US4487780A
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US
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Method of treatment of rheumatoid arthritis
Assignee: Individual
•
Filing: 1982-02-05
•
Granted: 1984-12-11
•
Expires: 2002-02-05
Abstract
Abstract Rheumatoid arthritis is treated with substituted cysteine compounds having a lower toxicity-to-effectiveness ratio than penicillamine. Such compounds are specific alpha-substituted cysteines, beta-monosubstituted cysteines, beta-di-substituted cysteines other than penicillamine, N-acetyl penicillamine and the N-acetyl derivatives of the alpha and beta-substituted compounds mentioned above. Any of the compounds may be used synergistically in combination with suitable copper compounds or with suitable gold compounds in the treatment of arthritis. The same compounds are effective in the treatment of cystinuria and heavy metal poisoning. The same compounds as well as penicillamine are effective in combination with copper in the treatment of heavy metal poisoning.
Inventors
- 👤 Israel H. Scheinberg
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 13:17
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/28; A61K31/30
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
177 words
Method of treatment of rheumatoid arthritis comprising the step of administering to a patient with a rheumatoid arthritis treatment effective amount of a sulfhydryl compound selected from the group consisting of beta-monosubstituted cysteine, the substituent being selected from a first subgroup consisting of chloro, methyl, ethyl, hydroxymethyl and hydroxyethyl; beta-disubstituted cysteine, the substituents being selected from a second subgroup consisting of the pairs, ______________________________________
chloro, chloro,
methyl, chloro,
ethyl, chloro,
methyl, ethyl,
ethyl, ethyl,
hydroxymethyl, hydroxymethyl,
hydroxyethyl, hydroxylethyl,
hydroxymethyl, hydroxyethyl,
methyl, hydroxymethyl,
methyl, hydroxyethyl,
ethyl, hydroxymethyl,
ethyl, hydroxyethyl,
chloro, hydroxymethyl, and
chloro, hydroxyethyl;
______________________________________ alpha-substituted cysteine, the substituent being selected from a third subgroup identical with said first subgroup; beta-monosubstituted, alpha-substituted cysteine, the substituents in both positions being selected from a fourth subgroup identical with the members of said first subgroup; alpha-substituted, beta-disubstituted cysteine, the substituents being selected from a fifth subgroup consisting of the combinations of the members of said first subgroup with the members of said second subgroup; an N-acetyl derivative of a member of said group of sulfhydryl compounds; and combinations of said compounds.
Claim 2
Dependent Claim
177 words
Method of treatment of rheumatoid arthritis comprising the step of administering to a patient with a rheumatoid arthritis treatment effective amount of a sulfhydryl compound selected from the group consisting of beta-monosubstituted cysteine, the substituent being selected from a first subgroup consisting of chloro, methyl, ethyl, hydroxymethyl and hydroxyethyl; beta-disubstituted cysteine, the substituents being selected from a second subgroup consisting of the pairs, ______________________________________
chloro, chloro,
methyl, chloro,
ethyl, chloro,
methyl, ethyl,
ethyl, ethyl,
hydroxymethyl, hydroxymethyl,
hydroxyethyl, hydroxylethyl,
hydroxymethyl, hydroxyethyl,
methyl, hydroxymethyl,
methyl, hydroxyethyl,
ethyl, hydroxymethyl,
ethyl, hydroxyethyl,
chloro, hydroxymethyl, and
chloro, hydroxyethyl;
______________________________________ alpha-substituted cysteine, the substituent being selected from a third subgroup identical with said first subgroup; beta-monosubstituted, alpha-substituted cysteine, the substituents in both positions being selected from a fourth subgroup identical with the members of said first subgroup; alpha-substituted, beta-disubstituted cysteine, the substituents being selected from a fifth subgroup consisting of the combinations of the members of said first subgroup with the members of said second subgroup; an N-acetyl derivative of a member of said group of sulfhydryl compounds; and combinations of said compounds.
Claim 3
Dependent Claim
18 words
A method of treatment of rheumatoid arthritis, as defined in claim 1, wherein said sulfhydryl compound is β-methylcysteine.
Claim 4
Dependent Claim
18 words
A method of treatment of rheumatoid arthritis, as defined in claim 1, wherein said sulfhydryl compound is α-methylcysteine.
Claim 5
Dependent Claim
18 words
A method of treatment of rheumatoid arthritis, as defined in claim 1, wherein said sulfhydryl compound is α,β-dimethylcysteine.
Claim 6
Dependent Claim
22 words
A method of treatment of rheumatoid arthritis, as defined in claim 1, wherein said sulfhydryl compound is a metal complex with copper.
