5835-28-9Relevant academic research and scientific papers
2 - Morpholine alkone salt and its preparation method, 2 - process for preparation of method (by machine translation)
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Paragraph 0095; 0097; 0106; 0116; 0125; 0134, (2018/10/24)
The invention relates to a 2 - morpholine alkone salt and its preparation method, 2 - process for preparation of method, which belongs to the technical field of the synthesis of pharmaceutical intermediates. The 2 - morpholine alkone salt preparation method, comprises the following steps: the amino protecting group with N - (2 - hydroxyethyl) glycine, catalyst in the reflux solvent heating reflux reaction, with amino protecting group prepared 2 - morpholone; said catalyst is paratoluene sulfonic acid or concentrated sulfuric acid; the amino protecting group with 2 - morpholone acidification is carried out by removing the protecting group 2 - morpholine alkone salt. 2 - Morpholone is 2 - morpholine alkone salt in the solvent in the reaction with the alkali. The invention of 2 - morpholine alkone salt and 2 - morpholone in the preparation method, the use of cheap raw material, short synthetic route, all reaction intermediate and final products do not need column chromatographic purification. The method of low cost, high efficiency, and high product purity. (by machine translation)
NMR study of the composition of aqueous 2-aminoethanol solution used for absorption of carbon dioxide from fuel gases
Talzi
, p. 927 - 931 (2016/09/04)
The compositions of aqueous 2-aminoethanol solutions used in industry for absorption of carbon dioxide resulting from combustion of natural gas have been determined by1H and13C NMR spectroscopy. The absorption process does not involve generally accepted paths of thermal decomposition of the absorbent in the reaction with carbon dioxide, but the main path is non-oxidative decomposition of 2-aminoethanol into ammonia and ethylene oxide. Splitting of the NMR signals of carbamate anion formed by reaction of 2-aminoethanol with carbon dioxide has been rationalized by specific structure of the anion due to intramolecular hydrogen bonding.
Liposomal bortezomib nanoparticles via boronic ester prodrug formulation for improved therapeutic efficacy in vivo
Ashley, Jonathan D.,Stefanick, Jared F.,Schroeder, Valerie A.,Suckow, Mark A.,Kiziltepe, Tanyel,Bilgicer, Basar
, p. 5282 - 5292 (2014/07/08)
In this study, we describe the development of liposomal bortezomib nanoparticles, which was accomplished by synthesizing bortezomib prodrugs with reversible boronic ester bonds and then incorporating the resulting prodrugs into the nanoparticles via surface conjugation. Initially, several prodrug candidates were screened based upon boronic ester stability using isobutylboronic acid as a model boronic acid compound. The two most stable candidates were then selected to create surface conjugated bortezomib prodrugs on the liposomes. Our strategy yielded stable liposomal bortezomib nanoparticles with a narrow size range of 100 nm and with high reproducibility. These liposomal bortezomib nanoparticles demonstrated significant proteasome inhibition and cytotoxicity against multiple myeloma cell lines in vitro and remarkable tumor growth inhibition with reduced systemic toxicity compared to free bortezomib in vivo. Taken together, this study demonstrates the incorporation of bortezomib into liposomal nanoparticles via reversible boronic ester bond formation to enhance the therapeutic index for improved patient outcome.
NANOPARTICLE DRUG DELIVERY SYSTEMS
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Page/Page column 43; 44, (2014/08/19)
The invention provides pharmaceutical compositions and method of using the compositions, wherein the compositions comprise liposomes or micelles that contain one or more targeting peptides and/or anticancer drugs. In various embodiments, the components of the liposomes can include a) a phospholipid and optionally a lipid that is not a phospholipid; b) a pegylated lipid; c) a peptide-ethylene glycol (EG)-lipid conjugate wherein the peptide is a targeting ligand, and d) one or more drug-conjugated lipid, encapsulated drugs, or a combination thereof. The peptide- EG-lipid conjugate can be, for example, a compound of Formula (I) or Formula (II). The ethylene glycol (EG) segments of the peptide-EG-lipid conjugate can be, for example, EG6 to about EG36; and the EG segment can be conjugated to one or more lysine moieties.
Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE)
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Page/Page column 7-8, (2010/10/20)
This invention relates to novel compounds, compositions containing the compounds, that inhibit dipeptidyl peptidase (especially DPP-IV) and neprilysin (NEP, neutral endopeptidase) as well as dipeptidyl peptidase (especially DPP-IV) and angiotensin converting enzyme (ACE) and/or dipeptidyl Peptidase (especially DPP-IV) and vasopeptidases (especially ACE and NEP). These compounds and pharmaceutical compositions thereof are useful for the treatment as well as the prevention of type 2 diabetes mellitus.
Apoptotic compounds
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, (2008/06/13)
The invention provides methods and compositions for enhancing apoptosis of pathogenic cells. The general method comprises the of contacting the cells with an effective amount of an AV peptoid, wherein the AV peptoid is a peptide comprising AX1, wherein X1is V, I or L, or a peptide mimetic thereof, which interacts with an Inhibitor of Apoptosis protein (IAP) as measured by IAP binding, procaspase-3 activation or promotion of apoptosis, wherein apoptosis of the pathogenic cells is enhanced. The subject compositions encompass pharmaceutical compositions comprising a therapeutically effective amount of a subject AV peptoid in dosage form and a pharmaceutically acceptable carrier, wherein the AV peptoid is a peptide comprising AX1, wherein X1is V, I or L, or a peptide mimetic thereof, which inhibits the activity of an Inhibitor of Apoptosis protein (IAP) as measured by IAP binding, procaspase-3 activation or promotion of apoptosis. The invention also provides assays for identifying agents which modulates the interaction of an AV peptoid with an IAP, active compounds identified in such screens and their use in the foregoing compositions and therapeutic methods.
Hydroxamate based inhibitors of adenylyl cyclase. Part 1: The effect of acyclic linkers on P-site binding
Levy, Daniel E,Marlowe, Charles,Kane-Maguire, Kim,Bao, Ming,Cherbavaz, Diana B.,Tomlinson, James E.,Sedlock, David M.,Scarborough, Robert M.
, p. 3085 - 3088 (2007/10/03)
The adenylyl cyclases (ACs) are a family of enzymes that are key elements of signal transduction by virtue of their ability to convert ATP to cAMP. The catalytic mechanism of this transformation proceeds through initial binding of ATP to the purine bindin
An amino nitrile intermediate for the preparation of 2-hydroxyethyl iminodiacetic acid
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, (2008/06/13)
A novel intermediate useful in the synthesis of 2-hydroxyethyl iminodiacetic acid is disclosed. The intermediate can be formed by contacting 2-hydroxyethyl amine with glycolonitrile to form an aminonitrile which can be hydrolyzed and contacted with additional glycolonitrile to form the nitrile intermediate which can be converted to 2-hydroxylethyl iminodiacetic acid via hydrolysis.
Modified peptide and peptide libraries with protease resistance, derivatives thereof and methods of producing and screening such
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, (2008/06/13)
Peptoids are provided which are polymers comprised of monomer units wherein the monomer units include at least some substitute amino acids and may include conventional amino acids. The peptoids can be synthesized in large numbers so as to provide libraries of peptoids which can be screened in order to isolate peptoids of desired biological activity. Although the peptoids may include amino acids, they preferably include only substituted amino acids and are designed in a manner so as to have a particular biological activity. Certain peptoids are designed to mimic as closely as possible the activity of known proteins. Other peptoids are designed so as to have greater or lesser activity than known proteins and may be designed so as to block known receptor sites and/or elicit a desired immunogenic response and thereby act as vaccines. In that the peptoids are comprised of substitute amino acids they can be designed to have structures which natural proteins cannot conform to. A range of different amino acid substitutes are disclosed, as are their methods of synthesis and methods of using such amino acid substitutes in the synthesis of peptoids and peptoid libraries. Methods of screening the libraries in order to obtain desired peptoids of a particular biological activity are also disclosed. The peptoids are preferably linked to a pharmaceutically active drug forming a conjugate with increased binding affinity to a particular biological receptor site.
Influence of the type of junction in DNA-3'-peptide nucleic acid (PNA) chimeras on their binding affinity to DNA and RNA
Greiner, Beate,Breipohl, Gerhard,Uhlmann, Eugen
, p. 2151 - 2159 (2007/10/03)
The automated on-line synthesis of DNA-3'-PNA (PNA = Polyamide Nucleic Acids) chimeras 1-3 is described, in which the 3'-terminal part of the oligonucleotide is linked to the aminoterminal part of the PNA either via a N-(2-mercaptoethyl)- (X = S), a N-(2-
