149428-76-2Relevant academic research and scientific papers
NOVEL COMPOUND AND PHARMACETICAL COMPOSITION FOR PREVENTING OR TREATING OBESITY OR METABOLIC SYNDROME COMPRISING THEREOF
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Paragraph 0102-0104, (2021/01/29)
The present invention provides a compound represented by the following Chemical Formula 1 or a pharmaceutically acceptable salt thereof which can be effectively used for preventing or treating obesity or metabolic syndrome, and a pharmaceutical compositio
NOVEL AUTOPHAGY-TARGETING CHIMERA (AUTOTAC) COMPOUND, AND COMPOSITION FOR PREVENTING, ALLEVIATING, OR TREATING DISEASES THROUGH TARGET PROTEIN DEGRADATION COMPRISING SAME
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Paragraph 0147-0148, (2021/06/03)
The present invention relates to a novel AUTOTAC chimeric compound in which a new p62 ligand and a target-binding ligand are connected by a linker, a stereoisomer, hydrate, solvate or prodrug thereof, and a pharmaceutical or food composition for the prevention or treatment of diseases by degrading the target protein including the same as an active ingredient. They can target specific proteins to adjust their concentrations, and can also deliver drugs and other small molecule compounds to lysosomes. The AUTOTAC chimeric compound according to the present invention can be usefully used as a pharmaceutical composition for the prevention, amelioration or treatment of various diseases by selectively eliminating specific proteins.
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine σ ligands as potential antipsychotic drugs
Nakazato, Atsuro,Ohta, Kohmei,Sekiguchi, Yoshinori,Okuyama, Shigeru,Chaki, Shigeyuki,Kawashima, Yutaka,Hatayama, Katsuo
, p. 1076 - 1087 (2007/10/03)
Receptor antagonists may be effective antipsychotic drugs that do not induce motor side effects caused by ingestion of classical drugs such as haloperidol. We obtained evidence that 1-(2-dipropylaminoethyl)-4-methoxy- 6H-dibenzo[b,d]pyran hydrochloride 2a had selective affinity for σ receptor over dopamine D2 receptor. This compound was designed to eliminate two bonds of apomorphine 1 to produce structural flexibility for the nitrogen atom and to bridge two benzene rings with a -CH2O- bond to maintain the planar structure. In light of the evidence, N,Y-dipropyl-2-(4-methoxy-3- benzyloxylphenyl)ethylamine hydrochloride 10b was designed. Since compound 10b had eliminated a biphenyl bond of 6H-dibenzo[b,d]pyran derivative 2a, it might be more released from the rigid structure of apomorphine 1 than compound 2a. The chemical modification of compound 10b led to the discovery that N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxyl)phenyl]ethylamine hydrochloride 10g (NE- 100), the best compound among arylalkoxyphenylalkylamine derivatives 3, had a high and selective affinity for σ receptor and had a potent activity in an animal model when the drug was given orally. We report here the design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine derivatives 3.
Alkoxyphenylalkylamine derivatives
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, (2008/06/13)
An alkoxyphenylalkylamine derivative represented by the following formula: STR1 (wherein X1 and X2 may be either the same or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy g
