- Minimalistic β-sitosterol based designer surfactants for efficient cross-coupling in water
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In this contribution, we report about the synthesis, the aggregation properties and their application in cross-coupling catalysis of two new designer surfactants comprising a rigid hydrophobic portion based on β-sitosterol directly linked by an etheric bond to methyl polyoxoethylene chains. The proposed amphiphilic compounds represent a minimalistic approach with respect to the Lipshutz's third generation designer surfactant Nok. The amphiphiles displayed improved chemical stability, shorter synthesis, and good properties in Pd-catalyzed cross-coupling reactions in water under mild conditions, as compared with other neutral commercially available surfactants.
- Fabris, Fabrizio,Frigatti, Davide,Lorenzetto, Tommaso,Scarso, Alessandro
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supporting information
(2022/03/16)
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- Naloxegol Oxalate and Solid Dispersion thereof
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The present invention relates to solid dispersion of Naloxegol oxalate. Further, the present invention relates to an improved process for Naloxegol oxalate and intermediates thereof.
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- triAZOLOtriAZINE DERIVATIVES AS A2A RECEPTOR ANTAGONISTS
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The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyperfunctioning, such as certain types cancers. Compounds of formula (1) and methods of preparing the compounds are disclosed in the invention.
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Page/Page column 54
(2020/01/24)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF (5Α,6Α)-17-ALLYL-6-(2,5,8,11,14,17,20- HEPTAOXADOCOSAN-22-YLOXY)-4,5-EPOXYMORPHINAN-3,14-DIOL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
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The present invention relates to an improved process for the preparation of (5α, 6α)-17-allyl-6-(2, 5, 8, 11, 14, 17, 20- heptaoxadocosan-22-yloxy)-4, 5-epoxymorphinan-3, 14-diol which is represented by the following structural formula-1 or its pharmaceut
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- NALOXEGOL OXALATE AND SOLID DISPERSION THEREOF
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The present invention relates to solid dispersion of Naloxegol oxalate. Further, the present invention relates to an improved process for Naloxegol oxalate and intermediates thereof.
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- Supramolecular graft copolymers in moderately polar media based on hydrogen-bonded aromatic oligoamide units
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By exploiting hetero-complementary aromatic oligoamide units containing hextuple hydrogen bonds, supramolecular graft copolymers were successfully constructed in moderately polar media.
- Pan, Xusong,Chen, Chao,Peng, Jiang,Yang, Yongan,Wang, Yinghan,Feng, Wen,Deng, Pengchi,Yuan, Lihua
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supporting information
p. 9510 - 9512
(2012/11/06)
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- Pharmaceutical compositions of insulin drug-oligomer conjugates and methods of treating diseases therewith
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Pharmaceutical compositions that include insulin, an insulin drug-oligomer conjugate, a fatty acid component, and a bile salt component or a bile salt component without a fatty acid component are described. The insulin drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component, when together, can be present in a weight-to-weight ratio of between 1:15 and 15:1. Methods of treating an insulin deficiency in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.
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- Calcitonin drug-oligomer conjugates, and uses thereof
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Calcitonin drug-oligomer conjugates that include a calcitonin drug coupled to an oligomer including a single polyalkylene glycol moiety consisting of between 4 and 10 polyalkylene glycol subunits are disclosed. Pharmaceutical compositions including such conjugates and methods of treating bone disorders by administering such conjugates are also disclosed.
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- NMR relaxometric study of new Gd(III) macrocyclic complexes and their interaction with human serum albumin.
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Five novel Gd(iii) complexes based on the structure of the heptadentate macrocyclic 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid (DO3A) ligand have been synthesized and their (1)H and (17)O NMR relaxometric properties investigated in detail. The co
- Botta, Mauro,Quici, Silvio,Pozzi, Gianluca,Marzanni, Giovanni,Pagliarin, Roberto,Barra, Serena,Geninatti Crich, Simonetta
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p. 570 - 577
(2007/10/03)
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- Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same
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Methods for synthesizing proinsulin polypeptides are described that include contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also provided as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates and other pro-polypeptide-oligomer conjugates are also provided.
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- Mixtures of growth hormone drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
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A mixture of conjugates in which each conjugate in the mixture comprises a growth hormone drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed.
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- Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
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A mixture of conjugates in which each conjugate in the mixture comprises an insulin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may also be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may also result in less inter-subject variability than polydispersed mixtures of similar conjugates.
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- Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same
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Methods for synthesizing proinsulin polypeptides are described that include contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also provided as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates and other pro-polypeptide-oligomer conjugates are also provided.
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- Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
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A mixture of conjugates in which each conjugate in the mixture comprises a calcitonin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may lower serum calcium levels in a subject by 10, 15 or even 20 percent or more. Moreover, the mixture may be more effective at surviving an in vitro model of intestinal digestion than non-conjugated calcitonin. Furthermore, the mixture may exhibit a higher bioavailability than non-conjugated calcitonin.
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