1135-39-3Relevant academic research and scientific papers
Novel degradable poly(ethylene glycol) hydrogels for controlled release of protein
Zhao,Harris
, p. 1450 - 1458 (1998)
Hydrogels have become increasingly important in the biomedical field. This paper describes synthesis and characterization of two types of novel degradable poly(ethylene glycol) (PEG) hydrogels with potential utility as delivery carriers for bioactive drug
Stereoselective Synthesis of cis-2,5-Disubstituted Tetrahydrofuran-3-ones via an Acyl Radical Cyclization
Andrew Evans, P.,Roseman, Jamine D.
, p. 31 - 34 (1995)
Treatment of the acyl selenide 7 with triphenyltin hydride and triethylborane generates the acyl radical which undergoes 5-exo trigonal cyclization to afford the 2,5-disubstituted tetrahydrofuran-3-ones 10a/b in 97percent yield as a 94:6 mixture of diastereoisomers.
CARRIER-LINKED PRODRUGS HAVING REVERSIBLE CARBOXYLIC ESTER LINKAGES
-
Paragraph 0267-0268, (2020/05/30)
The invention provides a carrier-linked prodrugs, wherein the biologically active moieties comprise at least one carboxylic acid and wherein the linkage between the drug moiety and linker is in the form of an ester wherein the hydroxyl group required for ester formation is provided by the linker moiety and the carboxyl group required for ester formation is provided by the drug moiety. The hydroxyl group of the linker is sterically hindered by the presence of an alkyl or aryl group on the carbon directly bound to or adjacent to the carbon carrying the hydroxyl group (a-carbon). The steric effect of the alkyl or aryl group enables greater control of the rate of hydrolytic degradation of such carrier-linked prodrugs.
Sustained release composition of prostacyclin
-
Page/Page column 63; 64, (2018/03/28)
The present invention relates to sustained release compositions of prostacyclin, as well as uses thereof, in particular for the prevention and/or treatment of pulmonary arterial hypertension.
Carrier-linked treprostinil prodrugs
-
Page/Page column 95; 96, (2017/02/28)
The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).
SUSTAINED RELEASE COMPOSITION OF PROSTACYCLIN
-
Page/Page column 87, (2013/03/26)
The present invention relates to sustained release compositions of prostacyclin, as well as uses thereof, in particular for the prevention and/or treatment of pulmonary arterial hypertension.
CARRIER-LINKED TREPROSTINIL PRODRUGS
-
Page/Page column 119; 120, (2013/03/26)
The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).
CARRIER-LINKED PRODRUGS HAVING REVERSIBLE CARBOXYLIC ESTER LINKAGES
-
Page/Page column 84, (2013/03/26)
The invention provides a carrier-linked prodrugs, wherein the biologically active moieties comprise at least one carboxylic acid and wherein the linkage between the drug moiety and linker is in the form of an ester wherein the hydroxyl group required for ester formation is provided by the linker moiety and the carboxyl group required for ester formation is provided by the drug moiety. The hydroxyl group of the linker is sterically hindered by the presence of an alkyl or aryl group on the carbon directly bound to or adjacent to the carbon carrying the hydroxyl group (α-carbon). The steric effect of the alkyl or aryl group enables greater control of the rate of hydrolytic degradation of such carrier-linked prodrugs.
Selective esterifications of primary alcohols in a water-containing solvent
Wang, Yong,Aleiwi, Bilal A.,Wang, Qinghui,Kurosu, Michio
supporting information, p. 4910 - 4913,4 (2012/12/12)
Oxyma and an oxyma derivative, (2,2-dimethyl-1,3-dioxolan-4-yl)methyl 2-cyano-2-(hydroxyimino)acetate (5b), displayed a remarkable effect on selective esterifications of primary alcohols. A wide range of carboxylic acids could be esterified with primary alcohols by using EDCI, NaHCO3, and Oxyma or Oxyma derivative 5b in 5% H2O-CH3CN. Oxyma derivative 5b is particularly useful, since it could be removed after the reaction via a simple basic or an acidic aqueous workup procedure.
Selective esterifications of primary alcohols in a water-containing solvent
Wang, Yong,Aleiwi, Bilal A.,Wang, Qinghui,Kurosu, Michio
supporting information, p. 4910 - 4913 (2013/01/15)
Oxyma and an oxyma derivative, (2,2-dimethyl-1,3-dioxolan-4-yl)methyl 2-cyano-2-(hydroxyimino)acetate (5b), displayed a remarkable effect on selective esterifications of primary alcohols. A wide range of carboxylic acids could be esterified with primary alcohols by using EDCI, NaHCO3, and Oxyma or Oxyma derivative 5b in 5% H2O-CH3CN. Oxyma derivative 5b is particularly useful, since it could be removed after the reaction via a simple basic or an acidic aqueous workup procedure.
