- Synthesis of further amino-halogen-substituted phenyl-aminoethanols
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Starting from clenbuterol as a lead structure, new 4-amino-phenyl-aminoethanol analogues have been synthesized by different approaches. In these compounds one or both of the chlorine atoms of clenbuterol are replaced by other residues. This has led to compounds with high intrinsic β2-mimetic and/or β1-blocking activities. 1-(4-Amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-ethanol hydrochloride (mabuterol) has been selected for clinical development. A detailed description is also given of the syntheses of new intermediate acetophenone derivatives as well as of the resolution of mabuterol into its enantiomers.
- Kruger,Keck,Noll,Pieper
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p. 1612 - 1624
(2007/10/02)
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- Phenylethanolamine derivatives and acid addition salts thereof for enhancing the growth rate of meat-producing animals and improving the efficiency of feed utilization thereby
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There is provided a method for enhancing the growth rate of meat-producing animals and/or improving the efficiency of feed utilization thereby, which involves, orally or parenterally, administering to said animals a growth-enhancing amount of a phenylethane compound or the acid addition salt thereof.
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- Phenylethanolamine derivatives and acid addition salts thereof for the depression of fat deposition in warm blooded animals
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There is provided a method for increasing lean meat deposition and/or improving lean meat to fat ratio in poultry, domestic pets, sheep, swine, rabbits, goats and cattle by administering, orally or parenterally, to said animals an effective amount of a phenylethane derivative or acid salt thereof.
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- Antiphlogistic pharmaceutical compositions containing a phenylethanolamine and methods of use
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The method of using compounds of the formula STR1 wherein R1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano, R2 is fluorine, cyano, trifluoromethyl, nitro or alkyl of 1 to 4 carbon atoms, R3 is cycloalkyl or alk
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- BRONCHOSPASMOLYTIC 1-(P-AMINO-PHENYL)-2-AMINO-ETHANOLS-(1) AND SALTS
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Racemic and optically active compounds of the formula wherein R1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano, R2 is fluorine, trifluoromethyl, nitro or cyano, and R3 is alkyl of 3 to 5 carbon atoms, hydroxy(alkyl of 3 to 5 carbon atoms), cycloalkyl of 3 to 5 carbon atoms, 1-(3,4-methylenedioxy-phenyl)-2-propyl or 1-(p-hydroxy-phenyl)-2-propyl, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as analgesics, uterospasmolytics, bronchospasmolytics and antispastics for the skeletal musculature, and especially as beta 2-receptor mimetics and beta 1-receptor blockers
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