US4190672A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Method and compositions of treating Parkinsonisms with levodopa and 3',4'-dihydroxy-2-methylisopropiophenone
Assignee: Individual
•
Filing: 1978-09-01
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Granted: 1980-02-26
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Expires: 1998-09-01
Abstract
Abstract Improved methods are provided for the treatment of the central nervous system dopamine-deficiency diseases (CNS-DADD's), including Parkinson's disease and other parkinsonisms, which comprises the administration of 3',4'-dihydroxy-2-methyl-isopropiophenone (DHMPP) in an amount effective to inhibit the conversion of levodopa to 3-O-methyldopa (OMD) by catechol-O-methyl transferase (COMT). The present method results in a reduction of the dosage of levodopa otherwise required to symptomatically control the CNS-DADD, providing a concomitant reduction in the untoward side effects of levodopa administration. Also provided are novel pharmaceutical compositions of levodopa and DHMPP.
Inventors
- 👤 Stanley Fahn
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 15:37
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/185; A61K31/19; A61K31/195; A61P; A61P25/00
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
90 words
A method of treating a central nervous system dopamine deficiency disease (CNS-DADD) in a human suffering from said CNS-DADD which comprises: (1) systemically administering to said human an amount on the order of 6-10 grams per day intravenously, or an equivalent dosage by routes other than intravenous administration, of 3',4'-dihydroxy-2-methyl-isopropiophenone (DHMPP), an amount of DHMPP effective to inhibit in vivo the conversion of levodopa to 3-O-methyldopa by catechol-O-methyl transferase (COMT); and (2) concomitantly systemically administering to said human an amount of levodopa effective to control the symptoms of said CNS-DADD.
Claim 2
Independent Claim
90 words
A method of treating a central nervous system dopamine deficiency disease (CNS-DADD) in a human suffering from said CNS-DADD which comprises: (1) systemically administering to said human an amount on the order of 6-10 grams per day intravenously, or an equivalent dosage by routes other than intravenous administration, of 3',4'-dihydroxy-2-methyl-isopropiophenone (DHMPP), an amount of DHMPP effective to inhibit in vivo the conversion of levodopa to 3-O-methyldopa by catechol-O-methyl transferase (COMT); and (2) concomitantly systemically administering to said human an amount of levodopa effective to control the symptoms of said CNS-DADD.
Claim 3
Independent Claim
80 words
A method of reducing the dosage of levodopa required for the effective symptomatic treatment of a central nervous system dopamine deficiency disease (CNS-DADD) in a human suffering from said CNS-DADD which comprises: concomitantly administering to said human an amount on the order of 6-10 grams per day intravenously, or an equivalent dosage by routes other than intravenous administration, of 3',4'-dihydroxy-2-methyl-isopropiophenone (DHMPP), an amount of DHMPP effective to inhibit in vivo the conversion of levodopa to 3-O-methyldopa by catechol-O-methyl transferase (COMT).
Claim 4
Independent Claim
80 words
A method of reducing the dosage of levodopa required for the effective symptomatic treatment of a central nervous system dopamine deficiency disease (CNS-DADD) in a human suffering from said CNS-DADD which comprises: concomitantly administering to said human an amount on the order of 6-10 grams per day intravenously, or an equivalent dosage by routes other than intravenous administration, of 3',4'-dihydroxy-2-methyl-isopropiophenone (DHMPP), an amount of DHMPP effective to inhibit in vivo the conversion of levodopa to 3-O-methyldopa by catechol-O-methyl transferase (COMT).
Claim 5
Dependent Claim
114 words
A solid pharmaceutical composition for the treatment of a central nervous system dopamine deficiency disease (CNS-DADD) in a human suffering from said CNS-DADD in a unit dosage form comprising (1) an amount of 3',4'-dihydroxy-2-methyl-isopropiophenone (DHMPP), which is effective to deliver a dosage on the order of 6-10 grams per patient per day intravenously, or an equivalent dosage by routes other than intravenous administration, an amount of DHMPP which is effective to inhibit in vivo the conversion of levodopa to 3-O-methyldopa by catechol-O-methyl transferase (COMT) when systemically administered to said human and (2) an amount of levodopa effective to control the CNS-DADD symptoms when concomitantly systemically administered to said human with said amount of DHMPP.
Claim 6
Dependent Claim
114 words
A solid pharmaceutical composition for the treatment of a central nervous system dopamine deficiency disease (CNS-DADD) in a human suffering from said CNS-DADD in a unit dosage form comprising (1) an amount of 3',4'-dihydroxy-2-methyl-isopropiophenone (DHMPP), which is effective to deliver a dosage on the order of 6-10 grams per patient per day intravenously, or an equivalent dosage by routes other than intravenous administration, an amount of DHMPP which is effective to inhibit in vivo the conversion of levodopa to 3-O-methyldopa by catechol-O-methyl transferase (COMT) when systemically administered to said human and (2) an amount of levodopa effective to control the CNS-DADD symptoms when concomitantly systemically administered to said human with said amount of DHMPP.
Claim 7
Dependent Claim
10 words
A compressed tablet or gelatin capsule according to claim 3.
Claim 8
Dependent Claim
9 words
A vaginal or rectal suppository according to claim 3.
Claim 9
Dependent Claim
133 words
A liquid pharmaceutical composition for the treatment of a central nervous system dopamine deficiency disease (CNS-DADD) comprising (1) 3',4'-dihydroxy-2-methyl-propiophenone (DHMPP) and (2) levodopa; in a weight ratio which is the fraction whose numerator is: (a) the amount of a unit dosage of DHMPP effective to deliver a dosage on the order of 6-10 grams per patient per day intravenously, or an equivalent dosage by routes other than intravenous administration, an amount of DHMPP which is effective to inhibit in vivo the conversion of levodopa to 3-O-methyldopa by catechol-O-methyl transferase (COMT) when systemically administered to said human; and whose denominator is (b) the amount of a unit dosage of levodopa effective to control the symptoms of said CNS-DADD when concomitantly systemically administered to said human with said amount of a unit dosage of DHMPP.
Claim 10
Dependent Claim
133 words
A liquid pharmaceutical composition for the treatment of a central nervous system dopamine deficiency disease (CNS-DADD) comprising (1) 3',4'-dihydroxy-2-methyl-propiophenone (DHMPP) and (2) levodopa; in a weight ratio which is the fraction whose numerator is: (a) the amount of a unit dosage of DHMPP effective to deliver a dosage on the order of 6-10 grams per patient per day intravenously, or an equivalent dosage by routes other than intravenous administration, an amount of DHMPP which is effective to inhibit in vivo the conversion of levodopa to 3-O-methyldopa by catechol-O-methyl transferase (COMT) when systemically administered to said human; and whose denominator is (b) the amount of a unit dosage of levodopa effective to control the symptoms of said CNS-DADD when concomitantly systemically administered to said human with said amount of a unit dosage of DHMPP.
Claim 11
Dependent Claim
7 words
A sterile solution according to claim 6.
Claim 12
Dependent Claim
6 words
A syrup according to claim 6.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-02-25 | 1983-08-27 | 1984-02-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-02-25 | 1987-08-27 | 1988-02-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-02-25 | 1991-08-27 | 1992-02-26 | $7700.00 | Window Closed / Lapsed |