207305-60-0Relevant articles and documents
Pleuromutilin compounds for treating novel coronavirus pneumonia secondary bacterial infectious diseases
-
Paragraph 0095-0097; 0119-0120, (2020/09/23)
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.
NOVEL ANTIBACTERIAL 3"-DERIVATIVES OF 4,6-DISUBSTITUTED 2,5-DIDEOXYSTREPTAMINE AMINOGLYCOSIDE ANTIBIOTICS
-
Page/Page column 198; 229, (2020/07/05)
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.
Preparation method of pradimicin antibiotics
-
Paragraph 0065-0067, (2019/01/08)
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.
STIMULUS-RESPONSIVE POLY(LACTIC-CO-GLYCOLIC)-BASED POLYMERS AND NANOPARTICLES FORMED THEREFROM
-
Page/Page column 21, (2016/12/12)
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.
Light-triggered intramolecular cyclization in poly(lactic- co -glycolic acid)-based polymers for controlled degradation
Olejniczak, Jason,Chan, Minnie,Almutairi, Adah
, p. 3166 - 3172 (2015/06/08)
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.
Tandem Ugi MCR/mitsunobu cyclization as a short, protecting-group-free route to benzoxazinones with four diversity points
Banfi, Luca,Basso, Andrea,Giardini, Lorenzo,Riva, Renata,Rocca, Valeria,Guanti, Giuseppe
experimental part, p. 100 - 109 (2011/03/21)
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.
A paradigm for solvent and temperature induced conformational changes
Shpasser, Dina,Balazs, Yael S.,Kapon, Moshe,Sheynis, Tania,Jelienk, Raz,Eisen, Moris S.
supporting information; experimental part, p. 8285 - 8289 (2011/08/07)
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
ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
-
Page/Page column 70, (2011/04/26)
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.
ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
-
Page/Page column 67-68, (2011/04/26)
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.
ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
-
Page/Page column 94-95, (2011/04/26)
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.