- Pleuromutilin compounds for treating novel coronavirus pneumonia secondary bacterial infectious diseases
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The present invention relates to novel pleuromutilin compounds, and a pharmaceutical composition and a use method thereof. Furthermore, the present invention also relates to a therapeutic method for treating bacterial infections, including infections caused by resistant microorganisms including multiple resistant microorganisms. The method and the compounds for treating secondary bacterial infectious diseases of novel coronavirus (COVID-19 or SARS-Cov-2) pneumonia, and the pharmaceutical composition of the compounds are especially provided, and provide scientific and technological support forwin-win new coronapneumonia epidemic prevention and control obstructing warfare.
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Paragraph 0095-0097; 0119-0120
(2020/09/23)
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- NOVEL ANTIBACTERIAL 3"-DERIVATIVES OF 4,6-DISUBSTITUTED 2,5-DIDEOXYSTREPTAMINE AMINOGLYCOSIDE ANTIBIOTICS
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The present invention relates to novel aminoglycoside compounds having antimicrobial properties and being suitable, for example, as therapeutic agents for use in the treatment of mammalian disease and in particular to novel therapeutic agents suitable for use in the treatment of microbial infection in mammals. The present invention further relates to the use of pharmaceutical compositions comprising said agents in the treatment of medical conditions in mammals, in particular in the treatment of microbial infection. The agents and pharmaceutical compositions of the invention are of particular relevance in the treatment of diseases associated with antibiotic-resistant microbes. The invention further relates to compounds for use in the treatment of diseases whose treatment is made otherwise difficult due to antibiotic-class-related bacterial resistance and provides novel therapeutic agents suitable for use in the treatment of multidrug-resistant (MDR) infections.
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Page/Page column 198; 229
(2020/07/05)
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- Preparation method of pradimicin antibiotics
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The invention provides a preparation method of pradimicin antibiotics, belonging to the field of pharmaceutical chemistry and pharmaceutical engineering. The preparation method comprises the followingsteps: freeing of sisomicin, protection of amino, selective introduction of protective groups, deprotection of amino, and the like. The preparation method is suitable for industrial production, thushaving good market prospects.
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Paragraph 0065-0067
(2019/01/08)
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- STIMULUS-RESPONSIVE POLY(LACTIC-CO-GLYCOLIC)-BASED POLYMERS AND NANOPARTICLES FORMED THEREFROM
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PLGA-based polymers include pendant nucleophiles protected with photocleavable protecting groups. Upon deprotection, the polymers degrade rapidly via intramolecular cyclization into small molecules. The polymer may be formulated as a nanoparticle, with an encapsulated payload, which may be an imaging agent, a bioactive agent or a pharmaceutical agent.
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Page/Page column 21
(2016/12/12)
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- Light-triggered intramolecular cyclization in poly(lactic- co -glycolic acid)-based polymers for controlled degradation
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Polylactide (PLA) and poly(dl-lactide-co-glycolide) (PLGA) are two prominent FDA-approved polymers because of their useful biodegradation into largely innocuous substances. Their hydrolytic degradation is slow and offers minimal control over degradation kinetics, especially in the minutes time scale. However, molecular engineering of their structures could allow triggered degradation. We have synthesized, by ring-opening polymerization (ROP), a series of PLGA-based polymers containing pendant nucleophiles protected with photocleavable groups. Upon deprotection, two of the polymers degrade rapidly via intramolecular cyclization into small molecules. Nanoparticles formulated from these polymers undergo rapid structural changes in response to UV light. This work introduces a novel polymeric structure to enable rapid on-demand degradation and expands the library of polymers that degrade by cyclization.
