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Claims for Patent: 5,135,950

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Claims for Patent: 5,135,950

Title: Stable polymorphic form of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide and the process for its preparation
Abstract:Stable and crystallographically essentially pure polymorphic form A of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitro-phenyl)acrylamide may be prepared by crystallizing crude synthesis product from lower aliphatic carboxylic acid such as formic or acetic acid with a catalytic amount of hydrochloric or hydrobromic acid added. The product is a potent inhibitor of catechol-O-methyl-transferase enzyme (COMT).
Inventor(s): Pippuri; Aino K. (Espoo, FI), Honkanen; Erkki J. (Vantaa, FI), Haarala; Jorma V. (Helsinki, FI)
Assignee: Orion-yhtyma Oy (Espoo, FI)
Application Number:07/606,717
Patent Claims: 1. The crystallographically essentially pure polymorphic form A of (E)-N,N-diethyl-2-cyano-3-(3,4dihydroxy-5-nitrophenyl)acrylamide having the infrared spectrum in potassium bromide having the following absorption bands:

2. A process for preparing crystallographically essentially pure polymorphic form A of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl) acrylamide having the infrared spectrum in potassium bromide having the following absorption bands:

which comprises crystallization of the crude N,N-diethyl-2-cyano-3-(3,4-dihydroxy -5-nitrophenyl acrylamide from lower aliphatic carboxylic acid containing a catalytic amount of hydrochloric or hydrobromic acid.

3. The process as claimed in claim 2, wherein said lower aliphatic carboxylic acid is acetic acid.

4. The process as claimed in claim 2, wherein said lower aliphatic carboxylic acid is formic acid.

5. A pharmaceutical composition for inhibiting catechol-O-methyl-transferase, said composition comprising a catechol-O-methyl-transferase inhibiting amount of the crystallographically essentially pure polymorphic form A of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide of claim 1 and a pharmaceutically acceptable carrier.

6. A method for inhibiting catechol-O-methyl -transferase in a patient, said method comprising administering a catechol-O-methyl-transferase inhibiting amount of the crystallographically essentially pure polymorphic form A of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide of claim 1, to a patient in need of such treatment.

7. A method for the treatment of Parkinson's Disease, said method comprising administering a catechol-O-methyl-transferase inhibiting amount of the crystallographically essentially pure polymorphic form A of (E)-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide of claim 1; and a sufficient amount of levodopa to treat Parkinson's disease, to a patient in need of such treatment.

8. The method as claimed in claim 7, further comprising administering a sufficient amount of a peripheral decarboxylase inhibitor to inhibit early dopamine formation.

9. The method as claimed in claim 8, wherein said peripheral decarboxylase inhibitor is carbidopa.

10. The method as claimed in claim 8, wherein said peripheral decarboxylase inhibitor is benserazide.
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