- 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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- Pharmacologically active CNS compound
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The invention provides a series of compounds of formula (I) and salts thereof, wherein for example,R1 and R2, which may be the same or different each represent -NR13R14 where R13 and R14 may each independently represent hydrogen or alkyl or, taken together with the nitrogen atom to which they are attached form a heterocyclic ring, optionally substituted by one or more alkyl or arylalkyl groups and optionally containing a further heteroatom;, R3 is hydrogen, haloalkyl, alkoxymethyl or alkyl;, R4 is hydrogen, nitro or halo;, R5 is hydrogen or halo;, R6 is hydrogen, halo, nitro, amino, alkylamino or dialkylamino;, R7 is hydrogen or halo;, R8 is hydrogen or halo; The compounds may be used for the treatment or prophylaxis of a neurodegenerative or other neurological disorder of the CNS, the aetiology or which includes excessive release of the neurotransmitter glutamate.
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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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