The invention relates to novel compounds which are both phosphodiesterase 4 (PDE4) enzymeinhibitorsand muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
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Page/Page column 63; 64
(2016/12/22)
THE (S)-ENANTIOMER OF MEPAZINE
The present invention relates to the (S)-enantiomer of mepazine, its applicability in therapy, a pharmacological composition comprising (S)-mepazine, and processes for the preparation of (S)- mepazine and one of its intermediates.
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Page/Page column 43; 44
(2015/01/16)
Structural analysis of phenothiazine derivatives as allosteric inhibitors of the MALT1 paracaspase
Second site: In the crystal structure of human MALT1casp-Ig3 (mucosa-associated lymphoid tissue lymphoma translocation protein 1) in complex with the tricyclic phenothiazine derivative thioridazine (violet in the picture), the inhibitor is bound in a hydrophobic pocket far from the active site. This explains the action of phenothiazine derivatives as noncompetitive, reversible inhibitors. Copyright
Schlauderer, Florian,Lammens, Katja,Nagel, Daniel,Vincendeau, Michelle,Eitelhuber, Andrea C.,Verhelst, Steven H. L.,Kling, Dale,Chrusciel, Al,Ruland, Juergen,Krappmann, Daniel,Hopfner, Karl-Peter
supporting information
p. 10384 - 10387
(2013/10/21)
PIPERAZINES AS ANTI-OBESITY AGENTS
The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
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Page/Page column 34-35
(2009/07/17)
METHODS OF USE FOR INHIBITORS OF AKT ACTIVITY
Invented is the use of 1 H-imidazo[4,5-c]pyridin-2-yl compounds in the treatment of specified cancers.
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Page/Page column 48
(2008/12/04)
INHIBITORS OF AKT ACTIVITY
Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 54
(2008/06/13)
N-HETEROCYCLYL-SUBSTITUTED AMINO-THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS
Aminothiazole compounds with N-containing cycloalkyl at the 2-amino position which are represented by the Formula (I), or a pharmaceutically acceptable prodrug of said compound, or pharmaceutically acceptable salt of said compound, modulate and/or inhibit the cell proliferation and activity of protein kinases.
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Page 112
(2010/02/08)
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