- A NOVEL SYNTHESIS OF ROYAL JELLY ACIDS AND QUEEN SUBSTANCE BY THE FIVE CARBON HOMOLOGATION USING β-VINYL-β-PROPIOLACTONE
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10-Hydroxy-(E)-2-decenoic acid, (E)-2-decenedioic acid (Royal jelly acids), and 9-oxo-(E)-2-decenoic acid (queen substance) were synthesized via 10-hydroxy-3-decenoic acid and 9,9-ethylenedioxy-3-decenoic acid, respectively, prepared easily by the regioselective ring-opening reaction of β-vinyl-β-propiolactone with Grignard reagents in the presence of copper(I) catalyst.
- Fujisawa, Tamotsu,Sato, Toshio,Itoh, Toshiyuki
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Read Online
- Synthesis of two novel oxocyclam-binding technetium complexes containing an analogue of cocaine
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In order to visualize and quantify dopamine transporters, the synthesis of two novel ligands labelled with technetium-99m (99mTc) has been investigated. A multi-step synthesis afforded two target ligands with a tropane skeleton and a macrocycli
- Turpin,Masri,Rich,Berthommier,Emond,Vidal,Auzeloux,Loc'H,Neuquelman,Mauclaire
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- Nitroimidazoles and hypoxia imaging: Synthesis of three Technetium-99m complexes bearing a nitroimidazole group: Biological results
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Several Tc-99m complexes were synthesized, substituted with a nitroimidazole group, in order to visualize hypoxic tissues. The complexes were tested on rats (isolated hearts) and showed no significant uptake under hypoxic conditions. (C) 2000 Elsevier Science Ltd.
- Riche, Francoise,Du Moulinet d'Hardemare, Amaury,Sepe, Sandrine,Riou, Laurent,Fagret, Daniel,Vidal, Michel
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- New and simple syntheses of the attractants of the female melon fly, dacus cucurbitee
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The attractant of the female melon fly, (E)-6-nonenyl acetate, and the two analogs, (E)-7-dodecenyl acetate and (E)-7-decenyl acetate were synthesized via hydrozirconation to control the regioselective coupling reactions and resulted in good yields.
- Yen, Yao-Pin,Chen, Pao-Hsing
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Read Online
- POLYMERIZABLE COMPOUND AND OPTICAL ANISOTROPIC BODY
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To provide a polymerizable compound giving such properties when added to a solution comprising a polymerizable composition that the resultant polymerizable composition has high storage stability and can induce a liquid crystal phase alignment in a short t
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Paragraph 0160-0161; 0169
(2021/02/19)
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- PROTEOLYSIS-TARGETING PROTACS INDUCING DEGRADATION OF C-MIC PROTEIN
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Disclosed are proteolysis-targeting chimeric molecules (PROTACs) that induce degradation of c-MYC protein. The disclosed PROTACs typically include a first targeting moiety that binds to c-MYC (MC-MYC) which may be derived from a substituted heterocycle that binds to c-MYC such as a substituted pyrazole. The first targeting moiety typically is linked via a bond or a linker (L) to a second targeting moiety that binds to an E3 ubiquitin ligase (ME3). AS such, the disclosed PROTACS may be described as having a formula Mc-MYC-L-ME3 or ME3-L-Mc-MYC.
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Paragraph 00251-00252; 00256-00258; 00359; 00362
(2020/12/30)
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- POLYMERIZABLE COMPOUND AND OPTICAL ISOMER
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The present invention provides a polymerizable compound having high storage stability without causing crystal precipitation when added to a polymerizable composition. The present invention also provides a polymerizable composition containing the compound. When the filmy polymer produced through polymerization of the polymerizable composition is irradiated with UV light, it hardly discolors or peels from substrate. Further, the present invention provides a polymer produced through polymerization of the polymerizable composition and an optically anisotropic body using the polymer.
