- Novel tenofovir mixed ester-amide prodrugs
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The invention relates to novel tenofovir mixed ester-amide prodrugs or pharmaceutically acceptable salts thereof, a preparation method thereof, pharmaceutical compositions containing the prodrug compounds, and application of the prodrugs in preparation of drugs for treating virus infection such as hepatitis B virus (HBV) or human immunodeficiency virus (HIV) infection.
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Paragraph 0121-0123
(2020/04/17)
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- Synthesis and use of achiral oxazolidine-2-thiones in selective preparation of trans 2,5-disubstituted tetrahydrofurans
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The use of achiral N-acetyloxazolidine-2-thiones in the C-glycosylation of lactol acetates has allowed us to prepare with high diastereoselectivity the expected trans 2,5-disubstituted tetrahydrofurans. A study based on the role of the steric hindrance of the N-acetyloxazolidine-2-thiones is reported. Wiley-VCH Verlag GmbH & Co. KGaA, 2009.
- Jalce, Gael,Franck, Xavier,Figadere, Bruno
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body text
p. 378 - 386
(2009/09/25)
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- ANTIFUNGAL AGENTS
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Compounds of formula (I), and pharmaceutically acceptable salts thereof, may be used in therapy, for example as antifungal agents: (I) wherein: Rl, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. Certain compounds of formula (I) are also provided. Compounds of formula (T), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
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Page/Page column 46
(2008/06/13)
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- Conformational Study of Heteropentapeptides Containing an α-Ethylated α,α-Disubstituted Amino Acid: (S)-Butylethylglycine (=2-Amino-2-ethylhexanoic Acid) within a Sequence of Dimethylglycine (= 2-Aminoisobutyric Acid) Residues
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Heteropentapeptides containing the α-ethylated α,α-disubstituted amino acid (S)-butylethylglycine and four dimethylglycine residues, i.e., CF3CO-[(S)-Beg]-(Aib)4-OEt (4) and CF3CO-(Aib)2-[(S)-Beg]-(Aib)2OEt (7), were synthesized by conventional solution methods. In the solid state, the preferred conformation of 4 was shown to be both a right-handed (P) and a left-handed (M) 310-helical structure, and that of 7 was a right-handed (P) 310-helical structure. IR, CD, and 1H-NMR spectra revealed that the dominant conformation of both 4 and 7 in solution was the 310-helical structure. These conformations were also supported by molecular-mechanics calculations.
- Tanaka, Masakazu,Oba, Makoto,Imawaka, Naoto,Tanaka, Yoshitsugu,Kurihara, Masaaki,Suemune, Hiroshi
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- BENZAMIDINE DERIVATIVES SUBSTITUTED BY AMINO ACID AND HYDROXY ACID DERIVATIVES AND THEIR USE AS ANTI-COAGULANTS
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This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
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- Synthesis of 1,1-Diphenylaminoalcohols
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The synthesis of 2-amino-2-methyl-1,1-diphenyl-1-propanol (2a) and some of its aryl- and N-substituted derivatives from amino acid esters and Grignard compounds is described.The limits of this synthesis are reported, and so are other methods for the synthesis of amino alcohols.
- Bertram, Juergen
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