- Synthesis and biological evaluation of potent bisubstrate inhibitors of the enzyme catechol O-methyltransferase (COMT) lacking a nitro group
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Inhibition of the enzyme catechol O-methyltransferase (COMT) represents a viable strategy for regulation of the catabolism of catecholamine neurotransmitters or their precursors, and is of considerable interest in the therapy of Parkinson's, disease. Here
- Paulini, Ralph,Lerner, Christian,Diederich, Francois,Jakob-Roetne, Roland,Zuercher, Gerhard,Borroni, Edilio
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p. 1856 - 1887
(2007/10/03)
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- New COMT inhibitors for the treatment of depression and impaired cognition
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The present invention relates to compounds of formula I wherein R1 is as defined in the specification and to esters thereof which are hydrolyzable under physiological conditions and to the pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of COMT and, thus, are useful for the treatment of diseases for which COMT inhibition is beneficial. The invention further relates to the treatment, control, or prevention of diseases such as depression, schizophrenia, Parkinson's disease, and to improve cognition.
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Page/Page column 18
(2010/02/12)
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