- Synthesis of New Propargylated 1-Pyrindane Derivatives as Rasagiline Analogues
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Rasagiline is a compound with important neuroprotective activity applicable to the treatment of neurodegenerative diseases. This work describes an easy and straightforward methodology to the synthesis of new propargylated rasagiline analogues derived from commercially available 6,7-dihydro-5H-cyclopenta[b] pyridine. Georg Thieme Verlag Stuttgart - New York.
- Pereira, Cidáliasilva,Salgado, Sofia,Rizzo-Aguiar, Fabio,Garcia-Mera, Xerardo,Rodríguez-Borges, Josée.
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- SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE
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The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.
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- Reaction of 2-alkyl pyridine N-oxide derivatives with Mosher's acyl chloride: First example of stereoselective Boekelheide rearrangement
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Treatment of 2-alkyl pyridine N-oxides with acylating reagents represents an established procedure for the introduction of oxygen functionality into alkyl group at the ortho position of N heteroaromatic rings. We have reported the first example of asymmet
- Andreotti, Daniele,Miserazzi, Emanuele,Nalin, Arnaldo,Pozzan, Alfonso,Profeta, Roberto,Spada, Simone
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scheme or table
p. 6526 - 6530
(2011/02/24)
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- SUBSTITUTED FLUOROETHYL UREAS AS ALPHA 2 ADRENERGIC AGENTS
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Therapeutic compounds, and methods, compositions, and medicaments related thereto are disclosed herein.
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Page/Page column 32
(2008/12/04)
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- Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H- indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management
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Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical companies in an effort to identify novel agents for pain management. Here we report that replacement of substituted benzyl groups by an indan rigid moiety in a previously described N-indazole-N′-benzyl urea series led to a number of TRPV1 antagonists with significantly increased in vitro potency and enhanced drug-like properties. Extensive evaluation of pharmacological, pharmacokinetic, and toxicological properties of synthesized analogs resulted in identification of (R)-7 (ABT-102). Both the analgesic activity and drug-like properties of (R)-7 support its advancement into clinical pain trials.
- Gomtsyan, Arthur,Bayburt, Erol K.,Schmidt, Robert G.,Surowy, Carol S.,Honore, Prisca,Marsh, Kennan C.,Hannick, Steven M.,McDonald, Heath A.,Wetter, Jill M.,Sullivan, James P.,Jarvis, Michael F.,Faltynek, Connie R.,Lee, Chih-Hung
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p. 392 - 395
(2008/09/17)
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- Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals
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The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines of the formula I, in which A, R1, R2, R3, R4, R5 and n have the meanings indicated in the claims. The compounds of fo
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Page/Page column 21
(2010/02/05)
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- β-Amino Ketones as Key Intermediates in the Synthesis of Pyridines: A Novel and Efficient Route to Annelated Bi- and Terpyridines
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The hydrochlorides of β-amino ketones 1a-e (Mannich bases) are easily obtained starting compounds for a novel synthesis of pyridines.Condensation with the heteroaromatic ketones 8, 9, and 10 yields 5,6-dihydro-1,10-phenanthrolines 3a-d, 13 and 4,5-diazafluorenes 4a-d, which have not yet been described in literature.Symmetrical terpyridines 3e, 4e are formed in a one-step reaction of 8, 9 with dimethylmethylenammonium chloride in the presence of an ammonia source.
- Westerwelle, Ulrich,Esser, Achim,Risch, Nikolaus
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p. 571 - 576
(2007/10/02)
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- Polyaza Cavity Shaped Molecules. Annelated Derivatives of 2-(2'-Pyridyl)-1,8-naphthyridine and 2,2'-Bi-1,8-naphthyridine
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A two-step method is presented for the oxidation of the 2-methylene position of 2,3-cycloalkenopyridines.The pyridyl ketones thus obtained may be reacted with 2-aminonicotinaldehyde to yield 3,3'-annelated derivatives of 2-(2'-pyridyl)-1,8-naphthyridine.T
- Thummel, Randolph P.,Lefoulon, Francois,Cantu, David,Mahadevan, Ramanathan
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p. 2208 - 2212
(2007/10/02)
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