- BI-FUNCTIONAL QUINOLINE ANALOGS
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Provided are compounds of Formula I: wherein X is: R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.
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Paragraph 0338
(2013/03/26)
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- Switching reaction pathways of trifluoromethylated thiobenzanilides by choice of different oxidative systems
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Trifluoromethylated thiobenzanilides are efficiently converted to 2-trifluoromethylbenzothiazoles via intramolecular oxidative cyclization under CAN/NaHCO3 oxidation, while the dimerized products with "-S-S-" bond linkage are obtained when PIDA
- Zhu, Jiangtao,Xie, Haibo,Li, Shan,Chen, Zixian,Wu, Yongming
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p. 306 - 309
(2011/06/20)
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- Direct ortho iodination of β- and γ-aryl alkylamine derivatives
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Two in one! A trifluoroacetamide protecting group not only masks an amine functionality, but also mimics peptidyl directing effects as a controlling unit in an efficient ortho iodination of a variety of biologically relevant small molecules (see example). (Chemical Equation Presented).
- Barluenga, Jose,Alvarez-Gutierrez, Julia M.,Ballesteros, Alfredo,Gonzalez, Jose M.
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p. 1281 - 1283
(2008/03/27)
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- Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
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The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
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Page/Page column 48
(2008/06/13)
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- A selenopyrylium photosensitizer for photodynamic therapy related in structure to the antitumor agent AA1 with potent in vivo activity and no long-term skin photosensitization
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Cationic chalcogenopyrylium dyes 5 were synthesized in six steps from p-aminophenylacetylene (9), have absorption maxima in methanol of 623, 654, and 680 nm for thio-, seleno-, and telluropyrylium dyes, respectively, and generate singlet oxygen with quant
- Leonard,Hall,Nelen,Davies,Gollnick,Camacho,Oseroff,Gibson,Hilf,Detty
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p. 4488 - 4498
(2007/10/03)
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- The synthesis of folic acid, multiply labelled with stable isotopes, for bio-availability studies in human nutrition
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Two different methods for the synthesis of folic acid, which are suitable for the incorporation of compounds multiply labelled with stable isotopes, are described. The first method is based on the use of a novel reductive amination to link 2-acetyIamino-4-hydroxy-6-formylpteridine withp-aminobenzoyl-L-glutamic acid. The second method is based on the penultimate formation of an amide bond between Ar-2-acetyl-Ar-10-trifluoroacetyIpteroic acid and dimethyl L-glutamate. Both methods have been used to transform [13C6]aniline into folic acid, labelled with [13C6] in the p-aminobenzoate moiety, and [3,3,4,4-2H4]-L-glutamic acid into folic acid, labelled with [2H4] in the glutamate moiety. Doubly labelled [13C6,2H 4]-p-aminobenzoyl-L-glutamate has also been prepared by the former method.
- Maunder, Peter,Finglas, Paul M.,Mallet, Anthony I.,Mellon, Fred A.,Aaqib Razzaque,Ridge, Brian,Vahteristo, Liisa,Witthoeft, Cornelia
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p. 1311 - 1323
(2007/10/03)
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- A Novel Aromatic Iodination Method Using F2
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A new method for direct aromatic iodination with IF, made in situ from the corresponding elements, is described.Depending on the reaction time and temperature, mono- or polyiodination can be achieved.Even deactivated aromatic rings can be directly iodinated without the presence of any Friedel-Crafts catalyst.Sensitive groups such as aromatic aldehydes are not affected by the reagent.
- Rozen, Shlomo,Zamir, Dov
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p. 3552 - 3555
(2007/10/02)
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