- FUSED BICYCLIC ISOXAZOLINES AS INHIBITORS OF CHOLESTEROL ESTER TRANSFER PROTEIN
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Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is (CH2) or O, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or pr
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Page/Page column 39
(2015/07/07)
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- Coupling reactions of aryl bromides with 1-alkynols catalysed by a tetraphosphine/palladium catalyst
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cis,cis,cis-1,2,3,4-Tetrakis(diphenylphosphinomethyl)cyclopentane/ [PdCl(C3H5)]2 system catalyses efficiently the coupling reactions of aryl halides with a variety of alkynols such as propargyl alcohol, but-1-yn-4-ol, pent
- Feuerstein, Marie,Doucet, Henri,Santelli, Maurice
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p. 1603 - 1606
(2007/10/03)
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- Novel 5-(3-aryl-2-propynyl)-5-(arylsulfonyl)thiazolidine-2,4-diones as antihyperglycemic agents
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Novel 5-(3-aryl-2-propynyl)-5-(arylsulfonyl)thiazolidine-2,4-diones and 5-(3-aryl-2-propynyl)5-(arylsulfanyl)thiazolidine-2,4-diones were prepared and evaluated as oral antihyperglycemic agents in the obese, insulin resistant db/db mouse model at 100 mg/kg and, if the analogue had sufficient potency, 20 mg/kg. The sulfonylthiazolidinediones, 2, were more potent than the corresponding sulfanylthiazolidinedione congeners, 1. With regard to substituent effects on the 3-propynyl phenyl ring (Ar') of 2, 4-halogen substitution generally resulted in the more potent analogues. Substituent effects on the phenylsulfonyl moiety (Ar) of 2 were less clear, although para-halogen substitution on Ar generally was preferable. 2-Pyridinesulfonyl derivatives (Ar = 2-pyridine in 2) also had good potency. Several compounds from series 2 were effective at lowering glucose and insulin in the obese, insulin resistant ob/ob mouse at the 50 mg/kg oral dose. Compound 20 significantly improved the glucose tolerance of obese, insulin resistant Zucker rats at the 20 mg/kg dose level and had no effect on plasma glucose or on glucose tolerance in normal rats fasted for 18 h at the 100 mg/kg level.
- Wrobel, Jay,Li, Zenan,Dietrich, Arlene,McCaleb, Michael,Mihan, Brenda,Sredy, Janet,Sullivan, Donald
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p. 1084 - 1091
(2007/10/03)
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- Rodenticidal 1-(3,5-bistrifluoromethylphenyl)-3-(4-t-butylpiperidino)prop-1-yne
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The hitherto unknown phenylpropargylamine derivative 1-(3,5-bistrifluoromethylphenyl)-3-(4-tert-butylpiperidino)prop-1-yne, and acid addition salts thereof, have been found to be useful for killing warm-blooded vermin, especially rodents. Processes for the preparation of the new phenylpropargylamine derivative are described and so are suitable rodenticidal compositions.
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