- HETEROCYCLIC AMIDES USEFUL FOR THE TREATMENT OF CANCER AND PSORIASIS
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The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2or R3 is (Z).
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Page/Page column 111
(2009/04/25)
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- MELANOCORTIN TYPE 4 RECEPTOR AGONIST PIPERIDINOYLPYRROLIDINES
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The present invention relates to a class of melanocortin MCR4 agonists of general formula (I), wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
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Page/Page column 61-62
(2008/06/13)
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- PYRIDYL AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS
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The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
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Page/Page column 40-41
(2008/06/13)
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- Preparation and antioxidant activity of α-pyridoin and its derivatives
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Focusing on α-pyridoin (1, 1,2-di(2-pyridyl)-1,2-ethenediol) as the lead compound of the novel antioxidative enediol, we synthesized 5,5′- or 6,6′-bis-substituted derivatives of 1 from disubstituted pyridines. The antioxidant activity of 1 and its synthetic derivatives 2-7 was evaluated by DPPH (1,1-diphenyl-2-picrylhydrazyl radical) scavenging assay and inhibition of lipid peroxidation. In the DPPH assay, 1 exhibited an activity stronger than that of ascorbic acid, and 5,5′-dimethyl-(5) or 5,5′-dimethoxy- substituted derivatives (6) exhibited more potent activity than 1. The DPPH scavenging activities of α-pyridoins were correlated with their oxidation potential and thus the electron density of enediol. 5 and 6 effectively inhibited lipid peroxidation in the rat liver microsome/tert-butyl hydroperoxide system. Therefore, 5 and 6 serve as good candidates for a pharmacologically useful enediol antioxidant.
- Hatanaka, Masashi,Takahashi, Kyoko,Nakamura, Shigeo,Mashino, Tadahiko
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p. 6763 - 6770
(2007/10/03)
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- Synthesis of (R)-(+)-methyl 3-amino-3-(5-hydroxy-2-pyridinyl)propanoate, an analog of L-azatyrosine
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A concise asymmetric synthesis of (R)-(+)-methyl 3-amino-3-(5-hydroxy-2-pyridinyl)propanoate 2, a β-amino acid analog of L-azatyrosine 1 starting from the commercially available (-)-Andersen reagent (-)-3 in good overall yield is described.
- Adamczyk, Maciej,Reddy, Rajarathnam E.
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p. 1047 - 1054
(2007/10/03)
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- Intramolecular alkylation of aromatic compounds, XXXIV: Synthesis of pyridinylmethyl indolines as potential precursors of ergolines
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The carbinoles 3 prepared from the N-protected indolaldehydes 2 and bromomethoxypyridine 1 can smoothly be hydrogenolized to the lutidinylindoles 4 which in turn give the corresponding indolines 5 by NaCNBH3-reduction. Treatment of 3a by acid the trihetarylmethane 9 and 5-methoxypyridine-2-carboxaldehyde 10 are generated. The acetylpyridine 7 is found as a by-product of 3c. As by-product of the reduction the borane adduct 8 is detected.
- Reimann,Erdle
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p. 907 - 912
(2007/10/03)
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