204580-28-9Relevant academic research and scientific papers
PRODRUG OF NITROXOLINE AND USE THEREOF
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Page/Page column 106-107, (2021/08/24)
The present invention relates to the prodrug of nitroxoline and use thereof. Specifically, the present invention relates to a compound of formula (I) or the pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition comprising the same, as well as a use thereof in anti-infective and anti-tumor drugs. The compound of formula (I) has better pharmacokinetic parameters such as water solubility, blood concentration or half-life relative to nitroxoline. The compound of formula (I) can reduce the number of administrations, and has the possibility of being applied in other fields than the urinary tract field. The definition of each group in formula (I) is as defined in the description.
NITROXOLINE PRODRUG AND USE THEREOF
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Paragraph 0214; 0496-0497, (2021/11/26)
Provided are a nitroxoline prodrug and a use thereof. Specifically, provided are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a composition containing the compound, and a use thereof in the preparation of anti-infective and antitumor drugs, and definitions of groups in formula (I) are as stated in the specification. The compound represented by formula (I) has better pharmacokinetic parameters such as solubility, blood medicine concentration, or half-life period than nitroxoline. The compound represented by formula (I) can reduce the frequency of drug administration, and has potential for application in other fields other than the field of urinary tracts.
INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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Page/Page column 111; 112, (2019/07/20)
The present invention provides a compound of formula (II): an inhibitor of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases. Its prodrugs are disclosed.
Total Synthesis and Stereochemical Revision of the Anti-Tuberculosis Peptaibol Trichoderin A
Kavianinia, Iman,Kunalingam, Lavanya,Harris, Paul W. R.,Cook, Gregory M.,Brimble, Margaret A.
supporting information, p. 3878 - 3881 (2016/08/16)
The first total synthesis of the postulated structure of the aminolipopeptide trichoderin A and its epimer are reported. A late-stage solution phase C-terminal coupling was employed to introduce the C-terminal aminoalcohol moiety. This methodology provides a foundation to prepare analogues of trichoderin A to establish a structure-activity relationship. NMR spectroscopic analysis established that the C-6 position of the 2-amino-6-hydroxy-4-methyl-8-oxodecanoic acid (AHMOD) residue in trichoderin A possesses an (R)-configuration as opposed to the originally proposed (S)-configuration.
PYRIMIDINE FGFR4 INHIBITORS
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Page/Page column 119-120, (2015/05/05)
Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.
PYRIMIDONE DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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Paragraph 0160-0161, (2014/07/22)
The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
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Page/Page column 62, (2013/06/27)
Compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for t
CHEMICAL COMPOUNDS
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Page/Page column 54, (2012/02/15)
The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
Efficient synthesis of heterocyclic compounds using ethenetricarboxylic acid diesters
Yamazaki, Shoko,Iwata, Yuko,Fukushima, Yugo
supporting information; experimental part, p. 655 - 659 (2009/06/20)
Ethenetricarboxylic acid diester 1a is a useful compound bearing two reactive sites, a CO2H group and a Michael acceptor. Reactions of 1a and reagents with oxygen and nitrogen nucleophilic moieties have been examined. The reaction of 1a with 2-
Synthesis and evaluation of carbamate prodrugs of a phenolic compound
Igarashi, Yasushi,Yanagisawa, Erika,Ohshima, Toshihiro,Takeda, Shuichi,Aburada, Masaki,Miyamoto, Ken-Ichi
, p. 328 - 333 (2007/10/03)
A series of carbamates of the phenolic compound 1 were prepared and evaluated in vivo as its prodrug. Each carbamate was orally administered to rats, and plasma concentrations of the parent compound 1 were measured with the passage of time. We judged which carbamate was suitable for the prodrug of 1 from both the AUC value of 1 and absence of the carbamate in plasma. The AUC value of 1 after oral administration of 2b was approximately 40-fold higher than that for an administration of 1, and the bioconversion from 2b to 1 was excellent. As a whole, di-substituted carbamates resulted in higher plasma concentrations of 1 than did mono-substituted ones. However di-substituted carbamates were almost always detected in plasma. As a result, we found that the ethycarbamoyl derivative 2b demonstrates the best prodrug property in this series.
