- NCO-chelated organoantimony(III) and organobismuth(III) dichlorides: Syntheses and structures
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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.
- Vrana, Jan,Jambor, Roman,Ruzicka, Ales,Holecek, Jaroslav,Dostal, Libor
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- SUBSTITUTED 2- AMIDOQUINAZOL-4-ONES AS MATRIX METALLOPROTEINASE-13 INHIBITORS
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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.
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Paragraph 1897-1899
(2015/12/23)
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- COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
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The present invention provides novel beta-secretase inhibitors of the general formula (I), where the variables A1, A2, L1, L2, L3, R1, R2, R3, R4, R5, R6 and R7 are as defined in the claims, a method for their use in treating Alzheimer's disease, and methods for their use in reducing memapsin 2 catalytic activity.
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Page/Page column 54-55
(2008/06/13)
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- Protonation Susceptibility and Fragmentation Capability of Functional Groups in Chemical Ionization Mass Spectrometry of Simple Bifunctional Compounds. Semi-quantitative Interpretation of Spectra.
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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.
- Nakata, Hisao,Kadoguchi, Kenji,Konishi, Hideyuki,Takeda, Naohito,Tatematsu, Akira
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