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Paragraph 0221
(2018/04/02)
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- A BISPHENOL DERIVATIVE HAVING AN ESTER BOND
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PROBLEM TO BE SOLVED: To provide a production intermediate useful for obtaining a compound having an ester bond, and a production method to obtain a compound having an ester bond, using the same, with convenience and high purity; specifically, to provide a bisphenol derivative having an ester bond, a method for producing the same, and a compound produced from the bisphenol derivative as an intermediate; and to further provide a polymer obtained by the polymerization of a polymerizable composition containing the compound produced from the bisphenol derivative as an intermediate, and an optical anisotropic body using the polymer. SOLUTION: A bisphenol derivative having an ester bond is represented by general formula (I-C), where at least one of A1 and A2 is substituted with one substituent L. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
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Paragraph 0292-0293; 0297
(2018/06/13)
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- Donepezil–melatonin hybrids as butyrylcholinesterase inhibitors: Improving binding affinity through varying mode of linking fragments
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Hybrid inhibitors of acetyl- and butyrylcholinesterase are compounds that combine structural motifs of two different classical inhibitors, leading to a dual binding ligand. A rapidly growing collection of those compounds involves a wide diversity of structural motifs, but the way of linking two active fragments and its impact on the affinity toward cholinesterases usually remains beyond the extent of investigation. We present hereby a detailed analysis of this aspect using melatonin–donepezil hybrids. A new series of compounds, in which two fragments are connected using a carbamate linker, exhibits excellent activity and selectivity toward butyrylcholinesterase.
- ?ozińska, Iwona,?wierczyńska, Aleksandra,Mol?da, Zuzanna,Hartman, Alwin M.,Hirsch, Anna K. H.,Czarnocki, Zbigniew
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- POLYMERIZABLE COMPOUND AND OPTICALLY ANISOTROPIC BODY
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The present invention provides a compound represented by the general formula (I), and a polymerizable composition containing the compound. When the polymerizable composition containing the compound represented by the formula (I) is used to form a filmy product, the resulting filmy product exhibits less change over time in phase difference and reverse wavelength dispersion and when the filmy polymer is irradiated with UV light, peeling from a substrate is unlikely to be caused. Further, the invention provides a polymer obtained through polymerization of the polymerizable composition and an optically anisotropic body obtained using the polymer.
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Paragraph 0193; 0196
(2018/11/21)
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- POLYMERIZABLE COMPOUND AND OPTICALLY ANISOTROPIC BODY
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There is provided a polymerizable composition, by which discoloration or alignment defects are less likely to occur when a filmy polymer, which is obtained by adding a polymerizable compound to the polymerizable composition and polymerizing this composition, is irradiated with ultraviolet light. There are also provided a polymer obtained by polymerizing the polymerizable composition, and an optically anisotropic body using the polymer. The present invention provides a polymerizable low-wavelength dispersive or polymerizable reverse-wavelength dispersive compound having a partial structure represented by Formula (Z-0). Further, the present invention provides a composition containing the compound; a polymer obtained by polymerizing the composition; and an optically anisotropic body obtained by using the polymer.
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Page/Page column 147; 149
(2017/05/28)
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- POLYMERIZABLE COMPOUND AND OPTICAL ANISOTROPIC BODY
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PROBLEM TO BE SOLVED: To provide a polymerizable compound giving such properties when added to a solution comprising a polymerizable composition that the resultant polymerizable composition has high storage stability and can induce a liquid crystal phase
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Paragraph 0161; 0169
(2018/03/27)
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- POLYMERIZABLE COMPOUND AND OPTICAL ANISOTROPIC MATERIAL
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PROBLEM TO BE SOLVED: To provide a polymerizable compound having high storage stability when added to a polymerizable composition, less likely causing an alignment defect when a film type polymerized product is produced by using the polymerizable composition, and less likely causing discoloration of a film-like polymerized product obtained therefrom even when the product is irradiated with UV light for a long time, and to provide a polymer obtained by polymerizing the above polymerizable composition, and an optical anisotropic material using the polymer. SOLUTION: The present invention provides a compound represented by general formula (I), and also provides a polymerizable composition comprising the above compound, a polymer obtained by polymerizing the composition, and an optical anisotropic material or the like using the polymer. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0163; 0164
(2018/03/30)
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- Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C
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Protein kinase C (PKC) is a widely studied molecular target for the treatment of cancer and other diseases. We have approached the issue of modifying PKC function by targeting the C1 domain in the regulatory region of the enzyme. Using the X-ray crystal structure of the PKC δ C1b domain, we have discovered conveniently synthesizable derivatives of dialkyl 5-(hydroxymethyl)isophthalate that can act as potential C1 domain ligands. Structure-activity studies confirmed that the important functional groups predicted by modeling were indispensable for binding to the C1 domain and that the modifications of these groups diminished binding. The most promising compounds were able to displace radiolabeled phorbol ester ([3H]PDBu) from PKC α and δ at Ki values in the range of 200-900 nM. Furthermore, the active isophthalate derivatives could modify PKC activation in living cells either by inducing PKC-dependent ERK phosphorylation or by inhibiting phorbol-induced ERK phosphorylation. In conclusion, we report here, for the first time, that derivatives of isophthalic acid represent an attractive novel group of C1 domain ligands that can be used as research tools or further modified for potential drug development.
