1515-86-2Relevant articles and documents
The Effect of Phenyl Ring Torsional Rigidity on the Photophysical Behavior of Tetraphenylethylenes
Shultz, David A.,Fox, Marye Anne
, p. 6311 - 6320 (1989)
The synthesis and photochemical behavior of several members of the bismetacyclophanylidene series are presented.The properties of these compounds are compared to a model compound, tetra-3-tolylethylene.The photophysical properties of the tethered tet
SUBSTITUTED 2- AMIDOQUINAZOL-4-ONES AS MATRIX METALLOPROTEINASE-13 INHIBITORS
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Paragraph 1894-1896, (2015/12/23)
The present invention provides a novel amide derivative having a matrix metalloproteinase inhibitory activity, and useful as a pharmaceutical agent, which is a compound represented by the formula (I) wherein ring A is an optionally substituted, nitrogen containing heterocycle, ring B is an optionally substituted monocyclic homocycle or an optionally substituted monocyclic heterocycle, Z is N or NR1 (R1 is a hydrogen atom or an optionally substituted hydrocarbon group), is a single bond or a double bond, R2 is a hydrogen atom or an optionally substituted hydrocarbon group, X is an optionally substituted spacer having 1 to 6 atoms, ring C is (1) an optionally substituted homocycle or (2) an optionally substituted heterocycle other than a ring represented by (II) (X′ is S, O, SO, or CH2), and at least one of ring B and ring C has substituent(s), provided that N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]2 hydroxypropyl}5,6 dimethyl 4 oxo 1,4 dihydrothieno[2,3-d]pyrimidine-2-carboxamide is excluded, or a salt thereof.
N-(ARYLALKYL)-N'-PYRAZOLYL-UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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Paragraph 00616; 00650, (2014/06/11)
Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
NCO-chelated organoantimony(III) and organobismuth(III) dichlorides: Syntheses and structures
Vrana, Jan,Jambor, Roman,Ruzicka, Ales,Holecek, Jaroslav,Dostal, Libor
experimental part, p. 1041 - 1050 (2011/08/09)
The novel NCO chelating ligand L, 1-CH2N(CH3) 2-3-CH2OCH3-C6H4, was prepared in four steps from commercially available m-tolunitrile in a good yield. Successful lithiation of this ligand was achieved by the reaction with n-BuLi in hexane. Using of this in situ prepared organolithium compound LLi in the reactions with MCl3 (M = Sb, Bi) in 1:1 molar ratio led to isolation of the desired mono-organocompounds MLCl2 (M = Sb (1), Bi (2)). Their structures were studied both in solution (NMR) and in the solid state (X-ray diffraction), and were compared with those of the NCN- and OCO-chelating analogues.
1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents
Khanna, Ish K.,Weier, Richard M.,Yu, Yi,Xu, Xiang D.,Koszyk, Francis J.,Collins, Paul W.,Koboldt, Carol M.,Veenhuizen, Amy W.,Perkins, William E.,Casier, Jacquelen J.,Masferrer, Jaime L.,Zhang, Yan Y.,Gregory, Susan A.,Seibert, Karen,Isakson, Peter C.
, p. 1634 - 1647 (2007/10/03)
Series of 1,2-diarylimidazoles has been synthesized and found to contain highly potent and selective inhibitors of the human COX-2 enzyme. The paper describes a short synthesis of the target 1,2-diarylimidazoles starting with aryl nitriles. Different portions of the diarylimidazole (I) were modified to establish SAR. Systematic variations of the substituents in the aryl ring B have yielded very potent (IC50 = 10-100 nm) and selective (1000-12500) inhibitors of the COX-2 enzyme. The study on the influence of substituents in the imidazole ring established that a CF3 group at position 4 gives the optimum oral activity. A number of the diarylimidazoles showed excellent inhibition in the adjuvant induced arthritis model (e.g., ED50 = 0.02 mpk for 22 and 34). The diarylimidazoles are also potent inhibitors of carrageenan-induced edema (ED50 = 9-30 mpk) and hyperalgesia (ED50 = 11- 40 mpk). Several orally active diarylimidazoles show no GI toxicity in the rat and mouse up to 200 mpk.
Protonation Susceptibility and Fragmentation Capability of Functional Groups in Chemical Ionization Mass Spectrometry of Simple Bifunctional Compounds. Semi-quantitative Interpretation of Spectra.
Nakata, Hisao,Kadoguchi, Kenji,Konishi, Hideyuki,Takeda, Naohito,Tatematsu, Akira
, p. 67 - 70 (2007/10/02)
Positive-ion, methane-mediated chemical ionization mass spectra were measured for simple bifunctional aromatic compounds of the type m-XCH2C6H4CH2Y, where X = NH2 and N(CH3)2, and Y = OH and OCH3.Essentially only three peaks of ions, +, + and +, have appeared for each compound.Since the two functional groups XCH2- and YCH2- do not interact with each other after protonation or after fragmentation, they are assumed to be protonated and to undergo fragmentation independently.The relative protonation susceptibility and fraction of fragmentating + can be estimated for each functional group in these compounds.A semi-quantitative interpretation of the observed spectra is presented.
THE EFFECT OF ARYL SUBSTITUENTS ON ARYLCARBENE REACTIVITY
Tomioka, Hideo,Tabayashi, Kazuo,Ozaki, Yasuji,Izawa, Yasuji
, p. 1435 - 1440 (2007/10/02)
Substituted (p-MeO, p-Me, H, p-Cl, p-Br, m-Br, m-MeO, 3,4-Cl2, p-CO2Me, m-CN and p-CN) monophenylcarbenes are generated in a binary mixture of substrates (methanol, cis-4-methyl-2-pentene and cyclohexane) and the relative rate of O - H insertion into methanol to stereospecific cyclopropanation of the olefin to C - H insertion into cyclohexane are calculated from the ratios of products and substrates.It is found (i) that the reactivities of the substrates decrease in the order of methanol, olefin and cyclohexane and (ii) that electron-donating substituents generally lead to reaction with the more reactive substrates while the reaction with the less reactive substrates is favoured in the case of electron-withdrawing substituents.These results are interpreted in terms of the change in the electrophilicity of the singlet arylcarbene by the substituents rather than the change in the singlet-triplet equilibrium.