Claim 7
Independent Claim
25 words
A method of treatment of rheumatoid arthritis, as claimed in any of claims 1 to 4 and 5, wherein said sulfhydryl compound is administered orally.
Claim 8
Independent Claim
25 words
A method of treatment of rheumatoid arthritis, as claimed in any of claims 1 to 4 and 5, wherein said sulfhydryl compound is administered parenterally.
Claim 9
Dependent Claim
21 words
A method of treatment of rheumatoid arthritis, as claimed in claim 1, wherein said sulfhydryl compound is cysteine complexed with copper.
Claim 10
Dependent Claim
21 words
A method of treatment of rheumatoid arthritis, as defined in claim 1, wherein said sulfhydryl compound is β-methylcysteine complexed with copper.
Claim 11
Dependent Claim
36 words
A method of treatment of rheumatoid arthritis, as claimed in claim 5, wherein the mol ratio of said sulfhydryl to the copper in said source of copper lies in the range from about 1 to 5.
Claim 12
Independent Claim
48 words
A method of treatment of rheumatoid arthritis comprising the step of administering to a patient with rheumatoid arthritis, a rheumatoid arthritis treatment effective amount of a complex of a sulfhydryl of the group of sulfhydryls consisting of cysteine, α-methylcysteine and β-methylcysteine, complexed with copper said complex being water-soluble.
Claim 13
Independent Claim
48 words
A method of treatment of rheumatoid arthritis comprising the step of administering to a patient with rheumatoid arthritis, a rheumatoid arthritis treatment effective amount of a complex of a sulfhydryl of the group of sulfhydryls consisting of cysteine, α-methylcysteine and β-methylcysteine, complexed with copper said complex being water-soluble.
Claim 14
Dependent Claim
176 words
A composition effective in the treatment of rheumatoid arthritis, comprising a water-soluble complex of at least one sulfhydryl compound selected from the groups consisting of cysteine, beta-monosubstituted cysteine, the substituent being selected from a first subgroup consisting of chloro, methyl, ethyl, hydroxymethyl and hydroxyethyl; beta-disubstituted cysteine, the substituents being selected from a second subgroup consisting of the pairs, ______________________________________
chloro, chloro,
methyl, chloro,
ethyl, chloro,
methyl, ethyl,
ethyl, ethyl,
hydroxymethyl, hydroxymethyl,
hydroxyethyl, hydroxylethyl,
hydroxymethyl, hydroxyethyl,
methyl, hydroxymethyl,
methyl, hydroxyethyl,
ethyl, hydroxymethyl,
ethyl, hydroxyethyl,
chloro, hydroxymethyl, and
chloro, hydroxyethyl;
______________________________________ alpha-substituted cysteine, the substituent being selected from a third subgroup identical with said first subgroup; beta-monosubstituted, alpha-substituted cysteine, the substituents in both positions being selected from a fourth subgroup identical with the members of said first subgroup; alpha-substituted, beta-disubstituted cysteine, the substituents being selected from a fifth subgroup consisting of the combinations of the members of said first subgroup with the members of said second subgroup; and an N-acetyl derivative of a member of said group of sulfhydryl compounds; and combinations of said compounds; complexed with copper.
Claim 15
Dependent Claim
176 words
A composition effective in the treatment of rheumatoid arthritis, comprising a water-soluble complex of at least one sulfhydryl compound selected from the groups consisting of cysteine, beta-monosubstituted cysteine, the substituent being selected from a first subgroup consisting of chloro, methyl, ethyl, hydroxymethyl and hydroxyethyl; beta-disubstituted cysteine, the substituents being selected from a second subgroup consisting of the pairs, ______________________________________
chloro, chloro,
methyl, chloro,
ethyl, chloro,
methyl, ethyl,
ethyl, ethyl,
hydroxymethyl, hydroxymethyl,
hydroxyethyl, hydroxylethyl,
hydroxymethyl, hydroxyethyl,
methyl, hydroxymethyl,
methyl, hydroxyethyl,
ethyl, hydroxymethyl,
ethyl, hydroxyethyl,
chloro, hydroxymethyl, and
chloro, hydroxyethyl;
______________________________________ alpha-substituted cysteine, the substituent being selected from a third subgroup identical with said first subgroup; beta-monosubstituted, alpha-substituted cysteine, the substituents in both positions being selected from a fourth subgroup identical with the members of said first subgroup; alpha-substituted, beta-disubstituted cysteine, the substituents being selected from a fifth subgroup consisting of the combinations of the members of said first subgroup with the members of said second subgroup; and an N-acetyl derivative of a member of said group of sulfhydryl compounds; and combinations of said compounds; complexed with copper.
