- Development of Dipeptidic hGPR54 Agonists
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A series of dipeptides were designed as potential agonists of the human KiSS1-derived peptide receptor (hGPR54). While the sequence Arg-Trp-NH2was the most efficient in terms of affinity, we established a convergent synthetic strategy to optimi
- Doebelin, Christelle,Bertin, Isabelle,Schneider, Séverine,Schmitt, Martine,Bourguignon, Jean-Jacques,Ancel, Caroline,Simonneaux, Valerie,Simonin, Frédéric,Bihel, Frédéric
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p. 2147 - 2154
(2016/11/04)
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- Modulators of methyl modifying enzymes, compositions and uses thereof
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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
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Page/Page column 162; 163
(2015/12/26)
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- MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein
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Paragraph 00324; 00327
(2013/06/05)
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- Direct carboxylation of arenes and halobenzenes with CO2 by the combined use of AlBr3 and R3SiCl
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The Lewis acid-mediated direct carboxylation of aromatic compounds with CO2 is efficiently promoted by the addition of silyl chlorides bearing three alkyl and/or aryl substituents in total on the silicon atom. Thus, toluene, xylenes, mesitylene, and some other alkylbenzenes are treated with a 1:1 mixture of AlBr3 and Ph3SiCl in neat substrates under CO2 pressure (3.0 MPa) at room temperature, to give the corresponding carboxylic acids in 60-97% yields, based on AlBr3. Polycyclic arenes, including naphthalene, phenanthrene, and biphenyl, are regioselectively carboxylated in 91-98% yields with the aid of 1 molar equiv of AlBr3 and Ph3SiCl in an appropriate solvent, chosen from benzene, chlorobenzene, and fluorobenzene. These solvents, as well as bromobenzene, resist carboxylation; however, they are also carboxylated in moderate yields when treated with a 1:5 mixture of AlBr3 and iPrSiCl at elevated temperatures. The FT-IR spectrum of a mixture prepared by exposing a suspension of AlBr3 and Ph3SiCl in cyclohexane to CO 2 exhibits an absorption band around 1650 cm-1, assigned to the C=O stretching vibration of a species consisting of CO2, AlBr3, and Ph3SiCl, which suggests that the silyl chlorides activate CO2 in cooperation with AlBr3. 1H NMR analysis of unworked-up reaction mixtures reveals that the products merge as aluminum carboxylates. The mass balance concerning silicon indicates that the silyl chlorides are recycled during the reaction sequence. On the basis of these observations, a feasible mechanism is proposed for the present carboxylation.
- Nemoto, Koji,Yoshida, Hiroki,Egusa, Naoki,Morohashi, Naoya,Hattori, Tetsutaro
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experimental part
p. 7855 - 7862
(2011/02/21)
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- Alpha-helical mimetics
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Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.
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- Amine Compounds
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There is provided a compound exhibiting an activity of suppressing immune response with reduced adverse drug reactions, which compound is useful in the chemotherapy for preventing or treating, for example, a wide range of various autoimmune diseases including systemic erythematodes, chronic rheumatoid arthritis, Type I diabetes, inflammatory bowel disease, biliary cirrhosis, uveitis, multiple sclerosis or other disorders, or chronic inflammatory diseases, or cancers, lymphoma or leukemia, or resistance to organ or tissue transplantation or rejection against transplantation. Novel amine compounds having an S1P1/Edg1 receptor agonist effect, possible stereoisomers or racemic bodies of the compounds, or pharmacologically acceptable salts, hydrates or solvates of the compound, the stereoisomers or the racemic bodies, or prodrugs of the compounds, the stereoisomers, the racemic bodies, the salts, the hydrates or the solvates, are provided.
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Page/Page column 161
(2008/12/08)
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- 4-Aminoquinolines: Novel nociceptin antagonists with analgesic activity
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Small-molecule nociceptin antagonists were synthesized to examine their therapeutic potential. After a 4-aminoquinoline derivative was found to bind with the human ORL1 receptor, a series of 4-aminoquinolines and related compounds were synthesized and their binding was evaluated. Elucidation of structure - Activity relationships eventually led to the optimum compounds. One of these compounds, N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide hydrochloride (11) not only antagonized nociceptin-induced allodynia in mice but also showed analgesic effect in a hot plate test using mice and in a formalin test using rats. Its analgesic effect was not antagonized by the opioid antagonist naloxone. These results indicate that this nociceptin antagonist has the potential to become a novel type of analgesic that differs from μ-opioid agonists.
- Shinkai,Ito,Iida,Kitao,Yamada,Uchida
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p. 4667 - 4677
(2007/10/03)
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- Reduction of olefins on solid support using diimide
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The reduction of solid supported olefinic substrate using diimide is described. The diimide, prepared from sulfonylhydrazide, was found to efficiently reduce the olefinic substrates. Typically, the reaction proceeds in over 90% yield to afford the reduction product cleanly after cleavage from the Wang resin.
- Lacombe, Patrick,Castagner, Bastien,Gareau, Yves,Ruel, Rejean
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p. 6785 - 6786
(2007/10/03)
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- Liquid Crystalline Asymmetric Bisphenyl-4,4'-bibenzyldicarboxylates and Polysiloxanes with Bisphenyl-4,4'-bibenzyldicarboxylat Components in the Side Chains, Synthesis and Characterization
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Asymmetric bisphenyl bibenzyl-4,4'-dicarboxylates with an alkenyloxy- or the 10-undecenoylgroup in the p-position of one terminal benzene ring and the butyl-, an alkoxy- or the thiomethylgroup in the p-position of the other terminal benzene ring (12-14) are synthesized.The olefins 12-14 are added to a poly(methylhydrogensiloxane) 15 to give mesomorphic side chain polysiloxanes 16-18.Data of liquid crystalline properties of 12-14, 16-18 and precursors are discussed.
- Boberg, Friedrich,Mueller, Enno,Reddig, Wolfram
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p. 136 - 142
(2007/10/02)
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