- Fullerene derivatives as dual inhibitors of HIV-1 reverse transcriptase and protease
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In the present study, we newly synthesized three types of novel fullerene derivatives: pyridinium-type derivatives trans-3a and 4a-5b, piperidinium-type derivative 9, and proline-type derivatives 10a-12. Among the assessed compounds, 5a, 10e, 10f, 10i, 11
- Yasuno, Takumi,Ohe, Tomoyuki,Kataoka, Hiroki,Hashimoto, Kosho,Ishikawa, Yumiko,Furukawa, Keigo,Tateishi, Yasuhiro,Kobayashi, Toi,Takahashi, Kyoko,Nakamura, Shigeo,Mashino, Tadahiko
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supporting information
(2020/11/20)
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- NOVEL METHODS OF USING NITRIC OXIDE DONOR COMPOUNDS FOR TREATMENT OF COVID-19 AND OTHER INFECTIOUS DISEASES
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The present invention provides novel methods of using nitric oxide donor compounds for treating infectious diseases, for example, COVID-19.
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Paragraph 00149
(2021/10/11)
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- AZETIDIN-3-YLMETHANOL DERIVATIVES AS CCR6 RECEPTOR MODULATORS
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The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders.
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Page/Page column 178
(2021/11/06)
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- COMPOUNDS AND METHODS FOR THE TREATMENT OF OCULAR DISORDERS
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Described herein are compositions and methods for the treatment of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory/ infections disease of the anterior surface of the eye. Said compositions and methods comprise keratolytic conjugate which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eye, ocular surface or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.
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Paragraph 00182; 00184-00185
(2020/10/27)
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- Direct anti Glycolate Aldol Reaction of Protected Chiral N-Hydroxyacetyl Thiazolidinethiones with Acetals Catalyzed by a Nickel(II) Complex
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The direct and stereocontrolled addition of (S)-4-isopropyl-N-(2-pivaloyloxyacetyl)-1,3-thiazolidine-2-thione to dialkyl acetals of aromatic and α,β-unsaturated aldehydes catalyzed by 2.5–5 mol-% of a nickel(II) complex permits the synthesis of diastereom
- Romo, Juan Manuel,Romea, Pedro,Urpí, Fèlix
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p. 6296 - 6305
(2019/11/05)
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- Cyclodextrin derivative inclusion compound for treating pancreatic cancer
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The invention relates to a cyclodextrin derivative inclusion compound for treating the pancreatic cancer. The existing ways of two active ingredients in the inclusion compound are different, wherein gemcitabine is bonded to a beta-cyclodextrin derivative in a chemical bonding mode first, and then the beta-cyclodextrin derivative further includes erlotinib to form a drug-loaded inclusion compound.Compared with a conventional cyclodextrin inclusion compound, and the beta-cyclodextrin derivative inclusion compound can constantly release the erlotinib and the gemcitabine in the body, so that theerlotinib and the gemcitabine maintain within the effective effect concentration range in the blood for a long time. Therefore, by means of the beta-cyclodextrin derivative inclusion compound, the drug combination curative effect can be obviously improved, and an unexpected excellent effect is generated.
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Paragraph 0032; 0035-0037
(2018/04/21)
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- Biomimetic synthesis, antibacterial activity and structure-activity properties of the pyroglutamate core of oxazolomycin
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Biomimetic intramolecular aldol reactions on oxazolidine templates derived from serine may be used to generate densely functionalised pyroglutamates, which are simpler mimics of the right hand side of oxazolomycin. Some of the compounds from this sequence exhibit in vivo activity against S. aureus and E. coli, suggesting that pyroglutamate scaffolds may be useful templates for the development of novel antibacterials, and cheminformatic analysis has been used to provide some structure-activity data.
- Angelov, Plamen,Chau, Yui Kwan Sonia,Fryer, Paul J.,Moloney, Mark G.,Thompson, Amber L.,Trippier, Paul C.
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scheme or table
p. 3472 - 3485
(2012/06/01)
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- An efficient synthesis of the precursor of AI-2, the signalling molecule for inter-species quorum sensing
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Autoinducer-2 (AI-2) is a signalling molecule for bacterial inter-species communication. A synthesis of (S)-4,5-dihydroxypentane-2,3-dione (DPD), the precursor of AI-2, is described starting from methyl glycolate. The key step was an asymmetric reduction of a ketone with (S)-Alpine borane. This new method was highly reproducible affording DPD for biological tests without contaminants. The biological activity was tested with the previously available assays and compared with a new method using an Escherichia coli reporter strain thus avoiding the use of the pathogenic Salmonella reporter.
- Ascenso, Osvaldo S.,Marques, Jo?o C.,Santos, Ana Rita,Xavier, Karina B.,Rita Ventura,Maycock, Christopher D.
