- SUBSTITUTED POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVE PRODRUG
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The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
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Page/Page column 0697; 0698; 0699
(2013/08/14)
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- (S)-N-(5-Chlorothiophene-2-sulfonyl)-β,β-diethylalaninol a Notch-1-sparing γ-secretase inhibitor
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Accumulation of beta-amyloid (Aβ), produced by the proteolytic cleavage of amyloid precursor protein (APP) by β- and γ-secretase, is widely believed to be associated with Alzheimer's disease (AD). Research around the high-throughput screening hit (S)-4-chlorophenylsulfonyl isoleucinol led to the identification of the Notch-1-sparing (9.5-fold) γ-secretase inhibitor (S)-N-(5-chlorothiophene-2-sulfonyl)-β,β-diethylalaninol 7.b.2 (Aβ 40/42 EC50 = 28 nM), which is efficacious in reduction of Aβ production in vivo.
- Cole, Derek C.,Stock, Joseph R.,Kreft, Anthony F.,Antane, Madelene,Aschmies, Suzan H.,Atchison, Kevin P.,Casebier, David S.,Comery, Thomas A.,Diamantidis, George,Ellingboe, John W.,Harrison, Boyd L.,Hu, Yun,Jin, Mei,Kubrak, Dennis M.,Lu, Peimin,Mann, Charles W.,Martone, Robert L.,Moore, William J.,Oganesian, Aram,Riddell, David R.,Sonnenberg-Reines, June,Sun, Shaiu-Ching,Wagner, Erik,Wang, Zheng,Woller, Kevin R.,Xu, Zheng,Zhou, Hua,Jacobsen, J. Steven
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scheme or table
p. 926 - 929
(2009/09/06)
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- Bisoxazoline and bioxazoline chiral ligands bearing 4-diphenylmethyl shielding substituents. Diels-Alder reaction of cyclopentadiene with 3-acryloyl-2-oxazolidinone catalyzed by the aqua nickel(II) complex
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Enantiopure 2-amino-3,3-diphenyl-1-propanol was synthesized by the hidantoin route starting from diphenyl-acetaldehyde followed by subsequent functional group transformations and optical resolution by a chiral HPLC. The amino alcohol can be converted into two new chiral ligands: 4,4'-bis(diphenylmethyl)-2,2'-bioxazoline and 2,2'-isopropylidenebis(4-diphenylmethyloxazoline), and further to complexes with copper(II) trifluoromethanesulfonate and nickel(II) perchlorate hexahydrate. The nickel(II) aqua complex obtained from the bisoxazoline effectively catalyzed the Diels-Alder reactions of cyclopentadiene with 3-acryloyl-2-oxazolidinone in high endo-selectivities and moderate enantioselectivities via a square planar transition structure.
- Kanemasa,Adachi,Yamamoto,Wada
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p. 681 - 687
(2007/10/03)
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- 3,3-diphenyl prop-2-yl amino acid derivatives and their use as tachykinin antagonists
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Compounds of formula (I), or a salt or prodrug thereof, wherein R1 represents H, C1-4 alkyl or CH2 COOH; R2 represents H or C1-4 alkyl, with the proviso that R1 and R2 are not both H; R3 and R4 each independently rely resent H, C1-, alkyl. C2-6 alkenyl C1-6 alkoxy, halo or trifluoromethyl; A1, A2, A3, and A4 each independently represent H, C1-6 alkyl, C1-6 alkenyl, C1-6 alkoxy, halo or trifluoromethyl; and A5 and A6 each independently represent H or C1-4 are tachykinin antagonists useful STR1
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