, Hisashi,Matsushita, Hiroko,Nakase, Kazuho,Wallace, Michael A.,Dean, Dennis,Sato, Nagaaki,Tokita, Shigeru,Kanatani, Akio
scheme or table, p. 2835 - 2839 (2010/03/31)
We have developed and characterized [35S]4a as a potent and selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R). Compound [35S]4a showed appreciable specific signals in brain slices prepared from wild-type mice
HETEROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CARDIOVASCULAR DISEASE
-
Page/Page column 234-235, (2008/06/13)
Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as defined herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.
MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISTS CONTAINING PIPERIDINE DERIVATIVES AS THE ACTIVE INGREDIENT
-
Page/Page column 29, (2010/02/14)
The invention provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: ???[wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for -O-, -CH2-, or the like; Y1, Y2, Y3 and Y4 stand for -CH-, -CF-, -N-, or the like; Z stands for lower alkyl, an aliphatic heterocyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin-concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.
