SAR of benzoylpyridines and benzophenones as p38α MAP kinase inhibitors with oral activity
摘要:
Benzoylpyridines and benzophenones were synthesized and evaluated in vitro as p38alpha inhibitors and in vivo in several models of rheumatoid arthritis. Oral activity was found to depend upon substitution: 1,1-dimethylpropynylamine substituted benzophenone 10b (IC50: 14 nM) and pyridinoyl substituted benzimidazole 17b (IC50: 21 nM) showed highest efficacy and selectivity with ED50S of 9.5 and 8.6 mg/kg po in CIA. (C) 2004 Elsevier Ltd. All rights reserved.
Arynes were found to insert into carbonâhalogen Ï-bonds of various acid halides, enabling acyl and halogen moieties to be introduced simultaneously into adjacent positions of aromatic rings.
氮烯能够插入各种酰卤中的碳-卤素σ键,从而使得酰基和卤素基团同时引入到芳香环的相邻位置。
Hallogenated aminobenzophenones and aminobenzoylpyridines as inhibitors of il-1and tnf
申请人:——
公开号:US20040097731A1
公开(公告)日:2004-05-20
Compounds of formula I and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.
Hallogenated aminobenzophenones and aminobenzoylpyridines as inhibitors of IL-1 and TNF
申请人:Révész Lászlo
公开号:US06919336B2
公开(公告)日:2005-07-19
Compounds of formula I and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNFα and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.
Poly(arylene thioether) copolymers and process for production thereof
申请人:Tosoh Corporation
公开号:EP0351136A2
公开(公告)日:1990-01-17
A novel class of poly(arylene) thioether) copolymers which are not only thermoplastic but thermosetting in nature. The copolymer may be prepared by copolymerizing a combination of dihalogenobenzonitrile, dihalogenobenzophenone and thioetherifying agent in an organic solvent.
The copolymers are highly resistant to heat and solvents and exhibit excellent mechanical properties at raised temperatures.
Catalytic regioselective Friedel-Crafts acylation of an array of anisoles/arenes with various acid chlorides using 5-20 mol % of magnetic nanopowder CuFe2O4 is reported. Unlike the conventional Friedel-Crafts reactions, which are catalyzed by moisture sensitive homogeneous catalysts/promoters, the nanopowder CuFe2O4 catalyst is moisture insensitive and the product/ketone-catalyst isolation is easily achieved using the magnetic properties of CuFe2O4. (C) 2013 Elsevier Ltd. All rights reserved.