- THIAZOLYL COMPOUNDS USEFUL AS KINASE INHIBITORS
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The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease
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Page/Page column 61
(2008/12/04)
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- Novel piperidinecarboxamide derivatives, method for preparing same and pharmaceutical compositions containing same
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The invention relates to compounds of formula: as well as their salts with inorganic or organic acids, their solvates and/or their hydrates, which exhibit a very high affinity both for the human NK2 receptors for neurokinin A and for the human NK3 receptors for neurokinin B and are antagonists of the said receptors. The invention also relates to their method of preparation, the pharmaceutical compositions containing them and their use for the preparation of medicaments.
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Page/Page column 6; 10
(2010/02/08)
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- Optically active phenyl pyrimidine derivatives as analgesic agent
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PCT No. PCT/EP96/03856 Sec. 371 Date Feb. 26, 1998 Sec. 102(e) Date Feb. 26, 1998 PCT Filed Sep. 3, 1996 PCT Pub. No. WO97/09317 PCT Pub. Date Mar. 13, 1997A pyrimidine of formula (I) and its pharmaceutically acceptable acid addition salts are useful as a
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- METABOLISM OF CHLOROPHENYLALANINES IN CROP AND WEED PLANTS IN RELATION TO THE FORMATION OF POTENTIAL HERBICIDAL END PRODUCTS
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Metabolism of 12 synthetic D,L-chlorophenylalanines has been examined in several crop and weed plants.Twenty-five gram samples of excised shoots or leaves of bushbean, soybean, corn, pigweed, lambsquarters, and giant foxtail were allowed to metabolize 10-4 M solutions of the D,L-chlorophenylalanines for 24 hr in continuous light.The plant samples were then extracted in 80percent methanol and the soluble acidic metabolites fractionated into ether.Each ether concentrate was partially purified by fractional elution from a PrepSep C18 coloumn and then analysed by HPLC.Collected fractions were esterified with pentafluorobenzylbromide and examined by GC-MS to demonstrate the presence of PFB-esters of chlorophenylacetic, chlorobenzoic and/or chlorocinnamic acids.Since certain of these metabolites are known to be potent plant growth-regulators and herbicides, the results are discussed in relation to the potantial herbicidal action of certain chlorophenylalanines by the mechanism of 'lethal synthesis'.Key Word Index - Phaseolus vulgaris; Glycine max.; Leguminosae; Zea mays; Amaranthus retroflexus; Chenopodium album; Setaria faberii; metabolism; D,L-chlorophenylalanines; chlorophenylacetic acids; chlorobenzoic acids; chlorocinnamic acids; growth regulators.
- Taylor, David C.,Wightman, Frank,Kazakoff, Clem W.
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- Antihypertensive Activity of 6-Arylpyridopyrimidin-7-amine Derivatives
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A series of 51 6-arylpyridopyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat.A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyridopyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg.Normalized blood pressure levels could then be maintained by single daily oral doses.The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.
- Bennett, Lawrence R.,Blankley, C. John,Fleming, Robert W.,Smith, Ronald D.,Tessman, Deirdre K.
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p. 382 - 389
(2007/10/02)
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