- Efficient synthesis of indoles using [3,3]-sigmatropic rearrangement of N-trifluoroacetyl enehydrazines
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[3,3]-Sigmatropic rearrangement of N-trifluoroacetyl enehydrazines provides a novel method for the construction of indoles. N-Trifluoroacetyl enehydrazine having a cyclopentene ring smoothly underwent [3,3]-sigmatropic rearrangement followed by cyclizatio
- Miyata, Okiko,Takeda, Norihiko,Kimura, Yasuo,Takemoto, Yoshiji,Tohnai, Norimitsu,Miyata, Mikiji,Naito, Takeaki
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p. 3629 - 3647
(2007/10/03)
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- Isosteric ramatroban analogs: Selective and potent CRTH-2 antagonists
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The chemoattractant receptor-homologous molecule expressed on T H2 cells (CRTH-2), also found on eosinophils and basophils, is a prostaglandin D2 receptor involved in the recruitment of these cell types during an inflammatory response. In this report, we describe the synthesis and optimization of a ramatroban isostere that is a selective and potent antagonist of CRTH-2 which may be useful in the treatment of certain diseases.
- Robarge, Michael J.,Bom, David C.,Tumey, L. Nathan,Varga, Norbert,Gleason, Elizabeth,Silver, Daniel,Song, Jianping,Murphy, Steven M.,Ekema, George,Doucette, Chris,Hanniford, Doug,Palmer, Marc,Pawlowski, Gary,Danzig, Joel,Loftus, Margaret,Hunady, Karen,Sherf, Bruce A.,Mays, Robert W.,Stricker-Krongrad, Alain,Brunden, Kurt R.,Harrington, John J.,Bennani, Youssef L.
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p. 1749 - 1753
(2007/10/03)
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- TRICYCLIC COMPOUNDS
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A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents -NR3-CO-, -CO-NR3- and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and the like); M represents an alkylene linking group (a carbon atom constituting the carbon chain may be replaced with a nitrogen atom, an oxygen atom and the like); X represents -S-, -O-, -NR4-, -NR5-CO- and the like (R4 and R5 represent a hydrogen atom, a lower alkyl group and the like) or a single bond; Y represents an alkyl group, an aryl group, an amino group, an aromatic heterocyclic group and the like; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower acyl group; and R21, R22 and R23 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like] or a salt thereof. The compound is useful as an active ingredient of medicaments for diseases in which neuropeptide Y is involved, ingestion control for hyperphagia and the like.
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