- Process of preparing isocyanate compounds comprising non-chlorination derivatives and Composition thereof
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The present invention relates to a process for producing xylylene diisocyanate. The present invention relates to a process for preparing isocyanates comprising the obtained non-chlorinated derivatives. In particular, the present invention relates to an isocyanate composition comprising an unchlorinated derivative obtained by the reduction reaction and a polymerizable composition including the same.
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Paragraph 0149-0166
(2021/10/05)
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- Novel leucine ureido derivatives as inhibitors of aminopeptidase N (APN)
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Aminopeptidase N (APN/CD13) over expressed on tumor cells, plays a critical role in tumor invasion, metastasis, and tumor angiogenesis. Here we described the design, synthesis and preliminary activity studies of novel leucine ureido derivatives as aminopeptidase N (APN/CD13) inhibitors. The results showed that compound 8c had the most potent inhibitory activity against APN with the IC 50 value to 0.06 ± 0.041 μM, which could be used for further anticancer agent research.
- Ma, Chunhua,Jin, Kang,Cao, Jiangying,Zhang, Lei,Li, Xiaoguang,Xu, Wenfang
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p. 1621 - 1627
(2013/04/24)
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- Orally Active β-Lactam Inhibitors of Leukocyte Elastase-1. Activity of 3,3-Diethyl-2-azetidinones
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A thorough analysis of the mechanism of inhibition of human leukocyte elastase (HLE) by a monocyclic β-lactam and the mechanism of β-lactam hydrolysis led to the preparation of potent and highly stable inhibitors of HLE.This work led to the identification of 4--3,3-diethyl-1-carbonyl>-2-azetidinone (2) as the first orally active inhibitor of human leukocyte elastase (HLE).Analogs of 2 with different substituents on the urea N were synthesized and evaluated for their activity in vitro against HLE as well as in vivo in a hamster lung hemorrhage model.Compounds with a methyl or a methoxy group in the para position of the benzene ring were very potent in both assays.The results are discussed on the basis of the proposed model for the binding of this class of inhibitors to HLE and a possible mechanism of inhibition is presented.
- Shah, Shrenik K.,Dorn, Conrad P.,Finke, Paul E.,Hale, Jeffrey J.,Hagmann, William K.,et al.
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p. 3745 - 3754
(2007/10/02)
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