- BILE ACID-GCPII INHIBITOR CONJUGATES TO TREAT INFLAMMATORY DISEASES
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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.
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Page/Page column 39; 63
(2021/08/06)
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- Diagnostic device for the detection of disease related target structures
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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
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- DIAGNOSTIC DEVICE FOR THE DETECTION OF DISEASE RELATED TARGET STRUCTURES
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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
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- DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME
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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).
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- DENDRIMER BASED COMPOSITIONS AND METHODS OF USING THE SAME
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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
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Page/Page column 102
(2008/06/13)
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- Prodrugs of NAALAdase inhibitors
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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.
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- Synthesis and biological evaluation of (R)- and (S)-2-(phosphonomethyl)pentanedioic acids as inhibitors of glutamate carboxypeptidase II
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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
- Vitharana, Dilrukshi,France, Jessica E.,Scarpetti, David,Bonneville, George W.,Majer, Pavel,Tsukamoto, Takashi
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p. 1609 - 1614
(2007/10/03)
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- Design and pharmacological activity of phosphinic acid based NAALADase inhibitors
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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.
- Jackson,Tays,Maclin,Ko,Li,Vitharana,Tsukamoto,Stoermer,Lu,Wozniak,Slusher
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p. 4170 - 4175
(2007/10/03)
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- Phosphinic acid pseudopeptides analogous to glutamyl-γ-glutamate: Synthesis and coupling to pteroyl azides leads to potent inhibitors of folylpoly-γ-glutamate synthetase
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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.
- Valiaeva,Bartley,Konno,Coward
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p. 5146 - 5154
(2007/10/03)
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- Pharmaceutical compositions and methods of treating a glutamate abnormality and effecting a neuronal activity in an animal using NAALADase inhibitors
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The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor
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- Certain dioic acid derivatives useful as NAALADase inhibitors
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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
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- Inhibitors of NAALADase enzyme activity
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The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated alpha -Linked Acidic Dipeptidase (NA
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- PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATING COMPULSIVE DISORDERS USING NAALADASE INHIBITORS
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The present invention relates to a pharmaceutical composition and a method for treating a compulsive disorder using a NAALADase inhibitor.
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