- INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING ALPHA-V-BETA-3
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The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-3 integrin antagonists to target cells expressing alpha-V-beta-3.
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Page/Page column 45; 46
(2013/08/15)
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- Efficient synthesis of substituted 3-acyl-3,4-dihydrobenzo[d][1,2,3]triazines
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Acylated o-triazenylbenzylamines were cyclized to give 3-acyl-3,4-dihydrobenzo[d][1,2,3]triazines in good yields. Thus, a novel cyclization via a Jacobsen indazole-type reaction to aminoindazoles is observed in this context.
- Reingruber, Rüdiger,Vanderheiden, Sylvia,Muller, Thierry,Nieger, Martin,Es-Sayed, Mazen,Br?se, Stefan
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scheme or table
p. 3439 - 3442
(2009/09/25)
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- NOVEL COMPOUNDS
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The invention provides compounds of formula (I) wherein m, R1, n, R2, q, X, Y, Z, t, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their
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Page/Page column 31-32
(2008/06/13)
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- Anti-Helicobacter pylori agents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and some structurally rigid derivatives
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In order to find a new class of anti-Helicobacter pylori (H. pylori) agents, a series of 4-[(3-acetamido)phenyl]-2-(substituted guanidino)thiazoles and some structurally rigid analoges were synthesized and evaluated for antimicrobial activity against H. pylori. Among the compounds obtained, high anti-H. pyrori activities were observed in benzyl derivative 34 (MIC = 0.025 μg/mL) and phenethyl derivatives 35 and 36 (MIC = 0.037 μg/mL and 0.017 μg/mL). Though alkyl derivatives generally showed lower activity, the 2-methoxyethyl derivative 28 preserved significant activity (MIC = 0.32 μg/mL) and also exhibited more potent gastric antisecretory activity than ranitidine. Structural restriction by bridging between the thiazole and the phenyl rings with an alkyl chain did not improve the activity in this series.
- Katsura,Tomishi,Inoue,Sakane,Matsumoto,Morinaga,Ishikawa,Takasugi
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p. 3315 - 3321
(2007/10/03)
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- AROMATIC HYDROXYLATION OF BENZYLAMIDES BY POTASSIUM SUPEROXIDE
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N-benzylamides react with potassium superoxide in benzene in presence of 18-crown-6 ether to give ortho and para hydroxylated products.A mechanism is proposed for this reaction, involving the nucleophilic attack of superoxide anion to amide carbonyl and hydrogen abstraction from benzyle methylene by the substrate-superoxide adduct.
- Galliani, Guido,Rindone, Bruno
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p. 2313 - 2318
(2007/10/02)
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