955016-25-8Relevant articles and documents
Enantioselective Synthesis of cis and trans 4-Aminopipecolic Acids as γ-Amino Acids for the Construction of Cyclic RGD-Containing Peptidomimetics Antagonists of αVβ3 Integrin
Bianchini, Francesca,Contini, Alessandro,Dordoni, Francesca,Occhiato, Ernesto G.,Scarpi, Dina
, (2020/07/04)
A stereodivergent strategy to obtain enantiopure cis and trans 4-aminopipecolic acids (4-APAs) in a suitably protected form for peptide synthesis has been devised starting from a common, known precursor in turn easily prepared from commercial (R)-4-cyano-3-hydroxybutyric acid ethyl ester. The two isomers were efficiently obtained in 40 percent and 23 percent overall yields, respectively, in seven and ten steps. To demonstrate their usefulness in peptidomimetic synthesis, both 4-APA isomers were incorporated as γ-amino acids in a cyclic RGD-containing sequence, although for the trans 4-APA isomer a further amino acid in the sequence (L-Phe) was needed to allow ring closure. The two cyclopeptides were tested as αVβ3 integrin antagonists in comparison with cilengitide.
CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 00655-00657; 00763-00765, (2019/06/11)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.
COMPOUNDS FOR USE IN THE TREATMENT OF KINETOPLASTID INFECTION
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Page/Page column 75; 76, (2018/07/29)
The present invention relates to a class of novel heterocyclic compounds, to pharmaceutical compositions comprising the compounds and their use in the treatment of kinetoplastid infections.
