66773-34-0Relevant academic research and scientific papers
Biased agonist and medical application thereof
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Paragraph 0278-0282, (2021/01/24)
The invention relates to compounds shown in structural formulas I and II, stereoisomers or pharmaceutically acceptable salts thereof, and a pharmaceutical composition containing the compounds, the stereoisomers or the pharmaceutically acceptable salts thereof as active ingredients, and uses of the compound, the stereoisomer thereof or the pharmaceutically acceptable salt thereof in preparation ofanalgesic drugs.
Discovery of Biased Mu-Opioid Receptor Agonists for the Treatment of Pain
Ma, Mengjun,Li, Xiang,Tong, Kun,Cheng, Jingchao,Yu, Zixing,Ren, Fengxia,Zhong, Bohua,Shi, Weiguo
, p. 155 - 161 (2019/12/15)
G protein-biased mu-opioid receptor (MOR) agonists have been developed as promising new potent analgesic drugs with fewer adverse side effects than standard MOR agonists. PZM21 represents a unique chemotype unrelated to known opioids, which makes it a desirable lead for modification to find analgesics with new chemical entities. In the present study, we synthesized and tested novel PZM21 derivatives as potent biased MOR agonists by introducing a benzodioxolane group to replace the hydroxybenzene of PZM21. The new compounds displayed more potent analgesic activities in vivo and greater bias toward G protein signaling in vitro than did PZM21. These results suggest that the benzodioxolane group is essential for the maintenance of bias. Compounds 7 i ((S)-1-(3-(benzo[d][1,3]dioxol-4-yl)-2-(dimethylamino)propyl)-3-phenethylurea) and 7 j ((S)-1-(3-(benzo[d][1,3]dioxol-4-yl)-2-(dimethylamino)propyl)-3-benzylurea) could serve as new leads for further modifications to find novel biased MOR agonists with greater G protein signaling potency and less β-arrestin-2 recruitment.
Semiconductor device
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, (2007/10/16)
Provided is a DAD that improves resistance to latch-up and stabilizes breakdown voltage characteristic. Specifically, a first gate electrode (10) and a second drain electrode (13) are linear electrodes having a length not exceeding the length of a source electrode (9). An isolation region (20) is disposed on both end portions of these electrodes. The region surrounded by two isolation regions (20) and the source electrode (9) becomes a P channel MOS region (PR) where a P channel MOS transistor is to be formed. The isolation region (20) has a multi-trench structure that a plurality of trenches (21) are provided in a P type impurity region disposed so as to be rectangle as viewed in plan configuration. Each trench (21) is filled with a conductor such as polysilicon, and the filled conductor is disposed so that it makes no electrical contact with any specific part.
Copper(II) reagent-promoted degradation of N,N′-dialkyldiazenedicarboxamides
Yamaguchi, Jun-Ichi,Murayama, Yukihito,Suyama, Takayuki
, p. 329 - 333 (2007/10/03)
Degradation of N,N′-dialkyldiazenedicarboxamides with a copper(II) reagent, which was prepared from lithium 4-nitrophenoxide and copper(II) bromide in tetrahydrofuran, proceeded via formation of isocyanate to produce the corresponding 4-nitrophenyl N-alky
Multilevel selectivity in the mild and high-yielding chlorosilane- induced cleavage of carbamates to isocyanates
Chong, Pek Y.,Janicki, Slawomir Z.,Petillo, Peter A.
, p. 8515 - 8521 (2007/10/03)
The silane-induced cleavage of a series of N-p-tolylcarbamates and N- phenethylcarbamates to isocyanates has been investigated as a function of chlorosilane, carbamate substituent, and reaction conditions. Reaction yields were determined from the isolated ureas, which were formed by trapping the corresponding isocyanates with isobutylamine. Under room-temperature conditions, multilevel selectivity in carbamate activation has been demonstrated. This selectivity together with the generality of the methodology enhances the utility of carbamates as synthetic intermediates and protecting groups. To demonstrate the effectiveness of this selectivity, a series of biscarbamates were selectively monoactivated to isocyanates in excellent yields.
