- GLUCAGON ANTAGONISTS/INVERSE AGONISTS
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A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-
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Page/Page column 162
(2010/02/14)
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- Glucagon antagonists/inverse agonists
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Disclosed is a novel class of compounds of formula (I) wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
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- GLUCAGON ANTAGONISTS/INVERSE AGONISTS
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A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
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- Glucagon antagonists/inverse agonists
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Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorde
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- Glucagon antagonists/inverse agonists
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A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases
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- Glucagon antagonists/inverse agonists
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A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.
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- Syntheses of Amine Derivatives of Phencyclidine
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3-Aminophencyclidine (5) was synthesized by reduction of 3-nitrophencyclidine (3) using either H2 with Pd/C or Na2S in refluxing methanol.Attempts to isolate 4-aminophencyclidine (2), which we hoped to synthesize by hydrolysis of carbamate 15 which was isolated after reaction of amide 10 under Hofmann conditions employing bromine in CH3O(1-)/CH3OH at -40 deg C, were unsuccessful. 4-Aminomethylphencyclidine (18) was synthesized by LAH reduction of nitrile 13 as well as by reductive amination of aldehyde 20.Nitrile 13 and aldehyde 20 were synthesized from 4-bromophencyclidine (11) as was alcohol 26 which served as a precursor to 4-(2-aminoethyl)phencyclidine (19).Amine 19 was also synthesized by NaBH4 reduction of β-nitrostyrene 29 which was generated from aldehyde 20 by condensation with nitromethane using 1,5-diazabicycloundecene as the base catalyst followed by LAH reduction of resulting 4-(2-nitroethyl)phencyclidine (30).Mass spectra and 13C NMR spectra have been obtained on most of the phencyclidine derivatives.
- Johnson, Peter Y.,Pan, Robert,Wen, Jing Quan,Halfman, Clarke J.
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p. 2049 - 2054
(2007/10/02)
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- Derivatives of 6,7 or 8 cycloalkyl 4-oxo quinoline 3 carboxylic acid
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wherein Ph denotes a 1,2-phenylene radical which carries cycloaliphatic radical, Rx denotes a free or etherified hydroxyl group or a free or substituted amino group, Ro denotes an alkyl radical, a free hydroxyl group or a hydroxyl group etherified by lower alkyl or, above all, a hydrogen atom and R1 denotes an aliphatic or cycloaliphatic hydrocarbon radical which is optionally substituted by hydroxyl, an araliphatic radical or a hydrogen atom, and their salts, which possess valuable analgesic, anti-inflammatory, anti-microbial and histamine liberation inhibiting properties.
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