专利号:US-8372881-B2 优先权日:2005-06-20 标题 :Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis and use 发明人:ZERANGUE NOA; JANDELEIT BERND; LI YUNXIAO; GALLOP MARK A 权利人:XENOPORT INC; ZERANGUE NOA; JANDELEIT BERND; LI YUNXIAO; GALLOP MARK A 摘要:Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.
专利号:US-2008227851-A1 优先权日:2007-03-12 标题 :Laulimalide and laulimalide analogs 发明人:WENDER PAUL A 权利人:WENDER PAUL A 摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.
专利号:US-11279734-B2 优先权日:2017-12-01 标 题:Solution-phase affinity selection of inhibitors from combinatorial peptide libraries 发明人:PENTELUTE BRADLEY L; TOUTI FAYCAL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., K D of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly). These inventive peptides were rapidly generated and identified using novel methods described herein comprising combinatorial peptide synthesis and/or solution affinity selection.
专利号:US-2007128285-A1 优先权日:2005-07-12 标题 :Pharmaceutical composition for oral administration 发明人:JIN CHIKARA; TATSUMI NOBORU; DAIRAKU MASATAKE; FUKUSHIMA FUMINORI; SHIMIZU TOSHIO; TOGASHI MITSUO; NINOMIYA HIROSHI 权利人:JIN CHIKARA; TATSUMI NOBORU; DAIRAKU MASATAKE; FUKUSHIMA FUMINORI; SHIMIZU TOSHIO; TOGASHI MITSUO; NINOMIYA HIROSHI 摘要:Provided is a pharmaceutical composition for oral administration containing a 5-HT. 3 receptor antagonist, which is suitable for self-medication because of good preservation stability, low synthesis, good uniformity and good external appearance, and good smoothness in throat, and easiness to be taken. Concretely, it is a jellied pharmaceutical composition for oral administration containing a 5-HT. 3 receptor antagonist, a gelatinizing agent, and water; and having a pH of 7 or less. In particular, there is provided the pharmaceutical composition, where the gelatinizing agent is carrageenan, pectin, agar, alginic acid, sodium alginate, gelatin, manna, Kodak, konjakmannan, glucomannan, chitosan, xanthan gum, tamarind seed polysaccharide, gellan gum, karaya gum, or cassia gum, or preferably the pharmaceutical composition further containing a thickener.
专利号:US-7777070-B2 优先权日:2005-06-20 标题:Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis and use
专利号:US-2010036148-A1 优先权日:2005-06-20 标题:Acyloxyalkyl Carbamate Prodrugs of Tranexamic Acid, Methods of Synthesis and Use
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