A new class of inhibitors of secretory phospholipase A2: enolized 1,3-dioxane-4,6-dione-5-carboxamides
摘要:
Enolized 1,3-dioxane-4,6-dione-5-carboxamides a were identified as a new class of inhibitors of secretory phospholipase A(2) from human polymorphonuclear leucocytes (h-PMN PLA(2)). Among the more than 30 compounds synthesized, the most potent inhibitors (IC50 0.6-10 mu M) were found in the series of 2,4-disubstituted phenyl analogues of a. Compound 1a was selected for evaluation of its biological profile. This substance potently inhibited secretory PLA(2)s from several sources other than human PMNs, with a clear preference for group II over group I PLA(2), whereas human cytosolic PLA(2) and phospholipase C were not significantly affected. Inhibition of h-PMN PLA(2) was calcium-dependent. In intact mammalian cells stimulated in vitro, the release of arachidonic acid and the generation of prostaglandins and leukotrienes were inhibited at concentrations compatible with inhibition of PLA(2) as an underlying mechanism. In animal models in vivo (carragheenan oedema, adjuvant arthritis, pertussis pleurisy) 1a showed antiinflammatory activity, although the effect was rather weak compared with standard reference compounds.
Abstract The reaction between dialkyl acetylene dicarboxylate and 2-aryl-1,3-dioxane-4,6-dione derivatives in the presence of triphenylphosphine in ethyl acetate led to stable phosphorus ylides in good yields. These stabilized phosphorus ylides exist as a mixture of two geometrical isomers as a result of restricted rotation around the carbon–carbon partial double bond. The 1H NMR variable temperature spectra
CARBON FIBER MOLDING MATERIAL, MOLDING MATERIAL, AND CARBON FIBER-STRENGTHENING COMPOSITE MATERIAL
申请人:Toray Industries, Inc.
公开号:EP2789648A1
公开(公告)日:2014-10-15
Provided is a carbon fiber forming raw material having excellent interfacial adhesion between carbon fibers and a thermosetting resin and capable of giving a molded article having excellent mechanical characteristics. The carbon fiber forming raw material is a carbon fiber forming raw material (Z) as a prepreg including sizing agent-coated carbon fibers and a thermosetting resin or a carbon fiber forming raw material (Y) as a forming material that includes sizing agent-coated carbon fibers and has a woven fabric form or a braid form. The sizing agent includes components (A) and (B). The component (A) is an epoxy compound having two or more epoxy groups or two or more types of functional groups. The component (B) is one or more compounds selected from the group consisting of a tertiary amine compound, a tertiary amine salt, a quaternary ammonium salt, a quaternary phosphonium salt, and a phosphine compound. The component (B) is contained in an amount of 0.1 to 25 parts by mass relative to 100 parts by mass of the component (A).
POLYMERIZABLE COMPOSITION FOR OPTICAL MATERIAL, AND OPTICAL MATERIAL AND PLASTIC LENS OBTAINED FROM COMPOSITION
申请人:Mitsui Chemicals, Inc.
公开号:EP3351564A1
公开(公告)日:2018-07-25
A polymerizable composition for an optical material according to the present invention, including: a monomer mixture (A) including a polymerizable monomer having a (meth) acrylic group, a photochromic compound (B) which is at least one selected from compounds represented by Formulae (1) and (2) ; and an ultraviolet absorbing agent (C) which is at least one selected from compounds represented by Formulae (a) to (c) .
PC-L-Chain (1)
PC-L-Chain-L'-PC' (2)
POLYMERIZABLE COMPOSITION FOR OPTICAL MATERIALS, OPTICAL MATERIAL OBTAINED FROM SAID COMPOSITION, AND PLASTIC LENS
申请人:Mitsui Chemicals, Inc.
公开号:EP3351574A1
公开(公告)日:2018-07-25
A polymerizable composition for an optical material according to the present invention includes a polyisocyanate compound (A), a polyol compound (B) having a number average molecular weight of 100 or more, a difunctional or higher functional active hydrogen compound (C) (but, excluding the compound (B)), a photochromic compound (D), and an ultraviolet absorber (E).