- 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 41; 42
(2021/04/30)
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- GLUCOPYRANOSYL DERIVATIVE AND USE THEREOF
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The present invention relates to a glucopyranosyl derivative and a use thereof. In particular, the present invention relates to a glucopyranosyl derivative that is used as an inhibitor of sodium-dependent glucose transporters (SGLTs), particularly being used as an inhibitor of sodium-dependent glucose transporter-1 (SGLT1), and a pharmaceutically acceptable salt or stereoisomer thereof, further relating to a pharmaceutical composition containing the derivative. The present invention further relates to a use of the compound and a pharmaceutical composition thereof in the preparation of a drug for treating diabetes and diabetes-related diseases.
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Paragraph 0360-0362
(2020/12/16)
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- The synthesis of α,α-disubstituted α-amino acids via ichikawa rearrangement
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An approach to α,α-disubstituted α-amino acids is reported. The key step is allyl cyanate-to-isocyanate rearrangement. As demonstrated, the resultant allyl isocyanates can be directly trapped with various nucleophiles, for instance, alcohols, amines, and organometallic reagents, to provide a broad range of N-functionalized allylamines. The developed method has been successfully applied in the synthesis of two bioactive peptides: 2-aminoadamantane-2-carboxylic acid derived P2X7-evoked glutamate release inhibitor and 4-amino-tetrahydropyranyl-4-carboxylic acid derived dipeptide GSK-2793660, which is currently in clinical trials as cathepsin C inhibitor for the treatment of cystic fibrosis, noncystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis.
- Szczes?niak, Piotr,Pieczykolan, Micha?,Stecko, Sebastian
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p. 1057 - 1074
(2016/02/19)
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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 39-40
(2015/02/19)
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- Foldamer-mediated remote stereocontrol: >1,60 asymmetric induction
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An N-terminal L-α-methylvaline dimer induces complete conformational control over the screw sense of an otherwise achiral helical peptide foldamer formed from the achiral quaternary amino acids Aib and Ac6c. The persistent right-handed screw-sense preference of the helix enables remote reactive sites to fall under the influence of the terminal chiral residues, and permits diastereoselective reactions such as alkene hydrogenation or iminium ion addition to take place with 1,16-, 1,31-, 1,46- and even 1,61-asymmetric induction. Stereochemical information may be communicated in this way over distances of up to 4 nm. Reaction at a distance: By inducing a quantitative, persistent preference for right-handed helicity, chirality at one end of an otherwise achiral helical molecule is able to control the stereoselectivity of reactions at sites located up to 60 bonds away, shattering previous records for remote stereochemical control. Copyright
- Byrne, Liam,Sola, Jordi,Boddaert, Thomas,Marcelli, Tommaso,Adams, Ralph W.,Morris, Gareth A.,Clayden, Jonathan
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supporting information
p. 151 - 155
(2014/01/17)
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- Microbial enantioselective removal of the N-benzyloxycarbonyl amino protecting group
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In order to deprotect N-carbobenzoxy-l-aminoacids (Cbz-AA) and related compounds, a series of microorganisms was selected from soil by enrichment cultures with Cbz-l-Glu as sole nitrogen source. A lyophilized whole-cell preparation of two Arthrobacter sp. strains grown on Cbz-Glu or Cbz-Gly exhibited a high cleavage activity. The conditions of hydrolysis have been optimized and a quantitative enantioselective deprotection of several Cbz-dl-amino acids was obtained, as well as the deprotection of N-carbamoylester derivatives of several synthetic amino compounds. The preparation of Cbz-d-allylglycine and l-allylglycine in high yield and high optical purity is described as an application of this method.
- Maurs, Michele,Acher, Francine,Azerad, Robert
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- Facing the gem-dialkyl effect in enzyme inhibitor design: Preparation of homocycloleucine-based azadipeptide nitriles
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A tough nut to crack: In contrast to azadipeptide nitriles containing a P2 leucine residue, the synthesis of the corresponding homocycloleucine-based inhibitors was more difficult; possibly due to the gem-dialkyl effect. A synthetic route to the first hom
- Frizler, Maxim,Lohr, Friederike,Luelsdorff, Michael,Guetschow, Michael
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supporting information; experimental part
p. 11419 - 11423
(2011/11/29)
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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 23
(2008/12/05)
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- Versatile synthesis of free and N-benzyloxycarbonyl-protected 2,2-disubstituted taurines
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An effective and versatile method was developed to synthesize N-benzyloxycarbonyl-protected and free 2,2-disubstituted taurines. Several novel 2,2-disubstituted taurines, including aliphatic/aromatic and cyclic/acyclic derivatives, were obtained, which demonstrates the generality of this method. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Wang, Boyuan,Zhang, Wei,Zhang, Leilei,Du, Da-Ming,Liu, Gang,Xu, Jiaxi
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p. 350 - 355
(2008/09/18)
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- AMIDE STABILIZED HYDROXYETHYLAMINES
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This invention pertains to amide and ester derivatives of hydroxyethylamine compounds that serve as effective beta-secretase inhibitors. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprisi
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Page/Page column 28
(2010/11/28)
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- Synthesis and pharmacological evaluation of glycine-modified analogues of the neuroprotective agent glycyl-L-prolyl-L-glutamic acid (GPE)
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The synthesis of 10 G*PE analogues, wherein the glycine residue has been modified, is described by coupling readily accessible dibenzyl-l-prolyl-l- glutamate 2 with various analogues of glycine. Pharmacological evaluation of the novel compounds was undertaken to further understand the role of the glycine residue on the observed neuroprotective properties of the endogenous tripeptide GPE.
- Lai, Michelle Y.H.,Brimble, Margaret A.,Callis, David J.,Harris, Paul W.R.,Levi, Mark S.,Sieg, Frank
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p. 533 - 548
(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 35-36
(2010/02/11)
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- Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents
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This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.
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Page column 29
(2010/02/05)
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- Zinc promoted rapid and efficient synthesis of Fmoc- and Z-α,α-dialkylamino acids under neutral conditions
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The introduction of Nα-9-fluorenylmethyloxycarbonyl (Fmoc) and benzyloxycarbonyl (Z) groups into α,α-dialkylamino acids is described at neutral pH using Fmoc-Cl or Z-Cl as an acylating agent respectively in the presence of activated zing powder. The reaction is simple, fast and clean. It also permits the scale up with high yields. It is completely free from protected oligomer formation, which is a known side-reaction when Schotten-Baumann procedure is followed. All the Fmoc- and Z-amino acids prepared have been fully characterized.
- Babu, Vommina V. Suresh,Ananda, Kuppanna
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- Cyclic amide derivatives
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A cyclic amide derivative of formula (I): wherein R1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl group, a substituted sul
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- Achiral amino acid acyl esters of ganciclovir and its derivatives
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Compounds of the Formula I STR1 wherein X is hydrogen, chloro, amino or hydroxy; R1 is an achiral amino acid acyl residue with a tertiary α-carbon atom. Preferred achiral amino acid acyl residues have the formula STR2 wherein each R2
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- Synthesis and CCK-B Binding Affinities of Cyclic Analogues of the Potent and Selective CCK-B Receptor Antagonist CI-988
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A selected series of 14-membered macrocyclic compounds (2) has been prepared as potential CCK-B receptor selective ligands.The efficiency of a number of cyclising reagents has also been evaluated.
- Didier, Eric,Horwell, David C.,Pritchard, Martyn C.
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p. 8471 - 8490
(2007/10/02)
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