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experimental part
p. 1236 - 1241
(2011/03/22)
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- New insights into poly(lactic- co -glycolic acid) microstructure: Using repeating sequence copolymers to decipher complex NMR and thermal behavior
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Sequence, which Nature uses to spectacular advantage, has not been fully exploited in synthetic copolymers. To investigate the effect of sequence and stereosequence on the physical properties of copolymers, a family of complex isotactic, syndiotactic, and atactic repeating sequence poly(lactic-co-glycolic acid) copolymers (RSC PLGAs) were prepared and their NMR and thermal behavior was studied. The unique suitability of polymers prepared from the bioassimilable lactic and glycolic acid monomers for biomedical applications makes them ideal candidates for this type of sequence engineering. Polymers with repeating units of LG, GLG and LLG (L = lactic, G = glycolic) with controlled and varied tacticities were synthesized by assembly of sequence-specific, stereopure dimeric, trimeric, and hexameric segmer units. Specifically labeled deuterated lactic and glycolic acid segmers were likewise prepared and polymerized. Molecular weights for the copolymers were in the range Mn = 12-40 kDa by size exclusion chromatography in THF. Although the effects of sequence-influenced solution conformation were visible in all resonances of the 1H and 13C NMR spectra, the diastereotopic methylene resonances in the 1H NMR (CDCl3) for the glycolic units of the copolymers proved most sensitive. An octad level of resolution, which corresponds to an astounding 31-atom distance between the most separated stereocenters, was observed in some mixed sequence polymers. Importantly, the level of sensitivity of a particular NMR resonance to small differences in sequence was found to depend on the sequence itself. Thermal properties were also correlated with sequence.
- Stayshich, Ryan M.,Meyer, Tara Y.
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supporting information; experimental part
p. 10920 - 10934
(2010/09/17)
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- Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors
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The present invention provides a compound of formula (1) wherein R1-R5, R25, R26, Y and X2 are defined as in claim 1. The compounds activate human peroxisome proliferator activated receptors (hPPARs) and arc useful for the treatment of associated disorders such as cardiovascular disease and hypercholesteremia.
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- Studies toward diazonamide A: Initial synthetic forays directed toward the originally proposed structure
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A brief introduction into the chemistry of diazonamide A (1) is followed by first-generation sequences to access the originally proposed structure for this unusual marine natural product. These explorations identified a route capable of delivering a model compound possessing the complete heteroaromatic core of the natural product, highlighting in the process several unanticipated synthetic challenges which led both to new methodology as well as an improved synthetic plan that was successfully applied to fully functionalized intermediates.
- Nicolaou,Snyder, Scott A.,Huang, Xianhai,Simonsen, Klaus B.,Koumbis, Alexandros E.,Bigot, Antony
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p. 10162 - 10173
(2007/10/03)
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- Intramolecular Diels-Alder reactions of diester-tethered trienes. Synthesis of medium ring-containing carbocycles and heterocycles
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Intramolecular Diels-Alder reactions of cyclohexane-1,2- dicarboxylic anhydride-derived diester-tethered trienes are described. The stereoselectivities of most of the cycloaddition processes studied may be rationalised in terms of an preferred 'inside'-oriented diene giving rise to an endo-transition state.
- Craig, Donald,Ford, Mark J.,Gordon, Richard S.,Stones, James A.,White, Andrew J. P.,Williams, David J.
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p. 15045 - 15066
(2007/10/03)
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- Intramolecular Diels-Alder reactions of tethered homo- and heterotrienes. Synthesis of substituted cyclohexenes and six-membered heterocycles
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Intramolecular Diels-Alder reactions of a number of diester-tethered trienes are reported. All-carbon trienes 5, 7 and 13 show little or no selectivity for trans-fused products. Heterotrienes 21 and 25 exhibit good to excellent cis-selectivity, with low to good selectivity for one of the two cis-fused isomers.
- Craig, Donald,Gordon, Richard S.
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p. 8337 - 8340
(2007/10/03)
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- Preparation of protected 2-hydroxymethyl isocyanates: An application to agricultural synthesis
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The preparation of N-benzyloxymethyl isocyanate (4) and t-butyldiphenylsiloxymethyl isocyanate (9) via the diphenylphosphoryl azide modified Curtius rearrangement is described. These isocyanates have been amployed in the synthesis of a herbicide metabolit
- Roth,McClymont
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p. 411 - 420
(2007/10/02)
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- Claisen Rearrangements of Enantiomerically Pure C3-(Acyloxy)-(E)-vinylsilanes
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The Ireland ester Claisen rearrangement of chiral (R)- and (S)-(acyloxy)-(E)-vinylsilanes gives access to a wide range of α-chiral-β-silyl-(E)-hexenoic acids with useful levels of diastereoselectivity for both the 2,3-syn and 2,3-anti diastereomers as ill
- Sparks, Michelle A.,Panek, James S.
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p. 3431 - 3438
(2007/10/02)
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