- HYDROXAMATE COMPOUNDS AS ANTAGONISTS OF THE ADENOSINE A2A RECEPTOR
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The present invention relates to compounds of formula I shown below: (I) wherein R1, R2 and R3 are each as defined in the application. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions in which adenosine A2a receptor activity is implicated, such as, for example, cancer.
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Paragraph 00500; 00549
(2021/01/23)
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- Substituted benzimidazole compound and composition with compound
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The invention provides a substituted benzimidazole compound and a composition with the compound. The substituted benzimidazole compound is a compound of formula (I) as shown in the specification, or apharmaceutically acceptable salt, prodrug, aquo-complex or solvent compound, polycrystalline type compound, stereisomer or isotope variant of the compound. The compound provided by the invention canbe adopted to treat and/or prevent related diseases caused by MEK (Methyl Ethyl Ketone), such as excessive proliferative diseases, pancreatitis, kidney illness, blastocyte cell transplantation and angiogenesis or angiopoiesis related diseases.
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Paragraph 0164-0167; 0170-0171
(2019/03/31)
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- Heartleaf houtluynia derivatives and their use in medicine
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The invention relates to houttuynia cordata derivatives or esters thereof, or an enantiomer or a diastereomer, stereomer, tautomer, hydate, solvate, predrug, or pharmaceutically acceptable salt. In addition, the invention further relates to a preparation method of the houttuynia cordata derivatives, and an application of the houttuynia cordata derivatives in a drug; and the invention further relates to a pharmaceutical composition of the compound, and applications in preparing an antibacterial and anti-virus drug especially used for treating various urinary system diseases, and the advantages are that the water solubility is good, the bioavailability is high, the purity is high, and the toxic and side effects and the stimulation effect due to low purity can be greatly reduced.
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Paragraph 0336; 0337
(2018/02/04)
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- Prodrug design for the potent cardiovascular agent Nω- hydroxy-l-arginine (NOHA): Synthetic approaches and physicochemical characterization
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Nω-Hydroxy-l-arginine (NOHA) - the physiological nitric oxide precursor - is the intermediate of NO synthase (NOS) catalysis. Besides the important fact of releasing NO mainly at the NOS-side of action, NOHA also represents a potent inhibitor of arginases, making it an ideal therapeutic tool to treat cardiovascular diseases that are associated with endothelial dysfunction. Here, we describe an approach to impart NOHA drug-like properties, particularly by wrapping up the chemically and metabolically instable N-hydroxyguanidine moiety with different prodrug groups. We present synthetic routes that deliver several more or less highly substituted NOHA derivatives in excellent yields. Versatile prodrug strategies were realized, including novel concepts of bioactivation. Prodrug candidates were primarily investigated regarding their hydrolytic and oxidative stabilities. Within the scope of this work, we essentially present the first prodrug approaches for an interesting pharmacophoric moiety, i.e., N-hydroxyguanidine. The Royal Society of Chemistry 2011.
- Schade, Dennis,Kotthaus, Juerke,Klein, Nikola,Kotthaus, Joscha,Clement, Bernd
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supporting information; experimental part
p. 5249 - 5259
(2011/08/10)
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- Design of a "new motif" with β-amino acids and α-aminoxy acids: Synthesis of hybrid peptides with 12/10-helix
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(Figure Presented) Hybrid peptides are prepared from a C-linked carbo-β-amino acid ester (R-β-Caa) and an α-aminoxy acid (R-Ama) derived from S-lactic acid. Extensive NMR (in CDCl3 solution), CD, and MD studies on the tetra- and hexapeptides led to identification of robust 12/10-mixed helices. The dipeptide repeat having an R-β-Caa and an R-Ama thus provides a "new motif" to realize a 12/10-mixed helix, for the first time, in oligomers containing R-Ama. To understand the impact of side chains in the mixed helix formation, R-β-Caa/Ama (with no substitution in Ama) and S-β-hAla/R-Ama oligomers were investigated. NMR studies revealed the existence of 12/10-helices in these hybrid peptides, and the side chains of monomers were found to have a profound influence on their stabilities. These observations imply that the propensity of β-amino acid to prefer a mixed 12/10-helix governs the structural behavior in these peptides. The structural consequences of the lone-pair repulsion between nitrogen and oxygen atoms result in a new and interesting structural motif which behaves like "pseudo" β3,β2-peptides in generating 12/10-mixed helices.
- Sharma, Gangavaram V. M.,Manohar, Vennampalli,Dutta, Samit K.,Subash, Velaparthi,Kunwar, Ajit C.
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p. 3689 - 3698
(2008/09/19)
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- 1,3-Disubstituted-2- thioxo-imidazolidine-4,5-dione derivatives useful in the treatment of atherosclerosis
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Antiatherosclerotic compounds of Formula I are provided: wherein: R is lower alkyl, alkenyl, alkynyl, or —O—(CH2)n—COOR′; R′ is lower alkyl; n is an integer of 1-3; Ar is phenyl, or phenyl substituted with one or more of halogen, lower alkyl, alkenyl, alkynyl, alkoxy, perfluoroalkyl, perfluoroalkoxy, or alkylthio; and pharmaceutically acceptable salts thereof.
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- ORGANIC SYNTHESES WITHOUT SOLVENT : PREPARATION OF ALKOXYPHTHALIMIDES AND OF ALKOXYLAMINES
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Alkoxyphthalimides are prepared by alkylation of N-hydroxyphthalimide under solid-liquid phase transfer catalysis without solvent.When conversion of alkoxyphthalimides into alkoxylamines is nearly complete, neat hydrazine hydrate is added at room temperature.
- Galons, Herve,Fiet, Jean,Combet-Farnoux, Claude,Miocque, Marcel,Bram, Georges
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p. 521 - 528
(2007/10/02)
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