267875-78-5Relevant academic research and scientific papers
TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER
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Page/Page column 64; 65, (2021/01/29)
A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.
Structure-Activity Relationships in Metal-Binding Pharmacophores for Influenza Endonuclease
Credille, Cy V.,Dick, Benjamin L.,Morrison, Christine N.,Stokes, Ryjul W.,Adamek, Rebecca N.,Wu, Nicholas C.,Wilson, Ian A.,Cohen, Seth M.
, p. 10206 - 10217 (2018/11/23)
Metalloenzymes represent an important target space for drug discovery. A limitation to the early development of metalloenzyme inhibitors has been the lack of established structure-activity relationships (SARs) for molecules that bind the metal ion cofactor(s) of a metalloenzyme. Herein, we employed a bioinorganic perspective to develop an SAR for inhibition of the metalloenzyme influenza RNA polymerase PAN endonuclease. The identified trends highlight the importance of the electronics of the metal-binding pharmacophore (MBP), in addition to MBP sterics, for achieving improved inhibition and selectivity. By optimization of the MBPs for PAN endonuclease, a class of highly active and selective fragments was developed that displays IC50 values 50 values of ～10 nM, illustrating the utility of a metal-centric development campaign in generating highly active and selective metalloenzyme inhibitors.
A double-3, 2 - hydroxy pyridine ketone derivative and its preparation and use (by machine translation)
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, (2017/07/22)
The invention discloses a double-3, 2 - hydroxy pyridine ketone derivative and its preparation and use, is characterized in that the double 3, 2 - hydroxy pyridine ketone derivatives in order to monochloride, succinic acid alkone sodium salt derivative an
Synthesis and Chemical Reactivity of a 6-Me-3,2-Hydroxypyridinone Dithiazolide with Primary Amines: A route to New Hexadentate Chelators for Hard Metal(III) Ions
Pailloux, Sylvie L.,Nguyen, Sean,Zhou, Stephanie,Hom, Marisa E.,Keyser, Michelle N.,Smiles, Danil,Raymond, Kenneth N.
, p. 1065 - 1073 (2016/07/29)
A hydroxypyridinone building block, bifunctionalized with thiazoline, has been prepared from orthogonally protected 2-(3-(benzyloxy)-4-(ethoxycarbonyl)-6-methyl-2-oxopyridin-1(2H)-yl) acetic acid. The reactivity of the dithiazolide has been explored with
DI-MACROCYCLES
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Paragraph 00232, (2014/06/11)
The invention relates to chemical compounds and complexes that can be used in therapeutic and diagnostic applications.
MACROCYCLIC HOPO CHELATORS
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, (2011/04/14)
The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds comprise hydroxypyridinonyl moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability.
HIV INTEGRASE INHIBITORS
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, (2010/01/12)
Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein G, T, R1, R2, R3A, R3B, R4A, R4B, R5A, R5B, R6A and R6B are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
2-HYDROXY-1-OXO 1,2 DIHYDRO ISOQUINOLINE CHELATING AGENTS
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Page/Page column 36; 88; 89, (2010/11/28)
The invention provides a new class of strongly chelating multidentate ligands based on a 2-hydroxy-1-oxo-1,2-dihydro-isoquinoline-3-carboxylic acid scaffold (hereafter 1,2-HOIQO) in combination with polyamine backbones. The extremely stable bidentate 1,2- HOIQO moiety can be synthesized by standard synthetic methodology on a large scale. An advantageous feature is the possibility to introduce a wide range of substituents on the benzene ring by standard transformations (like electrophilic aromatic substitutions). This allows, for example, for the tuning of chemical, photophysical, and solubility properties, as well as the attachment of functional moieties, relevant for sensing and imaging applications (e.g. DNA, proteins, antibodies, fluorophores, etc.). The combination of the 1,2-HOIQO chelators with polyamine backbones provides very strongly binding ligands for a variety of metals including first-row transition metals, lanthanides, actinides, etc. Metal complexes of this kind are expected to be useful in a number of applications (e.g. luminescence, MRI, actinide sequestering, metal chelation therapy, metal radioisotope labeling, etc.).
Hydroxypyridonate and hydroxypyrimidinone chelating agents
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Page/Page column 11; 37, (2010/02/10)
The present invention provides hydroxypyridinone and hydroxypyrimidone chelating agents. Also provides are Gd(III) complexes of these agents, which are useful as contrast enhancing agents for magnetic resonance imaging. The invention also provides methods of preparing the compounds of the invention, as well as methods of using the compounds in magnetic resonance imaging applications.
Thrombin inhibitors
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2or N; d is CY3or N; e is CY4or N; f is CY5or N; g is CY6or N; Y4, Y5, and Y6are independently hydrogen, C1-4alkyl, or halogen; Y1and Y2are independently hydrogen, C1-4alkyl, C3-7cycloalkyl, halogen, NH2, OH or C1-4alkoxy, and Y3is hydrogen, C1-4alkyl, C3-7cycloalkyl, halogen, —CN, NH2, OH or C1-4alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.
