62631-17-8Relevant academic research and scientific papers
A synthetic approach to 5/5/6-polycyclic tetramate macrolactams of the discodermide type
Bodenschatz, Kevin,St?ckl, Julia,Winterer, Markus,Schobert, Rainer
, (2021/05/31)
A flexible synthetic route to the 16-membered tetramate-embedding macrocyclic scaffold present in various polycyclic tetramate macrolactams (PTMs) was developed which differs from the seminal synthesis of ikarugamycin by Boeckman Jr. in protecting groups and the order of connections. We also devised a short approach to various stereoisomers of the 5/5/6-tricarbocyclic motif found in discodermide and other PTMs, starting from the Weiss’ diketone.
A high optical activity chiral sea natural product synthesis method
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Paragraph 0057; 0058, (2017/08/25)
The invention discloses a synthetic method for a chiral marine natural product with high optical activity. According to the method, a marine natural product with the high optical activity is prepared by adopting chiral amino acid. The method specifically comprises the following steps: first, using L-ornithine monohydrochloride and D-ornithine monohydrochloride as starting raw materials, and performing copper ion complexing, amino protecting, esterifying, urea forming and cyclizing to obtain an intermediate 5; then, using N-methylpyrrole as a raw material, and performing electrophilic reaction, hydrolyzing, acidizing and acylating in sequence to obtain an intermediate 9; finally, enabling the intermediate 5 and the intermediate 9 to react to prepare corresponding chiral natural products, namely (S)-midpacamide or (R)-midpacamide. According to the synthetic method, synthetic steps are simple; the operation is simple and convenient; reaction conditions are mild; the original structure of the product prepared by the provided synthetic route is kept; the optical purity of the obtained marine natural product is greater than 99 percent; the marine natural product has a wide application prospect.
Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
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Paragraph 2510, (2015/09/22)
The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES
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, (2012/04/23)
The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
Organic Compounds
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Page/Page column 111, (2010/06/14)
A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
RGD mimetics containing a central hydantoin scaffold: α(v)β3 vs α(IIb)β3 selectivity requirements
Peyman, Anusch,Wehner, Volkmar,Knolle, Jochen,Stilz, Hans Ulrich,Breipohl, Gerhard,Scheunemann, Karl-Heinz,Carniato, Denis,Ruxer, Jean-Marie,Gourvest, Jean-Francois,Gadek, Thomas R.,Bodary, Sarah
, p. 179 - 182 (2007/10/03)
The synthesis of a series of RGD mimetic α(v)β3 antagonists containing a hydantoin scaffold is shown. The results demonstrate some of the structural requirements for the design of selective α(v)β3 antagonists (vs α(IIb)β3)
