- COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
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Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.
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Paragraph 0591
(2017/03/14)
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- New nucleotide-competitive non-nucleoside inhibitors of terminal deoxynucleotidyl transferase: Discovery, characterization, and crystal structure in complex with the target
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Terminal deoxynucletidyl transferase (TdT) is overexpressed in some cancer types, where it might compete with pol μ during the mutagenic repair of double strand breaks (DSBs) through the nonhomologous end joining (NHEJ) pathway. Here we report the discove
- Costi, Roberta,Cuzzucoli Crucitti, Giuliana,Pescatori, Luca,Messore, Antonella,Scipione, Luigi,Tortorella, Silvano,Amoroso, Alessandra,Crespan, Emmanuele,Campiglia, Pietro,Maresca, Bruno,Porta, Amalia,Granata, Ilaria,Novellino, Ettore,Gouge, Jéro?me,Delarue, Marc,Maga, Giovanni,Di Santo, Roberto
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p. 7431 - 7441
(2013/10/21)
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- PHARMACEUTICAL PREPARATIONS COMPRISING INSULIN, ZINC IONS AND A ZINC-BINDING LIGAND
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Novel preparations comprising branched ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The preparations have a prolonged action designed for flexible injection regimes.
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Page/Page column 230
(2008/06/13)
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- PHAMACEUTICAL PREPARATIONS COMPRISING INSULIN
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Novel preparations comprising ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer wherein the ligand is extended by protamine that are capable of prolonging the ac-tion of insulin preparations.
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Page/Page column 225
(2010/02/15)
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- Stabilised insulin compositions
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The present invention provides pharmaceutical compositions comprising insulin and novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The resulting preparations have improved physical and chemical stability.
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Page/Page column 120
(2008/06/13)
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- Solid-phase composite carrier and method
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Functionalized supports and methods for solid phase synthesis. Preferably, the functionalized support is azlactone-functionalized.
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Page/Page column 26
(2010/02/10)
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- PHARMACEUTICAL PREPARATIONS COMPRISING ACID-STABILISED INSULIN
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Novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer that are capable of prolonging the action of insulin preparations are disclosed.
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Page/Page column 226
(2010/02/08)
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- Novel ligands for the hisb10 zn2+ sites of the r-state insulin hexamer
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Novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer that are capable of prolonging the action of insulin preparations are disclosed.
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- Case studies in process screening and optimization utilizing a new automated reactor - Analysis system
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The application of a new automated workstation for conducting solution-phase reactions in parallel during chemical process development is described. The fully automated reactor - analysis system is capable of reagent/reactant addition, temperature and agitation control, and sample extraction/quench/injection for online HPLC analysis. Both precision and accuracy of the fluidic delivery and sampling systems were measured through the use of standard ultraviolet chromophore solutions in conjunction with HPLC analysis. Agitation efficiency was evaluated using a phase-transfer catalysis reaction known to be rate-dependent on stirring frequency. Chemistry cases examined included several single and multistep reactions studied to identify the best reagent/solvent combinations (screening) and optimal levels of continuous variables such as temperature, concentration, and stoichiometry (optimization). A multistep route to a chiral substituted imidazolidin-2-one was developed from initial route scouting through reaction condition screening, optimization, and scale-up. Reactions performed included alkylation, reduction, oxidation, reductive amination, displacement, and cyclization.
- Gooding, Owen W.,Lindberg, Thomas,Miller, Wendy,Munyak, Edward,Vo, Lanchi
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p. 283 - 293
(2013/09/07)
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- Improved functionalized resin for chemical synthesis
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A support functionalized by an indole or pyrrole aldehyde is useful for the solid phase synthesis of amide type compounds.
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- Indanediones-1,3 VIII. Hydroxy-2 indolyl-2 indanediones-1,3, (indolyl-3 methylene)-2 indanediones-1,3 et derives: recherche d'une activite anti-inflammatoire
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1,3-Indandiones VIII. 2-Hydroxy-2-indolyl-1,3-indandiones, 2-(indol-3-ylmethylene indandione and derivatives: search for anti-inflammatory activity.A series of 2-hydroxy-2-indolyl-1,3-indandiones, diversely substituted on the heterocycle were synthetized in order to study their anti-inflammatory activity.Catalytic hydrogenation gave 2,3-dihydroxy-1 indanones 6 and NaBH4 reduction of 3i led to the corresponding indanetriol 7i.Base-catalyzed isomerization of hydroxy-β-diketones 3 furnished 3-indololylcarbonyl phthalides 9.Only compound 3d exhibited a significant inhibition of mouse paw edema.Experimentation in the rat paw edema test confirmed the anti-inflammatory effect of 3d, but it was associated with an anti-coagulant activity. ω-Amino-alkylation of the indole nitrogen of 3d led to loss of anti-inflammatory activity.Introduction of a double bond between the indandione and indole nuclei, leading to 2-(indol-3-ylmethylene)-1,3 indandiones 12, proved ineffective in raising this activity. 2-hydroxy-2-indolyl-1,3-indandiones/ 2,3-dihydroxyindanones/ 1,2,3-indantriols/ 3-indolylcarbonyl-phthalides/ 2-(indol-3-ylmethylene)-1,3-indandiones/ anti-inflammatory activity/ anti-coagulant activity
- Courant, Jacqueline,Leblois, Danielle,Tandon, Manju,Robert-Piessard, Sylvie,le Baut, Guillaume,et al.
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p. 145 - 154
(2007/10/02)
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