- A Route to the C,D,E Ring System of the Aspidosperma Alkaloids
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A short synthetic sequence leading to the formation of the C,D,E-ring subunit of the Aspidosperma alkaloids is reported. This route is based on a ring fragmentation/intramolecular azomethine ylide 1,3-dipolar cycloaddition reaction sequence that gives the
- Giampa, Geoffrey M.,Fang, Jian,Brewer, Matthias
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- Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β2-adrenoceptor agonists
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A series of β2-adrenoceptor agonists with an 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one moiety is presented. The stimulatory effects of the compounds on human β2-adrenoceptor and β1-adrenoceptor were characterized by a cell-based assay. Their smooth muscle relaxant activities were tested on isolated guinea pig trachea. Most of the compounds were found to be potent and selective agonists of the β2-adrenoceptor. One of the compounds, (R)-18c, possessed a strong β2-adrenoceptor agonistic effect with an EC50 value of 24 pM. It produced a full and potent airway smooth muscle relaxant effect same as olodaterol. Its onset of action was 3.5 min and its duration of action was more than 12 h in an in vitro guinea pig trachea model of bronchodilation. These results suggest that (R)-18c is a potential candidate for long-acting β2-AR agonists.
- Yi, Ce,Xing, Gang,Wang, Siqi,Li, Xiaoran,Liu, Yichuang,Li, Jinyan,Lin, Bin,Woo, Anthony Yiu-Ho,Zhang, Yuyang,Pan, Li,Cheng, Maosheng
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- INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING LFA-1
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The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moi
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Paragraph 0119; 0120
(2013/08/14)
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- PYRIMIDINE AMIDE COMPOUNDS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.
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Page/Page column 21
(2012/10/07)
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- 1,2,4-Triazine Derivatives, Preparation and Use Thereof in Human Therapy
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The invention concerns 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a branched or linear C1-C7 alkyl or alkenyl radical, a C1/s
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Page/Page column 20-21
(2008/12/06)
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- Phenylacetamide derivatives and pharmaceutical compositions thereof
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The present invention provides novel phenylacetamide derivatives having the following formula STR1 wherein: X is a hydrogen, halogen, hydroxy, nitro, amino, R1, NR1 R2, NHR1 or OR1 wherein R1/su
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- Novel phenylacetamide derivatives and processes for the preparation thereof
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The present invention provides novel phenylacetamide derivatives having the following formula wherein:, X is a hydrogen, halogen, hydroxy, nitro, amino, R1, NR1R2, NHR1 or OR1 wherein R1 and R2 are an optionally substituted C1 8 alky
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- Synthesis of Isoquinobenzazepines
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A simple method for the synthesis of 12-alkoxyisoquinobenzazepines 6 in good yields starting from 3-(3-alkoxyphenyl)propylamines 1 and 1-isochromanone (2) is described.
- Meise, Werner,Schlueter, Gerd
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p. 639 - 642
(2007/10/02)
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