Pharmaceutical composition for the treatment of parkinson's...

A - Human Necessities – 61 – K

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A61K 31/195 (2006.01) C07C 43/23 (2006.01) C07C 45/56 (2006.01) C07C 45/67 (2006.01) C07C 45/74 (2006.01) C07C 47/565 (2006.01) C07C 47/575 (2006.01) C07C 49/835 (2006.01) C07C 49/84 (2006.01) C07C 59/56 (2006.01) C07C 59/64 (2006.01) C07C 59/68 (2006.01) C07C 205/22 (2006.01) C07C 205/23 (2006.01) C07C 205/26 (2006.01) C07C 205/34 (2006.01) C07C 205/37 (2006.01) C07C 205/43 (2006.01) C07C 205/45 (2006.01) C07C 205/56 (2006.01) C07C 205/57 (2006.01) C07D 207/333 (2006.01) C07D 211/32 (2006.01) C07D 211/58 (

Patent

CA 1289078

ABSTRACT OF THE DISCLOSURE Disclosed and claimed is a new pharmaceutical composition for use in the treatment of Parkinson's disease, which composition comprises levodopa and optionally a peripheric decarboxylase inhibitor such as carbidopa or benzerazide, in admixture with at least one catechol derivatives of formula (I): Image (I) or a salt thereof, wherein R1 and R2 independently represent hydrogen, optionally substituted acyl or aroyl, lower alkylcarbamoyl, X represents an electronegative substituent such as halogen, nitro, cyano, aldehyde, or trifluoromethyl and R3 represents alkyl substituted by lower alkoxy lower alkoxy, carboxy lower alkyl, thio or pyrrole group, or a group selected from: (A) Image or Image wherein R4 represents cyano or acyl and R5 represents cyano, alkoxycarbonyl, carboxyalkenyl, nitro, acyl, hydroxyalkyl, carboxyalkyl or one of the following optionally substituted groups: carbamoyl, aroyl or heteroaroyl, or R4 and R5 form together a five to seven membered, optionally substituted cycloalkanone ring; (B) (CH2)m-COR wherein m is 2-7 and R represents hydroxy, alkyl, - 2 - represents a hydroxyl group, an amino group, an oxo atom, an optionally substituted saturated or partiaily unsaturated lower hydrocarbon group being attached through an imino group or a lower alkylimino group to the rest of the molecule, or a saturated nitrogen containing heterocyclic group being attached through a nitrogen atom in the ring to the rest of the molecule; Z represents a -CO- or =C=N-(Z)p-R4 group; Z represents an oxygen atom or an imino group; the value of p is 0 or 1; and R4 represents a hydrogen atom or an optionally substituted saturated or partially unsaturated lower hydrocarbon group being optionally attached through a carbonyl group to the rest of he molecule.

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