- OXADIAZOLE MODULATORS OF S1P METHODS OF MAKING AND USING
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The invention is directed to Compounds of Formula (I): wherein each variable is defined herein, as well as methods of making and using the compounds as agonists of S1P1 and/or S1P5 for instance for treating graft versus host disease and autoimmune diseases.
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- THIADIAZOLE MODULATORS OF S1P AND METHODS OF MAKING AND USING
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The invention is directed to compounds of the formula: wherein each of the variables are defined herein, as well as methods of making and using the compounds as agonists of S1P1 and/or S1P5 for instance treating an autoimmune disease.
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- Efficient synthesis of a selective Y5 receptor antagonist
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A selective Y5 receptor antagonist, the hydrochloride of 2-methyl-4-pyrrolidinyl-6-[(E)-2-(3-trifluoromethylphenyl)-vinyl]pyridine, can be prepared in a 7-step synthesis.
- Guery, Sebastien,Rival, Yveline,Wermuth, Camille G.
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p. 1715 - 1719
(2007/10/03)
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- Carbonylation of hydrocarbylpalladium(II) complexes containing substituted pyridinecarboxylate chelating ligands. Steric and electronic manipulation of the CO-insertion mechanism
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Organopalladium(II) complexes of general formula [PdR(N-O)L] [R = Ph, N-O = pyridinecarboxylate (pyca), L = P(C6H11)3; R = Ph, N-O = 6-methylpyridinecarboxylate (mpyca), L = PPh3, PMePh2, P(C6H11)3 or PEt3; R = Ph, N-O = 4-nitropyridinecarboxylate (npyca), L = P(C6H11)3; R = Ph, N-O = 6-methyl-4-nitropyridinecarboxylate, L = P(C6H11)3; R = Me, N-O = mpyca, L = PPh3, P(CH2Ph)3 or P(C6H11)3; R = Me, N-O = npyca, L = PPh3, PMePh2 or P(C6H11)3] have been prepared, and their carbonylation reactions studied in detail. Kinetic studies of the CO-insertion process have indicated that the rate of reaction decreases as the basicity of the phosphine, L, increases. Complexes containing the highly basic phosphine P(C6H11)3 only undergo carbonylation if hemilability of the chelating ligand is promoted (by substitution of the N-O chelate). Substitution of the N-O ligand modifies the carbonylation pathway and provides an alternative route from that generally observed for palladium(II) and platinum(II) hydrocarbyl complexes of pyca. A mechanism for insertion of CO involving partial dissociation of the N-O chelate is proposed for these complexes. The crystal stucture of [PdMe(mpyca)(PPh3)] has been determined. The complex has square-planar co-ordination with the nitrogen of pyca trans to the phosphorus. Considerable distortion of the inner co-ordination sphere is evident, caused by steric interactions betwen the σ-methyl ligand and the methyl group on the N-O ligand.
- Hoare, Jason L.,Cavell, Kingsley J.,Hecker, Richard,Skelton, Brian W.,White, Allan H.
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p. 2197 - 2205
(2007/10/03)
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