Claim 16
Dependent Claim
25 words
A composition as claimed in claim 12 wherein said complex is the reaction product of said compound of said group of said compound of copper.
Claim 17
Dependent Claim
27 words
A composition as claimed in claim 13 wherein said reaction product is a member of the group consisting of copper-cysteine, copper α-methylcysteine, copper β-methylcysteine and copper α,β-dimethylcysteine.
Claim 18
Dependent Claim
196 words
A composition effective in the treatment of rheumatoid arthritis, comprising a water-soluble complex of at least one sulfhydryl compound selected from the groups consisting of cysteine, beta-monosubstituted cysteine, the substituent being selected from a first subgroup consisting of chloro, methyl, ethyl, hydroxymethyl and hydroxyethyl; beta-disubstituted cysteine, the substituents being selected from a second subgroup consisting of the pairs, ______________________________________
chloro, chloro,
methyl, chloro,
ethyl, chloro,
methyl, ethyl,
ethyl, ethyl,
hydroxymethyl, hydroxymethyl,
hydroxyethyl, hydroxylethyl,
hydroxymethyl, hydroxyethyl,
methyl, hydroxymethyl,
methyl, hydroxyethyl,
ethyl, hydroxymethyl,
ethyl, hydroxyethyl,
chloro, hydroxymethyl, and
chloro, hydroxyethyl;
______________________________________ alpha-substituted cysteine, the substituent being selected from a third subgroup identical with said first subgroup; beta-monosubstituted, alpha-substituted cysteine, the substituents in both positions being selected from a fourth subgroup identical with the members of said first subgroup; alpha-substituted, beta-disubstituted cysteine, the substituents being selected from a fifth subgroup consisting of the combinations of the members of said first subgroup with the members of said second subgroup; and an N-acetyl derivative of a member of said group of sulfhydryl compounds; and combinations of said compounds; complexed with copper, wherein the mole ratio of the sulfhydryl compound to the copper is in the range from about 1 to 5.
Claim 19
Dependent Claim
196 words
A composition effective in the treatment of rheumatoid arthritis, comprising a water-soluble complex of at least one sulfhydryl compound selected from the groups consisting of cysteine, beta-monosubstituted cysteine, the substituent being selected from a first subgroup consisting of chloro, methyl, ethyl, hydroxymethyl and hydroxyethyl; beta-disubstituted cysteine, the substituents being selected from a second subgroup consisting of the pairs, ______________________________________
chloro, chloro,
methyl, chloro,
ethyl, chloro,
methyl, ethyl,
ethyl, ethyl,
hydroxymethyl, hydroxymethyl,
hydroxyethyl, hydroxylethyl,
hydroxymethyl, hydroxyethyl,
methyl, hydroxymethyl,
methyl, hydroxyethyl,
ethyl, hydroxymethyl,
ethyl, hydroxyethyl,
chloro, hydroxymethyl, and
chloro, hydroxyethyl;
______________________________________ alpha-substituted cysteine, the substituent being selected from a third subgroup identical with said first subgroup; beta-monosubstituted, alpha-substituted cysteine, the substituents in both positions being selected from a fourth subgroup identical with the members of said first subgroup; alpha-substituted, beta-disubstituted cysteine, the substituents being selected from a fifth subgroup consisting of the combinations of the members of said first subgroup with the members of said second subgroup; and an N-acetyl derivative of a member of said group of sulfhydryl compounds; and combinations of said compounds; complexed with copper, wherein the mole ratio of the sulfhydryl compound to the copper is in the range from about 1 to 5.
Claim 20
Dependent Claim
36 words
A composition effective in the treatment of rheumatoid arthritis, comprising a water-soluble complex of at least one sulfhydryl compound selected from the group consisting of copper-cysteine, copper alpha-methyl cysteine, copper beta-methyl cysteine and copper alpha-beta-dimethyl cysteine.
Claim 21
Dependent Claim
36 words
A composition effective in the treatment of rheumatoid arthritis, comprising a water-soluble complex of at least one sulfhydryl compound selected from the group consisting of copper-cysteine, copper alpha-methyl cysteine, copper beta-methyl cysteine and copper alpha-beta-dimethyl cysteine.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-12-11 | 1988-06-11 | 1988-12-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-12-11 | 1992-06-11 | 1992-12-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-12-11 | 1996-06-11 | 1996-12-11 | $7700.00 | Window Closed / Lapsed |