18938-60-8Relevant articles and documents
Synthesis and preliminary biological evaluation of O-2((2-[ 18F]fluoroethyl)methylamino)ethyltyrosine ([18F]FEMAET) as a potential cationic amino acid PET tracer for tumor imaging
Chiotellis, Aristeidis,Mueller, Adrienne,Weyermann, Karin,Leutwiler, Dominique S.,Schibli, Roger,Ametamey, Simon M.,Kraemer, Stefanie D.,Mu, Linjing
, p. 1947 - 1959 (2014)
Amino acid transport is an attractive target for oncologic imaging. Despite a high demand of cancer cells for cationic amino acids, their potential as PET probes remains unexplored. Arginine, in particular, is involved in a number of biosynthetic pathways
Facile synthesis of sulfotyrosine-containing α-conotoxins
He, Chunmao,Li, Changpeng
supporting information, p. 7559 - 7564 (2020/10/14)
α-Conotoxins (Ctx) can selectively target distinct subtypes of nicotinic acetylcholine receptors (nAChRs), which are closely related to a number of neurological diseases, and they have been considered as ideal probes and model peptide drugs. Sulfotyrosine
Development of a Photoactivatable Protein Phosphatase-1-Disrupting Peptide
Henschke, Lars,K?hn, Maja,Makotta, Leslie,Trebacz, Malgorzata,Wang, Yansong
, (2020/02/04)
We describe here the development of a photoreleasable version of a protein phosphatase-1 (PP1)-disrupting peptide (PDP-Nal) that triggers protein phosphatase-1 activity. PDP-Nal is a 23 mer that binds to PP1 through several interactions. It was photocaged
DIMETHYLAMINOETHANOL SALT OF A GLP-1 RECEPTOR MODULATOR
-
Paragraph 125; 126; 127, (2018/04/17)
Crystalline 2-hydroxy-N,N-dimethylethanaminium 1 -(2-(5-(tert-butyl) -thiophene-2-carboxamido)-3-(4-(5-(4'-ethyl-[1,1'-bi(cyclohexan)]-3- en-4-yl)pyrimidin-2-yl)phenyl)propanoyl)azetidine-3-carboxylate salt, and methods related to synthesis and therapeuti
Base/Cryptand/Metal-Free Automated Nucleophilic Radiofluorination of [18F]FDOPA from Iodonium Salts: Importance of Hydrogen Carbonate Counterion
Maisonial-Besset, Aurélie,Serre, Audrey,Ouadi, Ali,Schmitt, Sébastien,Canitrot, Damien,Léal, Fernand,Miot-Noirault, Elisabeth,Brasse, David,Marchand, Patrice,Chezal, Jean-Michel
, p. 7058 - 7065 (2019/01/04)
As evidenced by the number of publications and patents published in the last years, the radiosynthesis of 6-[18F]fluoro-3,4-dihydroxy-L-phenylalanine ([18F]FDOPA) using the nucleophilic [18F]F- process remains currently a challenge for the radiochemists scientific community even if promising methods for the radiofluorination of electron-rich aromatic structures were recently developed from arylboronate, arylstannane or iodonium salt precursors. In such context, based on the use of an iodonium triflate salt precursor, we optimized a fast and efficient radiofluorination route fully automated and free from any base, cryptand or metal catalyst for the radiosynthesis of [18F]FDOPA. Using this method, this clinically relevant radiotracer was produced in 64 min, 27–38 % RCY d.c. (n = 5), >99 % RCP, >99 % ee., and high Am 170–230 GBq/μmol. In addition, this optimization study clearly highlighted the important role of a triflate-hydrogen carbonate counterion exchange during the radiolabeling process to achieve high fluorine-18 incorporation yields.
Development of a Kilogram-Scale Synthesis of a Novel Anti-HCV Agent, CH4930808
Haneishi, Tsuyoshi,Kato, Yoshiaki,Fukuda, Hiroshi,Shimamura, Tomoyuki,Tanokura, Takemi,Hiraide, Akira,Koyama, Kaichiro,Fudesaka, Masato,Maeda, Kenji,Nakata, Nobuyuki,Nagase, Masahiro,Yabuzaki, Takahiko,Takao, Hiroaki,Kigawa, Masaharu,Shimizu, Hitoshi,Shimizu, Makoto
, p. 236 - 240 (2018/02/23)
Herein, we report the kilogram-scale synthesis of CH4930808 (1), a novel anti-hepatitis C virus agent. While pursuing improved productivity using many through-process strategies, we conducted scrupulous impurity control. Finally, we successfully developed
NURR1:RXR ACTIVATING COMPOUNDS FOR SIMULTANEOUS TREATMENT OF SYMPTOMS AND PATHOLOGY OF PARKINSON'S DISEASE
-
Page/Page column 44, (2017/08/01)
The invention provides a series of substituted aryl pyrimidine compounds and the use of these compounds as therapeutics to treat or prevent neurodegenerative disorders, including Parkinson's disease. Compounds of the invention are also able to treat the s
THIAZOLIDINONE COMPOUNDS AND USE THEREOF
-
Paragraph 0708-0709, (2017/09/21)
A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
COMPOSITIONS CONTAINING, METHODS INVOLVING, AND USES OF NON-NATURAL AMINO ACIDS AND POLYPEPTIDES
-
Page/Page column 197, (2016/07/27)
Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oximine, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.
NOVEL GLP-1 RECEPTOR MODULATORS
-
Paragraph 0384, (2016/02/09)
Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where "?" represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.