63228-51-3Relevant academic research and scientific papers
Thermoresponsive Alignment Media in NMR Spectroscopy: Helix Reversal of a Copolyaspartate at Ambient Temperatures
Schwab, Mira,Schmidts, Volker,Thiele, Christina M.
, p. 14373 - 14377 (2018)
Poly(aspartic acid esters) are known to form either right-or left-handed α-helices depending on the ester group in the side chain, on solvent and/or on temperature. Polyphenethyl-l-aspartates (PPLA) exhibit a helix reversal from the right- to the left-handed form with increasing temperature. We have recently reported the application of polyphenethylaspartates as helically chiral alignment media. The thermoresponsivity observed for these polymers offers the possibility to measure different orientations of analytes before and after helix reversal of the alignment medium at 373 K. Herein we present a synthesized copolymer of phenethyl- and benzylaspartate as a new alignment medium undergoing this helix reversal at 303–313 K. Thus, the measurement of residual dipolar couplings (RDC) before and after the helix reversal is allowed for at ambient temperatures. A complete sign change of all 1H–13C RDCs was observed, which is close to the highest possible difference in NMR spectra.
A pH and temperature double sensibility of nanometer vesicle and its preparation method and application
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Paragraph 0044-0047, (2019/02/19)
The invention belongs to the fields of high polymer chemistry and biomedical engineering, and particularly discloses a pH and temperature sensitive polymer. The polymer is composed of a hydrophilic polyethylene glycol segment, and a lyophobic poly-(aspartic acid-diethyl-ethylenediamine-co-histamine-co-diisopropyl ethylenediamine) segment, and the ratio of the hydrophilic segment to the lyophobic segment is (1:10)-(1:12). The pH and temperature sensitive polymer can be used for preparing nano-vesicles loaded with hydrophilic anti-tumor drugs or/and ultrasonic contrast agents, and the nano-vesicles can be used for preparing tumor diagnosis drugs or tumor treatment drugs.
Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin
Sato, Shinichi,Tetsuhashi, Masashi,Sekine, Keiko,Miyachi, Hiroyuki,Naito, Mikihiko,Hashimoto, Yuichi,Aoyama, Hiroshi
, p. 4685 - 4698 (2008/12/20)
A series of hybrid compounds of bestatin (1) and actinonin (3), which promote degradation of cellular inhibitor of apoptosis protein 1 (cIAP1), were designed and synthesized. Structure-activity relationship studies indicated that absolute configuration, hydrophobicity at the α-position of the internal amide carbonyl group, and the presence of a small substituent at the α-position of the ester group are important factors for the expression of potent cIAP1 degradation-promoting activity. HAB-5A (30b) showed the most potent activity (IC50 = 0.53 μM) among the compounds prepared.
2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE DERIVATIVE AND MEDICINAL COMPOSITION
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, (2008/06/13)
The present invention has its object to provide a 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine derivative represented with the Formula (1) , or the pharmaceutically acceptable salt, which is effective as a therapeutic and prophylactic agent for diabetes, diabetic nephropathy, or glomerulosclerosis.
2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE DERIVATIVE AND MEDICINAL COMPOSITION
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Page/Page column 53, (2010/11/30)
A 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine derivative represented by the generalformula (1): [Chemical formula 1] (1) or a pharmaceutically acceptable saltthereof. They are useful as a therapeutic/preventive agent for diabetes, diabeticnephropathy, or glomerulosclerosis.
Dihydoxyhexanoic acid derivatives, their intermediates, and methods of making
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Page 16-17, (2010/02/05)
This invention relates to dihydroxyhexanoic acid derivatives and their intermediates, as well as to methods of preparing such compounds. Additionally, present invention relates to removing a protecting group from a protected amine wherein the method comprises reacting the protected amine with phosphoric acid.
Process for the preparation of omega-benzyl esters of amino diacids and of alkanesulphonates of these esters, and these alkanesulphonates
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Page 5, (2008/06/13)
The invention relates to a process for the preparation of an ?-benzyl ester of an amino diacid, characterized in that the amino diacid is reacted with a benzyl alcohol derivative of formula (I) 1 in which the R1 substituent or substituents, which are identical or different, represent a hydrogen atom, a C1 to C4 alkyl group, a C1 to C4 alkoxy group or a halogen atom and n is equal to 1, 2 or 3, in the presence of at least one mol per mole of the amino diacid of an alkanesulphonic acid, optionally in the presence of a solvent. The intermediate alkanesulphonates of the ?-benzyl esters of amino diacids and the ?-benzyl esters of amino diacids are obtained with a good yield and an excellent purity by virtue of this process.
Novel immunological adjuvant compounds and methods of preparation thereof
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, (2008/06/13)
This application relates to novel immunological adjuvant compounds of the formula: STR1 wherein each of R and R1 are the same or different and are hydrogen or an acyl radical; R2 is an unsubstituted or substituted alkyl radical, or an unsubstituted or substituted aryl radical; R6 is an alkyl radical X is an aminoacyl moiety; and Y is D-isoasparagine or D-isoglutamine.
Novel immunological adjuvant compounds and methods of preparation thereof
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, (2008/06/13)
This application relates to novel immunological adjuvant compounds of the formula: STR1 wherein each of R and R1 are the same or different and are hydrogen or an acyl radical; R2 is an unsubstituted or substituted alkyl radical, or an unsubstituted or substituted aryl radical; X is an aminoacyl moiety; and Y is D-isoasparagine or D-isoglutamine.
