- Total Synthesis and Structure-Activity Relationships Study of Odilorhabdins, a New Class of Peptides Showing Potent Antibacterial Activity
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The spread of antibiotic-resistant pathogens is a growing concern, and new families of antibacterials are desperately needed. Odilorhabdins are a new class of antibacterial compounds that bind to the bacterial ribosome and kill bacteria through inhibition
- Sarciaux, Matthieu,Pantel, Lucile,Midrier, Camille,Serri, Marine,Gerber, Cristelle,Marcia De Figueiredo, Renata,Campagne, Jean-Marc,Villain-Guillot, Philippe,Gualtieri, Maxime,Racine, Emilie
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- NOVEL PEPTIDE DERIVATIVES AND USES THEREOF
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The invention provides for novel peptide derivatives and compositions comprising the same. The invention further provides methods of treatment comprising administering novel peptide derivatives and/or compositions comprising the same.
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Paragraph 00176
(2016/04/20)
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- NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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The invention relates to novel heteroaryl and heterocycle compounds of formula I and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune diseases and cancer.
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Paragraph 231
(2016/08/23)
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- BARETTIN AND DERIVATIVES THEREOF FOR MEDICAL USE, IN PARTICULAR FOR THE TREATMENT OF DISEASES RELATED TO OXIDATIVE STRESS OR INFLAMMATION, AND FOR PRESERVING OR WASHING ORGANS
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The present invention relates to compounds of formula(I) herein, which includes barettin and derivatives thereof, or any pharmaceutically acceptable salt thereof for use as a medicament. Further the present invention relates to same compounds for use in t
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Page/Page column 22; 23
(2014/10/18)
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- NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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Provided are novel heteroaryl and heterocycle compounds of formula (I-1), (I-2) or (I-3) and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune disorders diseases and cancer.
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Page/Page column 138
(2014/02/16)
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- NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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The invention relates to novel heteroaryl and heterocycle compounds and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3k and for treating inflammatory and autoimmune disorders diseases and cancer.
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Page/Page column 109; 110
(2014/02/16)
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- NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITION AND METHODS THEREOF
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Disclosed are novel heteroaryl and heterocycle compounds of formula I-1, I-2 or I-3 and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune diseases and cancer.
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Page/Page column 136; 137
(2014/02/16)
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- Efficient synthesis of DOPA analogues in pepticinnamins E via asymmetric catalytic hydrogenation of dehydroamino esters
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One practical synthetic procedure with five steps was developed to prepare a series of N-protected-2-(diethoxyphosphoryl)glycinates with good yields, which was treated with aldehydes under mild condition to give different dehydroamino esters with high yields and excellent Z/E selectivity. The subsequently homogeneous enantioselective hydrogenation of the dehydroamino esters affords a series of new DOPA analogues.
- Sun, De-Qun,Sun, Li,Luo, Min
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experimental part
p. 1731 - 1734
(2012/08/28)
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- Bicyclic heterocycles as cannabinoid receptor modulators
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The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R3a, R4, A, B, n, Y and Z are described herein.
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Page/Page column 8
(2008/06/13)
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- Bicyclic heterocycles as cannabinoid receptor modulators
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The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds a
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Page/Page column 7
(2008/06/13)
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- Bicyclic heterocycles as cannabinoid receptor modulators
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The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds a
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Page/Page column 7
(2008/06/13)
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- C-linked galactosyl serine AFGP analogues as potent recrystallization inhibitors
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(Chemical Equation Presented) A series of C-linked antifreeze glycoprotein analogues have been prepared to evaluate antifreeze activity as a function of distance between the carbohydrate moiety and polypeptide backbone. The building blocks for these analogues were prepared using either an olefin cross-metathesis or catalytic asymmetric hydrogenation. Analysis of antifreeze protein-specific activity revealed that only analogue 2a (n = 1) was a potent recrystallization inhibitor and thus has potential medical and industrial applications.
- Liu, Suhuai,Ben, Robert N.
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p. 2385 - 2388
(2007/10/03)
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- Synthesis of the C-analog of 2-acetylamino-2-deoxy-β-D-glucopyranosyl L- and D-serine
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Glucosamine was transformed into N-tetrachlorophthaloyl-protected fluoride 5 which gave with allyltrimethylsilane as C-nucleophile in the presence of BF3·OEt2 as catalyst β-C-allyl derivative 6 in good yield. Removal of the TCP group
- Fuchss, Thomas,Schmidt, Richard R.
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p. 753 - 758
(2007/10/03)
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- Phosphono analogues of glutathione as new inhibitors of glutathione S-transferases
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Phosphono-analogues of glutathione containing the O=P(OR)2 moiety in place of the cysteinyl residue CH2SH 1a-1d were prepared by solution phase peptide synthesis. Benzyl, benzyloxycarbonyl, and tert-butyl protecting groups were used
- Kunze, Thomas
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p. 503 - 509
(2007/10/03)
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- A convenient synthesis of 2-(diethoxyphosphonyl)glycine and its derivatives
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A simple and very efficient method for the preparation of 2-(diethoxyphosphonyl)glycine and its N-methyl analog as the free acids is described and their conversion to the corresponding t-butyl esters demonstrated.
- Shankar,Scott
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p. 231 - 234
(2007/10/02)
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- FACILE SYNTHESIS OF α-PHOSPHORYLATED α-AMINO ACIDS
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Various α-phosphorylated α-amino acid derivatives were synthesized conveniently by the reaction of methyl α-methoxyhippurate and methyl α-methoxy-N-benzyloxycarbonyl-glycinate with phosphites under the Lewis acid.Hydrolysis of (12) with TMSI gave 2-phosph
- Ku, Bonchul,Oh, Dong Young
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p. 4465 - 4466
(2007/10/02)
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