200698-34-6Relevant academic research and scientific papers
BILE ACID-GCPII INHIBITOR CONJUGATES TO TREAT INFLAMMATORY DISEASES
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Page/Page column 39; 63, (2021/08/06)
GCPII inhibitors comprising 2-(phosphonomethyl) pentanedioic acid (2-PMPA) conjugated to a bile acid and their use for treating a disease or condition associated with elevated levels of GCPII, including inflammatory bowel disease.
Diagnostic device for the detection of disease related target structures
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Paragraph 0076; 0079; 0080, (2015/03/16)
The present invention provides a diagnostic device allowing highly specific and efficient in vivo and/or in vitro detection of a bio marker in a broad range of bodily fluids or tissues. The diagnostic device is composed of a binding agent that specificall
DIAGNOSTIC DEVICE FOR THE DETECTION OF DISEASE RELATED TARGET STRUCTURES
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Page/Page column 17; 18, (2015/03/16)
The present invention provides a diagnostic device allowing highly specific and efficient in vivo and/or in vitro detection of a bio marker in a broad range of bodily fluids or tissues. The diagnostic device is composed of a binding agent that specificall
DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME
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, (2009/04/24)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).
DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME
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Page/Page column 102, (2008/06/13)
The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The c
Synthesis and biological evaluation of (R)- and (S)-2-(phosphonomethyl)pentanedioic acids as inhibitors of glutamate carboxypeptidase II
Vitharana, Dilrukshi,France, Jessica E.,Scarpetti, David,Bonneville, George W.,Majer, Pavel,Tsukamoto, Takashi
, p. 1609 - 1614 (2007/10/03)
Both enantiomers of 2-(phosphonomethyl)pentanedioic acid (2-PMPA), a potent and selective inhibitor of glutamate carboxypeptidase II (GCP II), were successfully prepared through the resolution of racemic 2-(hydroxyphosphinoylmethyl)pentanedioic acid diben
Prodrugs of NAALAdase inhibitors
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, (2008/06/13)
The present invention relates to prodrugs of NAALADase inhibitors, pharmaceutical compositions comprising the same, and methods of using the same to treat glutamate abnormalities and prostate diseases.
Phosphinic acid pseudopeptides analogous to glutamyl-γ-glutamate: Synthesis and coupling to pteroyl azides leads to potent inhibitors of folylpoly-γ-glutamate synthetase
Valiaeva,Bartley,Konno,Coward
, p. 5146 - 5154 (2007/10/03)
Several routes to a complex phosphinate phosphapeptide analogous to the γ-glutamyl peptide Gluγ-Glu have been investigated. Formation of γ-phosphono glutamate derivatives via addition of a phosphorus-based radical to protected vinylglycine was found to be of limited value because of the elevated temperatures required. Alkylation and conjugate addition reactions of trivalent phosphorus (PIII) species were investigated. In situ generation of bis-trimethylsilyl esters of phosphinous acids proved to be an effective route to phosphinates of modest structural complexity. However, this chemistry could not be extended to the incorporation of an amino acid moiety at the N-terminal side of the desired phosphinate. A successful synthesis of the target phosphinate phosphapeptide was effected using PIII chemistry and dehydrohalogenation to yield an α,β-unsaturated phosphinic acid ester, following which conjugate addition of diethylacetamido malonate and acid-mediated hydrolysis afforded the desired phosphinate phosphapeptide. Coupling of the unprotected phosphinate phosphapeptide with two acyl azides derived from folic acid and methotrexate led to the corresponding pteroylphosphapeptides of interest as possible mimics of tetrahedral intermediates in the reaction catalyzed by folylpolyglutamate synthetase.
Design and pharmacological activity of phosphinic acid based NAALADase inhibitors
Jackson,Tays,Maclin,Ko,Li,Vitharana,Tsukamoto,Stoermer,Lu,Wozniak,Slusher
, p. 4170 - 4175 (2007/10/03)
A novel series of phosphinic acid based inhibitors of the neuropeptidase NAALADase are described in this work. This series of compounds is the most potent series of inhibitors of the enzyme described to date. In addition, we have shown that these compounds are protective in animal models of neurodegeneration. Compound 34 significantly prevented neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In addition, in the chronic constrictive model of neuropathic pain, compound 34 significantly attenuated the hypersensitivity observed with saline-treated animals. These data suggest that NAALADase inhibition may provide a new approach for the treatment of both neurodegenerative disorders and peripheral neuropathies.
Certain dioic acid derivatives useful as NAALADase inhibitors
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, (2008/06/13)
The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated alpha -Linked Acidic Dipeptidase (NAALADase) enzyme
