- BIS-HETEROARYL DERIVATIVES AS MODULATORS OF PROTEIN AGGREGATION
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The present invention relates to certain bis-heteroaryl compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto- temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer including melanoma.
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Paragraph 0157
(2017/02/24)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column
(2015/02/19)
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- THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column
(2013/07/31)
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- Evaluating the use of chiral anthracene templates to access pyroglutamic acids
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An approach for the asymmetric synthesis of pyroglutamic acid derivatives is described based on an anthracene chiral auxiliary. The introduction of a furan ring as a masked carboxylic acid moiety proceeded with excellent levels of diastereo-selectivity, followed by conversion into a carboxylate ester. The ensuing retro-Diels-Alder procedure using flash vacuum pyrolysis (FVP) followed by reduction gave pyroglutamate esters in good yield but poor enantioselectivity, the latter of which was found to be dependant on the electronic nature of the N-protecting group.
- Hasbullah, Siti Aishah,Jones, Simon
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experimental part
p. 2719 - 2725
(2011/02/16)
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- Novel Receptor Antagonists and Their Methods of Use
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The present invention relates to novel oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
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Page/Page column 15
(2008/06/13)
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- New AZT conjugates as potent anti-HIV agents
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In an attempt to discover anti-HIV agents with much reduced cytotoxicity from the currently available HIV-reverse transcriptase inhibitors, AZT conjugates of cholanic acids, 2-imidazolidone-4-carboxylic acid and its derivatives, and N,N′-disubstituted 5-hydroxy-tetrahydropyrimidin-2-ones have been synthesized and their anti-HIV profiles determined with CEM-SS cell line. The AZT conjugates with 2-imidazolidone-4-carboxylic acid and 2-pyrrolidone-5-carboxylic acid through an ester linkage, and with N,N′-diphenyl-5-hydroxy-tetrahydropyrimidin-2-one through a succinate tether showed significantly higher therapeutic indexes than AZT while they also retained or enhanced AZT's anti-HIV activity. Thus, structural features that favor the desired therapeutic profile of the conjugates appear to include a five-membered ring cyclic urea or lactam, and six-membered ring cyclic urea with N,N′-diphenyl substitution. Copyright Taylor & Francis Group, LLC.
- You, Zhengqing,Lee, Henry
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- Studies on pyrrolidinones. Synthesis of N-(2-nitrobenzyl)pyroglutamic acid
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While methyl N-(4-nitrobenzyl)pyroglutamate can be obtained from methyl-N-trimethylsilylpyroglutamate, the best way to obtain methyl N-(2-nitrobenzyl)pyroglutamate is to react 4-nitro benzyl bromide with the iminoether derived from methyl pyroglutamate.
- Rigo, Benoit,Dolaine, Regis,El Ghammarti, Samira,Couturier, Daniel
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p. 1063 - 1066
(2007/10/03)
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- A short, efficient chiral synthesis of a novel cholinergic channel activator, ABT-418 [(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole], from (S)-pyroglutamic acid
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ABT-418 [(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole] (1) is a cholinergic channel activator with potent cognitive and anxiolytic activities in animal models. A three-pot synthesis of enantiomerically pure ABT-418 starting from commercially available (S)-pyroglutamic acid is described. The overall yield of the synthesis is 43%.
- Lin, Nan-Horng
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p. 2563 - 2566
(2007/10/02)
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- Studies on Pyrrolidones. Synthesis and N-Alkylation of &β-Enaminoesters Derived from Pyroglutamic Acid
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The condensation of iminoether 7, derived from pyroglutamic acid (4), with active methylene reagents such as Meldrum's acid or methyl cyanoacetate, lead to β-enaminoesters 2.Solid-liquid phase transfer N-alkylation of these compounds is described.
- Fasseur, Dominique,Rigo, Benoit,Leduc, Catherine,Cauliez, Pascal,Couturier, Daniel
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p. 1285 - 1291
(2007/10/02)
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- DI- OR TRIPEPTIDE RENIN INHIBITORS CONTAINING LACTAM CONFORMATIONAL RESTRICTION IN ACHPA
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Enzyme di-or tripeptides of the formula: STR1 and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems which employ these novel peptides.
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