- Therapeutic uses of tri-aryl acid derivatives
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The use of triaryl acid derivatives of formula (I) and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
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Page/Page column 171
(2010/10/20)
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- BREAST CANCER RESISTANCE PROTEIN (BCRP) INHIBITOR
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The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (-NHCOCH3 group), a cyano group (-CN group), a formyl group (-CHO group), -COOR1 (R1 is hydrogen or C1-C4 alkyl) , -O(CH2)nCOOR2 (n=1-7: R2 is hydrogen or C1-C4 alkyl) , -OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., -OP(O) (OH)2) or a salt thereof, a sulfate group (i.e., -OSO3H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
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Page/Page column 14
(2010/02/14)
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- Asymmetric syntheses of highly hydrophobic chimeric aromatic amino acids: 2-Amino-3,3'-diarylpropionic acids
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Four conformationally constrained, highly hydrophobic, and enantiomerically pure chimeric aromatic amino acids have been asymmetrically synthesized in 7 steps with overall yields of 20-30%.
- Lin, Jun,Liao, Subo,Hruby, Victor J.
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p. 3117 - 3120
(2007/10/03)
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- De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the δ-opioid receptor
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On the basis of the structure-activity relationships of δ-opioid- selective peptide ligands and on a model of the proposed bioactive conformation for a potent and selective, conformationally constrained δ- opioid peptide ligand [(2S,3R)-TMT1]DP
- Liao, Subo,Alfaro-Lopez, Josue,Shenderovich, Mark D.,Hosohata, Keiko,Lin, Jun,Li, Xiaoping,Stropova, Dagmar,Davis, Peg,Jernigan, Kevin A.,Porreca, Frank,Yamamura, Henry I.,Hruby, Victor J.
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p. 4767 - 4776
(2007/10/03)
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- A practical synthesis of (R)-(-)-phenylephrine hydrochloride
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(R)-(-)-Phenylephrine hydrochloride is a clinically potent adrenergic agent and β-receptor sympathomimetic drug, exclusively marketed in the optically active form. An asymmetric synthesis has been developed with high enantiomeric excess based on hydrolytic kinetic resolution of a styrene oxide derivative using (R,R)-SalenCoIIIOAc complex.
- Gurjar, Mukund K.,Krishna, L. Murali,Sarma, Bugga V.N.,Chorghade, Mukund S.
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supporting information
p. 422 - 424
(2013/09/08)
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- Inhibition of pig kidney L-aromatic amino acid decarboxylase by 2,3- methano-m-tyrosines
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Both racemic (E)- and (Z)-2,3-methano-m-tyrosines (9E and 9Z) have been synthesized from a common intermediate, monoester (Z)-1-(ethoxycarbonyl)-2- [3-[(2-methoxyethoxy)methoxy]phenyl]cyclopropanecarboxylic acid (5). Quinine and ephedrine, respectively, w
- Ahmad,Phillips,Stammer
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p. 1410 - 1417
(2007/10/02)
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