19411-56-4Relevant academic research and scientific papers
PYRIMIDINE DERIVATIVES AS PGE2 RECEPTOR MODULATORS
-
Page/Page column 96; 97, (2018/12/13)
The present invention relates to pyrimidine derivatives of formula (I) wherein (R1)n, R3, R4a, R4b, R5a, R5b and Ar1 are as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (II) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.
Fluorescent amino acid derivatives
-
Page/Page column 7-8, (2011/04/26)
The subject of the present invention is to provide a fluorescent substance excitable under visible light, having higher photostability and a long fluorescence lifetime. Another subject is to provide a fluorescent substance consists of a non-natural amino
Introduction of a highly photodurable and common-laser excitable fluorescent amino acid into a peptide as a FRET acceptor for protease cleavage detection
Taki, Masumi,Yamazaki, Yoshito,Suzuki, Yuto,Sisido, Masahiko
scheme or table, p. 818 - 819 (2011/01/10)
Synthesis and photochemical properties of a benzoacridonecontaining fluorescent amino acid (badAla) which is photodurable and excitable by widely applicable 488 nm lasers was described. The amino acid carries a relatively small fluorophore that shows abso
Fluorescent Amino Acid Derivatives
-
, (2010/06/22)
The subject of the present invention is to provide a fluorescent substance excitable under visible light, having higher photostability and a long fluorescence lifetime. Another subject is to provide a fluorescent substance consists of a non-natural amino acid applicable to peptide synthesis systems. Searching fluorescent substances, which are fluorescent amino acids and excitable under visible light, having the lowest possible molecular weight for a high photostability resulted in forming a condensed polycyclic aromatic compound by subjecting a compound having an acridone structure to substitution with an amino acid and further condensation with a benzene ring. Thus, the subject is achieved by the fluorescent substance consisting of amino acid-substituted benzoacridone derivative excitable under visible light.
SUBSTITUTED AMINO PHENYLACETIC ACIDS, DERIVATIVES THEREOF, THEIR PREPARATION AND THEIR USE AS CYCLOOXYGENASE 2 (COX-2) INHIBITORS
-
Page 39-40, (2008/06/13)
Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3-C8)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3-C6)cycloalkylmonocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.
Carbon-Hydrogen and C-X (X=Cl or SiMe3) Bond Activation. 1-Cyclopalladation and Oxidation of Some Derivatives of 2-naphthalene
Valk, Jean-Marc,Belzen, Ruud van,Boersma, Jaap,Spek, Anthony L.,Koten, Gerard van
, p. 2293 - 2302 (2007/10/02)
The regioselective palladation reactions of 3-substituted derivatives of 2-naphthalene, C10H6(CH2NMe2)-2-R-3 (R=Cl, SiMe3 or OSiMe3), were studied.For the substrate with R=Cl, no cyclopalladation at position 1 was observed and the co-ordination complex was isolated.The 3-palladated product was formed in 10percent yield via C-Cl activation.The reaction of 2--3-methylnaphthalene with Pd(O2CMe)2 and work-up with LiCl did lead to palladation at position 1, the resulting complex being isolated in 96percent yield.The crystal structure of bis(acetonitrile) -3-methyl-1-naphthyl>palladium trifluoromethanesulfonate was solved.Monoclinic, space group P21/n, with a=13.193(1), b=11.801(1), c=14.797(1) Angstroem, β=105.15(1) deg, Z=4.The structure was refined to R=0.042 for 3455 reflections with I > 2.5?(I).Palladation at position 1 was also achieved by oxidative addition of 1-bromo-2-naphthalene to (dba=dibenzylideneacetone).Protection of C(3) with R=SiMe3 resulted in quantitative replacement of the SiMe3 group by palladium.Silicon-oxygen bond cleavage was observed when the substrate with R=OSiMe3 was treated with Pd(O2CMe)2.Palladium bis-2-naphtholate> was obtained quantitatively.Oxidation of several arylpalladium complexes with tBuO2H was achieved in the presence of (acac=acetylacetonate) or 2> (cod=cycloocta-1,5-diene) as catalyst.The corresponding 1-naphthols were prepared in yields varying from 33 to 78 percent.In a number of cases the corresponding 1,4-naphthoquinones were prepared in yields varying from 18 to 38percent.
