- SUBSTITUTED HETEROCYCLIC AZA DERIVATIVES
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The invention relates to heterocyclic aza derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 143; 144
(2013/03/26)
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- Substituted Heterocyclic Aza Compounds
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Heterocyclic aza compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also methods of using these compounds for the treatment and/or inhibition of pain and further diseases and/or disorders.
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Paragraph 0816
(2013/03/26)
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- Inhibition studies with rationally designed inhibitors of the human low molecular weight protein tyrosine phosphatase
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The human low molecular weight protein tyrosine phosphatase (HCPTP) is ubiquitously expressed as two isoforms in a wide range of human cells and may be involved in regulating the metastatic nature of epithelial tumors. A homology model is presented for th
- Zabell, Adam P. R.,Corden, Steven,Helquist, Paul,Stauffacher, Cynthia V.,Wiest, Olaf
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p. 1867 - 1880
(2007/10/03)
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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Page/Page column 24
(2010/01/31)
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- Modified aminoacids, pharmaceuticals containing these compounds and method for their production
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The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4and R11are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
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Example A3b)
(2008/06/13)
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- Synthesis of 6,6'-diamino-2,2'-biquinoline and 2,2'-bi-1,6- naphthyridine
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High-yield synthesis and characterization of the new heterocycles 6,6'- diamino-2,2'-biquinoline (3), 6,6'-bis(N,N-dimethyl-amino)-2,2'-biquinoline (4), and 2,2'-bi-1,6-naphthyridine (5) are described. The preparation of 3 and 4 is based on the coupling of 2-amino-6-chloroquinoline and 2-chloro-6- dimethylaminoquinoline in the presence of NiCl2·6H2O/PPh3/Zn in DMF (NiCRA). Compound 5 was synthesized through a condensation reaction of 4- aminopyridine-3-carbaldehyde and butane-2,3-dione.
- Janiak, Christoph,Deblon, Stephan,Uehlin, Lars
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p. 959 - 964
(2007/10/03)
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- Regiospecific Electrophilic Substitution of Aminopyridines: Ortho Lithiation of 2-, 3-, and 4-(Pivaloylamino)pyridines
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2- and 4-(pivaloylamino)pyridines have been shown to undergo metalation exclusively at C-3 and these smoothly react with a variety of electrophiles to produce 2,3- and 3,4-disubstituted pyridines, respectively.Removal of the pivaloyl protecting group results in overall electrophilic substitution of an aminopyridine.Utilization of this method is exemplified by efficient syntheses of 2- and 4-aminonicotinaldehydes.Minor modifications of the reaction conditions permitted exclusive ortho metalation of 2-(pivaloylamino)pyridines additionally functionalized by chloro, fluoro, or methyl groups.Although the major product from reaction of 3-(pivaloylamino)pyridine by this method was metalation at C-4, the reaction was complicated by substantial quantities of product derived from nucleophilic attack by n-butyllithium on the pyridine nucleus.
- Turner, James A.
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p. 3401 - 3408
(2007/10/02)
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