- PREPARATION AND USE OF REACTIVE OXYGEN SPECIES SCAVENGER
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A compound of Formula (I), pharmaceutically acceptable salts thereof, and individual enantiomers or diastereomers thereof are disclosed. Compositions and methods useful for treatment or suppression of diseases, developmental delays and symptoms related to
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Page/Page column 113
(2019/03/17)
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- GLYCOAMINO ACID AND USE THEREOF
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An object of the present invention is to provide glycoamino acid as an amino acid precursor with improved properties (particularly water-solubility, stability in water, bitter taste etc.). The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof.
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Page/Page column 7; 8
(2016/08/17)
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- Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists
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The present invention relates to a conjugated compound of Formula I : Q-Z-R4 wherein Q is a TLR7 and/or TLR8 agonist and Z-R4 is a TLR2 agonist, said conjugated compound being chosen among compounds of Formula II :
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- Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists
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A conjugated compound of Formula I: Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a TLR2 agonist, the conjugated compound being chosen among compounds of Formula II:
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- A class of novel Schiff's bases: Synthesis, therapeutic action for chronic pain, anti-inflammation and 3D QSAR analysis
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To discover analgesics for treating chronic pain 17 novel Schiff's bases, N,N′-(Z-allylidene-1,3-diyl)bisamino acid methyl esters were prepared from 1,1,3,3,-tetramethoxypropane and amino acid methyl esters. On tail-flick mouse model 20 μmol/kg of these Schiff's bases were orally administered, the analgesic action started 30 min after administration, reached the maximum 120 min after administration, and at 180 min this action was still observed. On a xylene-induced ear edema mouse model 20 μmol/kg of these Schiff's bases exhibited desirable anti-inflammation. Thus the present Schiff's bases are able to treat chronic pain from inflammation. The effect of the side chains of the amino acid residues of these Schiff's bases on the analgesic activity was explained with 3D QSAR.
- Zhou, Yinjian,Zhao, Ming,Wu, Yingting,Li, Chunyu,Wu, Jianhui,Zheng, Meiqing,Peng, Li,Peng, Shiqi
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experimental part
p. 2165 - 2172
(2010/05/18)
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- A new protocol for selective deprotection of N-tert-butoxycarbonyl protective group (t-Boc) with Sn(OTf)2
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A simple and efficient method for the selective removal of N-Boc group by employing tin(II) trifluoromethanesulfonate [Sn(OTf)2] in CH2Cl2 or solvent-free conditions was developed. The scope of this procedure is explored for the deprotection of a variety of amines, including amino acid derivatives.
- Bose, D. Subhas,Kumar, K. Kiran,Reddy, A.V. Narsimha
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p. 445 - 450
(2007/10/03)
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- Amino acid derivatives as HIV aspartyl protease inhibitors
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The present invention relates to a class of amino acid derivatives with HIV aspartyl protease inhibitory properties.
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- RGD mimetics containing a central hydantoin scaffold: α(v)β3 vs α(IIb)β3 selectivity requirements
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The synthesis of a series of RGD mimetic α(v)β3 antagonists containing a hydantoin scaffold is shown. The results demonstrate some of the structural requirements for the design of selective α(v)β3 antagonists (vs α(IIb)β3)
- Peyman, Anusch,Wehner, Volkmar,Knolle, Jochen,Stilz, Hans Ulrich,Breipohl, Gerhard,Scheunemann, Karl-Heinz,Carniato, Denis,Ruxer, Jean-Marie,Gourvest, Jean-Francois,Gadek, Thomas R.,Bodary, Sarah
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p. 179 - 182
(2007/10/03)
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- The (2-phenyl-2-trimethylsilyl)ethoxycarbonyl (Psoc) group - A novel amino protecting group
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A novel silicon containing protecting group has been developed based on the known 2-(trimethylsilyl)ethyl system. The new protecting group is cleaved under very mild conditions by treatment with tetra-n-butylammonium fluoride in CH2Cl2 much more rapidly than the 2-(trimethylsilyl)ethoxycarbonyl group, leading to less side reactions.
- Wagner,Heiner,Kunz
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p. 1753 - 1756
(2007/10/03)
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- Lewis Acid-Mediated Selective Removal of N-tert-Butoxycarbonyl Protective Group (t-Boc)
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A simple and efficient method for the selective cleavage of N-Boc protective groups from amines employing Lewis acid aluminum chloride, is described.The scope of this procedure is explored for the deprotection of a variety of amines including amino acid derivatives. - Keywords: aluminum chloride; t-Boc carbamates; selective cleavage
- Bose, D. Subhas,Lakshminarayana, V.
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- Syntheses and Reactions of Silyl Carbamates. 1. Chemoselective Transformation of Amino Protecting Groups via tert-Butyldimethylsilyl Carbamates
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The N-tert-butyldimethylsilyloxycarbonyl group (silyl carbamate) was synthesized from commonly used amino protecting groups such as N-tert-butoxycarbonyl (Boc) and N-benzyloxycarbonyl (Z) by treatment with tert-butyldimethylsilyl trifluoromethanesulfonate/2,6-lutidine and tert-butyldimethylsilane/Pd(OAc)2, respectively.This novel species, upon activation with fluoride ion, reacts with a variety of electrophiles to give N-ester type compounds in high yield.For example, the conversion of N-t-Boc compounds into their corresponding N-Z compounds via a silyl carbamate was accomplished under these mild reaction conditions.
- Sakaitani, Masahiro,Ohfune, Yasufumi
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p. 870 - 876
(2007/10/02)
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- Peptide-bond Formation, Chemoselective Acylation of Amino Acids, and Crosslinking Reaction between Amino Acids Utilizing a Functional Five-membered Heterocycle, 1,3-Thiazolidine-2-thione
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The monitored aminolysis of 3-acyl-1,3-thiazolidine-2-thiones has been extended to the peptide-bond formation, the chemoselective acylation of amino acids having multifunctional groups, and the crosslinking reaction between amino acids.
- Nagao, Yoshimitsu,Miyasaka, Tadayo,Seno, Kaoru,Fujita, Eiichi,Shibata, Daisuke,Doi, Etsushiro
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p. 2439 - 2446
(2007/10/02)
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- MONITORED AMINOLYSIS OF 3-ACYL-1,3-THIAZOLIDINE-2-THIONE WITH AMINO ACID AND ITS DERIVATIVE: PEPTIDE BOND FORMATION, CHEMOSELECTIVE ACYLATION, AND BRIDGING REACTION
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As a new extention of the monitored aminolysis of 3-acyl-1,3-thiazolidine-2-thione, its applications to peptide bond formation, chemoselective acylation of amino acid, and bridging reaction on the enzyme model are reported.
- Nagao, Yoshimitsu,Miyasaka, Tadayo,Seno, Kaoru,Yagi, Masahiro,Fujita, Eiichi
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p. 463 - 466
(2007/10/02)
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