- BICYCLIC COMPOUNDS AND METHODS FOR THEIR USE IN TREATING PITT HOPKINS SYNDROME
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Embodiments of this invention provide compounds, compositions, methods, and uses for therapeutic diketopiperazines, including cyclic G-2-Allyl Proline and other cyclic Glycyl Proline compounds to treat Pitt Hopkins Syndrome and symptoms thereof, as well a
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Page/Page column 38-40
(2021/04/30)
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- Development of glycine-α-methyl-proline-containing tripeptides with neuroprotective properties
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Herein is described the synthesis of novel glycine-α-methyl-proline-containing tripeptides (GPMeX tripeptides namely GPMeR, GPMeK, and GPMeH) with the aim of obtaining derivatives highly stable in human plasma and able to counteract neuroinflammatory processes that are distinctive of neurodegenerative pathologies. The syntheses of GPMeR, GPMeK, and GPMeH were all achieved both by introducing the ProMe residue into the Gly-Pro-Arg (GPR) sequence in place of the native Pro in P2 position and replacing the basic amino acid Arg in P3 position by Lys or His. Results showed that all novel GPMeX tripeptides are stable in human plasma (t1/2 > 51 h) and that GPMeH - generating stable intramolecular H-bond in a C11-turn by interaction of His imidazole ring and Gly carbonyl group - restored physiological levels of nitric oxide deriving from neuronal NOS (nNOS) activity, thus preventing the inflammatory response by suppression of the NF-kB activity and, consequently, the expression of inflammatory genes such as inducibile NOS (iNOS). Therefore, GPMeH could be a lead compound for further development of peptidomimetics able to contrast neuroinflammatory processes.
- Cacciatore, Ivana,Fornasari, Erika,Di Stefano, Antonio,Marinelli, Lisa,Cerasa, Laura Serafina,Turkez, Hasan,Aydin, Elanur,Moretto, Alessandro,Ferrone, Alessio,Pesce, Mirko,Di Giacomo, Viviana,Reale, Marcella,Costantini, Erica,Di Giovanni, Pamela,Speranza, Lorenza,Felaco, Mario,Patruno, Antonia
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p. 553 - 563
(2015/12/30)
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- NEUROPROTECTIVE BICYCLIC COMPOUNDS AND METHODS FOR THEIR USE IN TREATING AUTISM SPECTRUM DISORDERS AND NEURODEVELOPMENTAL DISORDERS
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Embodiments of this invention provide compositions and methods for therapeutic use of diketopiperazines including cyclic G-2-Allyl Proline and other cyclic Glycyl Proline compounds to treat symptoms of Autism Spectrum Disorders and Neurodevelopmental Diso
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Page/Page column 38
(2015/02/19)
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- 1 -(CYCLOPENT-2-EN-1 -YL)-3-(2-HYDROXY-3-(ARYLSULFONYL)PHENYL)UREA DERIVATIVES AS CXCR2 INHIBITORS
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The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
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Page/Page column 123
(2015/12/18)
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- TREATMENT OF AUTISM SPECTRUM DISORDERS USING GLYCYL-L-2-METHYLPROLYL-L-GLUTAMIC ACID
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This invention provides compounds, compositions and methods for treating Autism Spectrum Disorders (ASD) using glycyl-2-methyIprolyl-glutamic acid (G-2-MePE) and analogs thereof. Autism Spectrum Disorders include Autism, Autistic Disorder, Asperger Syndro
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Page/Page column 32; 33
(2014/06/23)
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- TREATMENT OF AUTISM SPECTRUM DISORDERES USING GLYCYL-L-2-METHYLPROLYL-L-GLUTAMIC ACID
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This invention provides compounds, compositions and methods for treating Autism Spectrum Disorders (ASD) using glycyl-2-methylprolyl-glutamic acid (G-2-MePE) and analogs thereof. Autism Spectrum Disorders include Autism, Autistic Disorder, Asperger Syndro
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Page/Page column 29; 30
(2012/08/08)
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- CYCLIC GLYCYL-2-ALLYL PROLINE IMPROVES COGNITIVE PERFORMANCE IN IMPAIRED ANIMALS
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Embodiments of this invention provide methods for therapeutic use of cyclic G-2-Allyl Proline to treat cognitive disorders as well as manufacture of medicaments including tablets, capsules, injectable solutions that are useful for treatment of such condit
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Page/Page column 21
(2008/12/05)
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- ANALOGS OF GLYCYL-PROLYL-GLUTAMATE
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Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson''s disease.
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Page/Page column 33
(2008/06/13)
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- Synthesis of proline-modified analogues of the neuroprotective agent glycyl-L-prolyl-glutamic acid (GPE)
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The synthesis of ten proline-modified analogues of the neuroprotective tripeptide GPE is described. Five of the analogues incorporate a proline residue with a hydrophobic group at C-2 and two further analogues have this side chain locked into a spirolactam ring system. The pyrrolidine ring was also modified by replacing the γ-CH2 group with sulfur and/or incorporation of two methyl groups at C-5.
- Harris, Paul W.R.,Brimble, Margaret A.,Muir, Victoria J.,Lai, Michelle Y.H.,Trotter, Nicholas S.,Callis, David J.
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p. 10018 - 10035
(2007/10/03)
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- NEUROPROTECTIVE BICYCLIC COMPOUNDS AND METHODS FOR THEIR USE
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Embodiments of this invention provide novel cyclic compounds structurally related to diketopiperazines and methods for their therapeutic use. Such compounds are neuroprotective and have utility as therapeutic agents for treatment of diseases, injuries and
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Page/Page column 33
(2010/02/11)
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