- Af Genn?s, Gustav Boije,Talman, Virpi,Aitio, Olli,Ekokoski, Elina,Finel, Moshe,Tuominen, Raimo K.,Yli-Kauhaluoma, Jari
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supporting information; experimental part
p. 3969 - 3981
(2010/01/16)
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- CAPSAICIN DERIVATES AND THE PRODUCTION AND USE THEREOF
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The invention relates to new compounds, namely capsaicin derivates, a new method for their production, and their use as micro-organism-repellent agents in paints and coatings, in particular for marine installations and ships, but also for land-based struc
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Page/Page column 8-9; 17-18
(2010/02/11)
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- Design, synthesis, and evaluation of new chemosensitizers in multi-drug-resistant Plasmodium falciparum
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A series of new chemosensitizers (modulators) against chloroquine-resistant Plasmodium falciparum were designed and synthesized in an attempt to fabricate modulators with enhancing drug-resistant reversing efficacy and minimal side effects. Four aromatic amine ring systems phenothiazine, iminodibenzyl, iminostilbene, and diphenylamine-were examined. Various tertiary amino groups including either noncyclic or cyclic aliphatic amines were introduced to explore the steric tolerance at the end of the side chain. The new compounds showed better drug-resistant reversing activity in chloroquine-resistant than in mefloquine-resistant cell lines and were generally more effective against chloroquine-resistant P. falciparum isolates from Southeast Asian (W2 and TM91C235) than those from South America (PC49 and RCS). Structure-activity relationship studies revealed that elongation of the alkyl side chain of the molecule retained the chemosensitizing activity, and analogues with four-carbon side chains showed superior activity. Furthermore, new modulators with phenothiazine ring exhibited the best chemosensitizing activity among the four different ring systems examined. Terminal amino function has limited steric tolerance as evidenced by the dramatic lose of the modulating activity, when the size of substituent at the amino group increases. The best new modulator synthesized in this study possesses all three optimized structural features, which consist of a phenothiazine ring and a pyrrolidinyl group joined by a four-carbon alkyl bridge. The fractional inhibitory concentration (FIC) index of the best compound is 0.21, which is superior to that of verapamil (0.51), one of the best-known multi-drug-resistant reversing agents. Some of the analogues displayed moderate intrinsic in vitro antimalarial activity against a W-2 clone of P. falciparum.
- Guan, Jian,Kyle, Dennis E.,Gerena, Lucia,Zhang, Quan,Milhous, Wilbur K.,Lin, Ai J.
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p. 2741 - 2748
(2007/10/03)
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- Antiarrhythmic (S)-enantiomers of methanesulfonamides
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Compounds of formula (I) and pharmacologically acceptable salts thereof wherein: n is 1 to 3, R is an alkyl, R1 is hydrogen or alkyl, R2 is alkyl, R3 is an alkyl; b) alkyl substituted with an aryl, heteroaryl or cycloalkyl
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- VINYL CATIONS. 40. pi - AND sigma -ROUTES TO VINYL CATIONS. SOLVOLYSES OF 2-METHYLCYCLOHEXENYL, CYCLOPENTYLIDENEETHYL, HEX-5-YN-1-YL, AND RELATED TRIFLATES.
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Three triflates were solvolyzed at various temperatures in water-alcohol mixtures, in TFE-water mixtures, in TFA, in TFIP, in HFIP, and in 100% TFE in the presence of various buffers and the resulting products were determined. The three reactants were also solvolyzed in a standard mixture (1:100:100 equals triflate:TFE:Na//2CO//3) at various temperatures, and the yields of products were compared. The solvolysis products were shown to be under kinetic control.
- Hanack,Fuchs,Collins
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p. 4008 - 4017
(2007/10/12)
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- SYNTHESIS OF BIFUNCTIONAL SPIN LABEL MOLECULES AND THEIR ORIENTATIONS IN MEMBRANES
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The synthesis of new derivatives of substituted pyrrolidine nitroxide free radicals is reported.The molecules are hydrophobic and bifunctional.A preliminary study of their orientation in lipid model membranes has been made by EPR.Molecules having chains of up to 17 atoms and polar end groups take up a conformation in membranes which is tentatively assigned to a bent configuration with both functional groups on one side of the membrane.These molecules are synthetic precursors of spin-labeled cross-linking reagents for membrane proteins.
- Tse-Tang, Man Wing,Gaffney, Betty Jean,Kelly, Robert E.
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p. 965 - 974
(2007/10/02)
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