- CHEMICAL COMPOUNDS
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A compound of formula (I), wherein Ar1, R21, R23, R24, R25, R26, R27, A, X, Y and W are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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- Diarylpyrazole compound, composition containing the same and application thereof
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The invention provides a diarylpyrazole compound, a composition containing the same and application thereof. The diarylpyrazole compound is the compound shown as formula (I) or its tautomer, stereisomer, prodrug, crystal form, pharmaceutically acceptable
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- A Straightforward Deracemization of sec-Alcohols Combining Organocatalytic Oxidation and Biocatalytic Reduction
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An efficient organocatalytic oxidation of racemic secondary alcohols, mediated by sodium hypochlorite (NaOCl) and 2-azaadamantane N-oxyl (AZADO), has been conveniently coupled with a highly stereoselective bioreduction of the intermediate ketone, catalyzed by ketoreductases, in aqueous medium. The potential of this one-pot two-step deracemization process has been proven by a large set of structurally different secondary alcohols. Reactions were carried out up to 100 mm final concentration enabling the preparation of enantiopure alcohols with very high isolated yields (up to 98 %). When the protocol was applied to the stereoisomeric rac/meso mixture of diols, these were obtained with very high enantiomeric excesses and diastereomeric ratios (95 % yield, >99 % ee, >99: 1 dr).
- Liardo, Elisa,Ríos-Lombardía, Nicolás,Morís, Francisco,González-Sabín, Javier,Rebolledo, Francisca
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supporting information
p. 3031 - 3035
(2018/06/27)
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- NOVEL HIGH AFFINITY QUINOLINE-BASED KINASE LIGANDS
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Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
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- Metallo-foldamers with backbone-coordinative oxime peptides: Control of secondary structures
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A new series of square-planar PdII-mediated foldamers with mononuclear and dinuclear helix or (double) hairpin structures were constructed by novel backbonecoordinative oxime peptides. Some of these metallo-foldamers allow significant structura
- Tashiro, Shohei,Matsuoka, Koji,Minoda, Ai,Shionoya, Mitsuhiko
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supporting information
p. 13123 - 13127
(2013/02/26)
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- Catalyst-controlled Wacker-type oxidation of protected allylic amines
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On the contrary: Utilizing the [Pd-(quinox)]-TBHP catalyst system, protected allylic amines were oxidized with high selectivity for the methyl ketone product. This is contrary to the results obtained by the substrate-controlled Tsuji-Wacker oxidation, which highlights the catalyst-controlled system presented here (see scheme). A variety of N-pro-tecting groups undergo selective oxidation with high ketone selectivity. TBHP = tert-butylhydroperoxide.
- Michel, Brian W.,McCombs, Jessica R.,Winkler, Andrea,Sigman, Matthew S.
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supporting information; experimental part
p. 7312 - 7315
(2010/11/05)
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- Reductive aldol and mannich-type reactions of azetidin-3-ones promoted by titanium tetraiodide
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A convenient method is described for the generation and reaction of the enolates of aminoacetone equivalents, which uses the reduction of azetidin-3-one with titanium tetraiodide and subsequent reactions with electrophiles. This methodology provides a str
- Hata, Shingo,Fukuda, Daisuke,Hachiya, Iwao,Shimizu, Makoto
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supporting information; experimental part
p. 473 - 477
(2010/08/23)
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- Novel high affinity quinoline-based kinase ligands
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Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
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Page/Page column 92
(2008/06/13)
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- γ-Carboline derivatives with anti-bovine viral diarrhea virus (BVDV) activity
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Based on anti-viral screening of our heteroaromatics derived from thalidomide, the γ-carboline skeleton has been identified as a superior scaffold structure for compounds with potent anti-bovine viral diarrhea virus (BVDV) activity. Structural development studies led to a potent anti-viral agent, SK5M (5-methyl-γ-carboline), with the EC50 of 0.26 μM.
- Sako, Kumiko,Aoyama, Hiroshi,Sato, Shinichi,Hashimoto, Yuichi,Baba, Masanori
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p. 3780 - 3790
(2008/12/20)
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- Molecular transporter between polymer platforms: Highly efficient chemoenzymatic glycopeptide synthesis by the combined use of solid-phase and water-soluble polymer supports
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(Figure Presented) The molecule standing at platform one ...: Rapid glycopeptide synthesis is achieved with a heterobifunctional "molecular transporter" (see scheme), which interfaces two types of polymer platforms for combined chemical and enzymatic synt
- Fumoto, Masataka,Hinou, Hiroshi,Matsushita, Takahiko,Kurogochi, Masaki,Ohta, Takashi,Ito, Takaomi,Yamada, Kuriko,Takimoto, Akio,Kondo, Hirosato,Inazu, Toshiyuki,Nishimura, Shin-Ichiro
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p. 2534 - 2537
(2007/10/03)
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- α-Amino Ketones - A Contribution to the Synthesis of Optically Active Derivatives of Amino Acids and Peptides
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The synthesis of N-Z-protected methyl ketones from amino acids via the chloromethyl ketones and dehalogenation of the latter with zinc in glacial acetic acid is described.Deprotection of the methyl ketones results in the formation of hydrohalogenides of the α-aminoalkyl methyl ketones further converted to N-acylated peptide ketones as analogs of peptide hormones or as competitively acting substrate analogs of proteolytic enzymes.Aminoacetone is conveniently prepared as well as methyl-pyrrolidyl ketone and methyl-piperidyl ketone.
- Fittkau, Siegfried,Jahreis, Guenther,Peters, Klaus,Balaspiri, Lajos
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p. 529 - 538
(2007/10/02)
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