- Olejniczak, Jason,Chan, Minnie,Almutairi, Adah
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p. 3166 - 3172
(2015/06/08)
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- Tandem Ugi MCR/mitsunobu cyclization as a short, protecting-group-free route to benzoxazinones with four diversity points
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A tandem Ugi/Mitsunobu protocol, starting from o-aminophenols, α-hydroxy acids, amines and aldehydes gives benzo[b][1,4]oxazin-3-ones of general formula 1 in two high-yielding steps, with the introduction of up to four diversity inputs. The mildness of the methodology allows the stereospecific synthesis of enantiomerically pure products as well as the introduction of additional functional groups. The overall procedure can also be carried out in a one-pot manner. A tandem Ugi/Mitsunobu protocol, starting from o-aminophenols and α-hydroxy acids, gives benzo[b][1,4]oxazin-3-ones, with the introduction of up to four diversity inputs, in two high-yielding steps. The procedure may be carried out in a one-pot fashion and has a very broad scope, also allowing the synthesis of enantiomerically pure products.
- Banfi, Luca,Basso, Andrea,Giardini, Lorenzo,Riva, Renata,Rocca, Valeria,Guanti, Giuseppe
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experimental part
p. 100 - 109
(2011/03/21)
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- A paradigm for solvent and temperature induced conformational changes
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The complex conformational dependency on environment of Boc-amine (see scheme) has been investigated. This model organic molecule has many features applicable to areas of chemistry, biology, physics, and computational chemistry. It is soluble in both non-polar and polar solvents, conformationally heterogeneous, and capable of supramolecular assembly. Copyright
- Shpasser, Dina,Balazs, Yael S.,Kapon, Moshe,Sheynis, Tania,Jelienk, Raz,Eisen, Moris S.
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supporting information; experimental part
p. 8285 - 8289
(2011/08/07)
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- ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): (Formula (I)), including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2, R3, Z1 and Z2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 70
(2011/04/26)
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- ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): (Formula (I)), including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2, R3, Z1 and Z2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 67-68
(2011/04/26)
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- ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Compounds having antibacterial activity are disclosed. The compounds have one of the following structures (I) or (II): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2, R3 and Z1 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 94-95
(2011/04/26)
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- ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): (I) including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Ql, Q2, Rl, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 56
(2010/04/28)
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- ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Compounds having antibacterial activity are disclosed. The compounds have the following structure (I) or (II): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 100
(2010/12/17)
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- ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): (I) including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 56
(2010/04/28)
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- TREATMENT OF URINARY TRACT INFECTIONS WITH ANTIBACTERIAL AMINOGLYCOSIDE COMPOUNDS
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A method for treating a urinary tract infection in a mammal in need thereof is disclosed, the method comprising administering to the mammal an effective amount of an antibacterial aminoglycoside compound.
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Page/Page column 75
(2010/12/17)
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- DNA sequence selectivity of hairpin polyamide turn units
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A class of hairpin polyamides linked by 3,4-diaminobutyric acid, resulting in a β-amine residue at the turn unit, showed improved binding affinities relative to their α-amino-γ-turn analogs for particular sequences. We incorporated β-amino-γ-turns in six-
- Farkas, Michelle E.,Li, Benjamin C.,Dose, Christian,Dervan, Peter B.
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supporting information; experimental part
p. 3919 - 3923
(2010/03/02)
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- ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Compounds of structure (I): having antibacterial activity are disclosed, including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 72
(2009/06/27)
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- Cyclic hexapeptides having antibiotic activity
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This invention relates to new polypeptide compound represented by general formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
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- Covalent capture purification of polypeptides after SPPS via a linker removable under very mild conditions
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The covalent purification of polypeptides possessing an N-terminal cysteine or threonine residue via formation of a thiazolidine or oxazolidine with an aldehyde-functionalized-resin has been successfully demonstrated. To extend the applicability of this approach to any possible N-terminal residue, a special linker derived from (S)-4-amino-2-hydroxy-butyric acid was incorporated into peptidyl-resin. This linker represents the connecting point between the capture unit (cysteine) useful for the isolation of the desired polypeptide and the desired N-terminus. The target polypeptide was recovered by periodate oxidation, which cleaved the covalent bond between the linker and the last residue of polypeptide under very mild conditions.
- Vizzavona, Jean,Villain, Matteo,Rose, Keith
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p. 8693 - 8696
(2007/10/03)
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