- Synthesis of Flubromazepam Positional Isomers for Forensic Analysis
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Designer benzodiazepines have recently appeared in many forensic cases as legal alternatives to federally scheduled drugs such as diazepam (Valium) and alprazolam (Xanax). Though current forensic instrumental techniques are often sufficient for identifying novel psychoactive substances, they may not readily differentiate between potential positional isomers. Additionally, characterization data for positional isomers of known designer benzodiazepines are widely nonexistent. In this study, flubromazepam, a recognized designer benzodiazepine since 2012, was targeted for synthesis and characterization due to its potential for federal scheduling and current legal status within the United States. A practical synthetic method was developed to prepare purified reference materials for each positional isomer of flubromazepam in which the positions of the bromine and fluorine substituents were varied. Possible isomers (9 of the 12) were successfully prepared and used for further analysis.
- Allred, B. McKay,France, Stefan,Jones, Lonnie V.,Ligon, Evelyn S.,Nawyn, Jason,Reinhardt, Daniel V.
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- Quinoline Compounds
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The present invention relates to novel compounds of the general formula (I) wherein R1, R4, R5 and X are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparatio
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Page/Page column 5; 7
(2009/04/24)
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- New vistas in quinoline synthesis
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The gold-catalyzed Friedlander reaction was applied to the condensation of 2-aminoarylketones with β-keto-esters, β-diketones, β-keto-amides, and β-keto-sulfones to afford a diverse range of 2,3,4-trisubstituted quinolines in 3-82% yield. The seven-membered rings 1,3-cycloheptadione and azepane-2,4-dione reacted smoothly in 75% yield. An alternative procedure for the synthesis of 3-(methanesulfonyl)quinolines was developed and provided an entry into late stage manipulation of the 4-position of these quinolines. The requisite 2-aminoarylketones for the Friedlander reaction were prepared in one pot by modified Sugasawa reaction using gallium(III) chloride and boron(III) chloride in 12-54% yield.
- Atechian, Sarkis,Nock, Nadine,Norcross, Roger D.,Ratni, Hassen,Thomas, Andrew W.,Verron, Julien,Masciadri, Raffaello
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p. 2811 - 2823
(2007/10/03)
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- Quinolines as allosteric enhancers of the GABAB receptors
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The present invention relates to compounds of formula I wherein R1 to R6 are as described herein, which compounds are active at the GABAB receptor and can be used for the preparation of medicaments useful in the treatment of CNS disorders comprising anxiety and depression.
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Page/Page column 10
(2008/06/13)
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- 3-Methanesulfonylquinolines as GABAB enhancers
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The present invention relates to compounds of formula I wherein R1, R2 and R3 are as defined in the specification, which are active at the GABAB receptor and which can be used for the treatment of CNS disorders.
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Page/Page column 9
(2010/11/25)
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- Indazole compounds, compositions thereof and methods of treatment therewith
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This invention is generally directed to the use of Indazole Compounds for treating or preventing diseases associated with protein kinases, including tyrosine kinases, such as proliferative diseases, inflammatory diseases, abnormal angiogenesis and diseases related thereto, atherosclerosis, macular degeneration, diabetes, obesity, pain and others. The methods comprise the administration to a patient in need thereof of an effective amount of an indazole compound that inhibits, modulates or regulates tyrosine kinase signal transduction. Novel indazole compounds or pharmaceutically acceptable salt thereof are presented herein.
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- Methods for treating an inflammatory condition or inhibiting JNK
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This invention is generally directed to Indazole Derivatives having the following structure: 1 or pharmaceutically acceptable salt thereof, wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of diseases and disorders that are responsive to JNK inhibition, such as an inflammatory disease or disorder. Thus, methods of treating such diseases and disorders are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
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- Design and Synthesis of 4-Azaindoles as Inhibitors of p38 MAP Kinase
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Inhibition of the biosynthesis of proinflammatory cytokines such as tumor necrosis factor and interleukin-1 via p38 has been an approach toward the development of a disease modifying agent for the treatment of chronic inflammation and autoimmune diseases.
- Trejo, Alejandra,Arzeno, Humberto,Browner, Michelle,Chanda, Sushmita,Cheng, Soan,Comer, Daniel D.,Dalrymple, Stacie A.,Dunten, Pete,Lafargue, JoAnn,Lovejoy, Brett,Freire-Moar, Jose,Lim, Julie,McIntosh, Joel,Miller, Jennifer,Papp, Eva,Reuter, Deborah,Roberts, Rick,Sanpablo, Florentino,Saunders, John,Song, Kyung,Villasenor, Armando,Warren, Stephen D.,Welch, Mary,Weller, Paul,Whiteley, Phyllis E.,Zeng, Lu,Goldstein, David M.
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p. 4702 - 4713
(2007/10/03)
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- Indazole derivatives as JNK inhibitors and compositions and methods related thereto
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Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
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