180150-74-7Relevant academic research and scientific papers
Cu(I)/chiral bisoxazoline-catalyzed enantioselective sommelet-hauser rearrangement of sulfonium ylides
Wang, Jianbo,Li, Shu-Sen
supporting information, p. 12343 - 12358 (2020/11/10)
Catalytic asymmetric thia-Sommelet-Hauser rearrangement of sulfonium ylides remains a great challenge due to its multistep reaction mechanism involving metal carbene formation, proton transfer, and [2,3]-sigmatropic rearrangement. In particular, the key problem of such reactions is the differentiation of the enantiotopic lone pair electrons of sulfur, which generates the sulfonium ylide intermediate bearing chirality on the sulfur atom. With a modified chiral bisoxazoline ligand, we developed a Cu(I)- catalyzed asymmetric thia-Sommelet-Hauser rearrangement with good to excellent enantioselectivities. Mechanistic studies provide insights into the details of the reaction mechanism.
SYMMETRICAL TRIS-ARYL-AMIDE DERIVATIVES AND THEIR USE AS ANTI-HEPARANASE
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Paragraph 0311; 0314, (2018/10/15)
The present invention relates to tris-aryl-amide derivatives having an anti-heparanase activity, in particular it relates to ureido/thioureido/ether tris-aryl-amide derivatives of formula The invention also relates to the use of such compounds as a medica
COMPOUND, CURED PRODUCT, POLYMER, PHOTO-ALIGNMENT FILM, OPTICALLY ANISOTROPIC BODY AND LIQUID CRYSTAL DISPLAY ELEMENT
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, (2018/08/30)
A compound and a polymer which can each form a photo-alignment film having excellent ability of controlling alignment, a photo-alignment film obtained using the polymer and an optically anisotropic body and a liquid crystal display element each having the photo-alignment film are provided. A compound represented by the general formula (1). In the formula, P represents a polymerizable group, Z and Z1 represent divalent linking groups, A and A1 represent divalent cyclic groups, and X1 to X5 each independently represent a hydrogen atom, a fluorine atom, a chlorine atom, a hydroxy group, a nitro group, a cyano group or an alkyl group having 1 to 40 carbon atoms which may have a substituent, provided that X1, X2, X4 and X5 are not simultaneously hydrogen atoms.
A photoinducible β-hairpin
Aemissegger, Andreas,Kraeutler, Vincent,Van Gunsteren, Wilfred F.,Hilvert, Donald
, p. 2929 - 2936 (2007/10/03)
A photochromic azobenzene linker was incorporated as a turn element into an amino acid sequence known to fold into a β-hairpin structure in aqueous solution. Oligomer formation when the linker was in its thermodynamically favored trans form prohibited str
1,5-benzodiazepine derivatives
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Referential example 2, (2010/01/30)
This invention relates to 1,5-benzodiazepine derivatives, which are each represented by the following formula (1): wherein R1represents a lower alkyl group, R2and R3may be the same or different and represent a hydrogen atom or a lower alkyl group, R4represents a cyclohexyl group or phenyl group, and n stands for an integer of from 1 to 3, and also to medicines containing the same. These compounds are useful as curatives or preventives for diseases in which a gastrin receptor and/or a CCK-B receptor takes part.
Aminophenol derivatives
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, (2008/06/13)
Aminophenol derivatives represented by the following formula (1): STR1 wherein X is O or S; A is alkylene, R 1 is phenyl, etc., R 2 and R 3 are H or alkyl; R 4 is substituted carbamoylalkyl, etc.; R 5 is substituted amino, etc.; their salts, and optical i
N-phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: Structure-activity studies and demonstration of in vivo activity
Collins, Jon L.,Shearer, Barry G.,Oplinger, Jeffrey A.,Lee, Shuliang,Garvey, Edward P.,Salter, Mark,Duffy, Claire,Burnette, Thimysta C.,Furfine, Eric S.
, p. 2858 - 2871 (2007/10/03)
Selective inhibition of the neuronal isoform of nitric oxide synthase (NOS) compared to the endothelial and inducible isoforms may be required for treatment of neurological disorders caused by excessive production of nitric oxide. Recently, we described N-(3-(aminomethyl)benzyl)acetamidine (13) as a slow, tight-binding inhibitor, highly selective for human inducible nitric oxide synthase (iNOS). Removal of a single methylene bridge between the amidine nitrogen and phenyl ring to give N-(3- (aminomethyl)phenyl)acetamidine (14) dramatically altered the selectivity to give a neuronal selective nitric oxide synthase (nNOS) inhibitor. Part of this large shift in selectivity was due to 14 being a rapidly reversible inhibitor of iNOS in contrast to the essentially irreversible inhibition of iNOS observed with 13. Structure-activity studies revealed that a basic amine functionality tethered to an aromatic ring and a sterically compact amidine are key pharmacophores for this class of NOS inhibitors. Maximal nNOS inhibition potency was achieved with N-(3-(aminomethyl)phenyl)-2- furanylamidine (77) (K(i-nNOS) = 0.006 μM; K(i-eNOS) = 0.35 μM; K(i-iNOS) = 0.16 μM). Finally, α-fluoro-N-(3-(aminomethyl)phenyl)acetamidine (74) (K(i- nNOS) = 0.011 μM; K(i-eNOS) = 1.1 μM; K(i-iNOS) = 0.48 μM) had excellent brain penetration and inhibited nNOS in a rat brain slice assay as well as in the rat brain (cerebellum) in vivo. Thus, N-phenylamidines should be useful in validating the role of nNOS in neurological disorders.
