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Title:
NOVEL TRIFLUOROMETHYLEPINEPHRINE COMPOUNDS AND METHODS OF MAKING AND USING THEREOF
Document Type and Number:
WIPO Patent Application WO2003103609
Kind Code:
A3
Abstract:
Disclosed herein are trifluoromethylepinephrine compounds having the following structural formula (I) wherein R<1>-R<5> are each independently selected from the group consisting of H, alkyl, alkoxyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, acyl, thioacyl, sulfonyl mercapto, alkylthio, carboxy, amino, alkylamino dialkylamino, carbamoyl, arylthio, and heteroarylthio; wherein X, Y, and Z are each independently selected from the group consisting of H or trifluoromethyl with the proviso that at least one of which is trifluoromethyl. Also disclosed are pharmaceutical compositions comprising the trifluoromethylepinephrine compounds and methods of making and using thereof. Novel trifluoroepinephrine intermediates are also disclosed.

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Inventors:
AMMANN JEFFREY R (US)
Application Number:
PCT/US2003/005976
Publication Date:
April 08, 2004
Filing Date:
February 28, 2003
Export Citation:
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Assignee:
US ARMY MED RES MAT COMMAND (US)
AMMANN JEFFREY R (US)
International Classes:
C07C211/27; C07C215/78; C07C217/70; C07C217/84; C07C217/86; C07C233/18; C07F7/04; C07F7/10; C07F7/18; (IPC1-7): C07C233/05; A61K31/135; A61K31/16; A61K31/275; C07C215/08; C07C255/03
Other References:
LU SHOU-FU ET AL.: "Syntheses of (R) and (S)-2- and 6-fluoronorepinephrine and (R) and (S)-2- and 6-fluoroepinephrine: Effect of stereochemistry on fluorine-induced adrenergic selectivities", J. MED. CHEM., vol. 43, April 2000 (2000-04-01), pages 1611 - 1619, XP002972692
MARKOVICH K.M. ET AL.: "Synthesis of helogenated trimetoquinol derivatives and evaluation of their beta agonist and thromboxane A2 (TXA2) antagonist activities", J. MED. CHEM., vol. 35, 1992, pages 466 - 479, XP002972693
See also references of EP 1487784A4
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