Patent US4558057A successfully refreshed from Google Patents.
US4558057A
Expired / Lapsed
US
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Purified antineoplaston fractions and methods of treating neoplastic disease
Assignee: Individual
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Filing: 1984-08-20
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Granted: 1985-12-10
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Expires: 2004-08-20
Abstract
Abstract Highly purified fractions from human urine exhibiting antineoplastic activity and processes for their preparation are described. The fractions comprise biologically active, small sized, low molecular weight peptides which exert cytostatic and cytotoxic activity toward neoplastic cell cultures and human neoplastic diseases. The fractions have been termed antineoplaston fractions. An antineoplastic active peptide common to each of the various antineoplaston fractions has been isolated and identified as 3-[N-phenylacetylaminopiperidine]-2, 6-dion. A synthetic mechanism for the preparation of 3-[N-phenylacetylaminopiperdine]-2, 6-dion is also disclosed, involving a combination reaction between L-glutamine and phenylacetyl chloride. Also disclosed are the hydrolysis degradation products of 3-[N-phenylacetylaminopiperidine]-2, 6-dion which also exhibit antineoplastic activity when administered according to the general teachings presented in this disclosure.
Inventors
- 👤 Stanislaw R. Burzynski
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 21:55
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/46; C07K14/47; A; A61; A61K; A61K31/00; A61K31/185; A61K31/19; A61K31/195; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; C07K4/00; C07K4/12; A61K38/00
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
13 words
A composition of matter consisting essentially of: ##STR3## or pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
13 words
A composition of matter consisting essentially of: ##STR3## or pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
16 words
A composition of matter extracted from urine consisting essentially of 3-[N-phenylacetylaminopiperidine]-2,6-dion or pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim
16 words
A composition of matter extracted from urine consisting essentially of 3-[N-phenylacetylaminopiperidine]-2,6-dion or pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
24 words
A pharmaceutical composition comprising a carcinostaticly effective amount of the composition of matter in accordance with claim 1 together with a pharmaceutically acceptable carrier.
Claim 6
Dependent Claim
66 words
A process for synthesizing the compound 3-[N-phenylacetylaminopiperidine]-2,6-dion comprising the steps of: providing a quantity of L-glutamine; providing a quantity of phenylacetyl halide; mixing together the L-glutamine and phenyl acetyl halide in a weakly alkaline aqueous solution to provide an aqueous reaction mixture; reacting said reaction mixture for a period of time to form the reaction product 3-[N-phenylacetylaminopiperidine]-2,6-dion; and recovering from the reaction mixture the product 3-[N-phenylacetylaminopiperidine]-2,6-dion.
Claim 7
Dependent Claim
66 words
A process for synthesizing the compound 3-[N-phenylacetylaminopiperidine]-2,6-dion comprising the steps of: providing a quantity of L-glutamine; providing a quantity of phenylacetyl halide; mixing together the L-glutamine and phenyl acetyl halide in a weakly alkaline aqueous solution to provide an aqueous reaction mixture; reacting said reaction mixture for a period of time to form the reaction product 3-[N-phenylacetylaminopiperidine]-2,6-dion; and recovering from the reaction mixture the product 3-[N-phenylacetylaminopiperidine]-2,6-dion.
Claim 8
Dependent Claim
13 words
The process according to claim 4 wherein the reaction mixture contains sodium bicarbonate.
Claim 9
Dependent Claim
15 words
The process according to claim 4 wherein the phenyl acetyl halide is phenyl acetyl chloride.
Claim 10
Dependent Claim
54 words
The process according to claim 5 wherein the product 3-[N-phenylacetylaminopiperidine]-2, 6-dion is recovered from the reaction mixture by: acidifying the reaction mixture; providing an immiscible organic solvent in contact with the aqueous reaction mixture; extracting into the organic solvent the excess reagents and by-products; and recovering the compound 3-[N-phenylacetylaminopiperidine]-2,6-dion from the aqueous reaction mixture.
Claim 11
Independent Claim
32 words
A method of inhibiting the growth of neoplastic cells from a person having neoplastic disease comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 12
Independent Claim
32 words
A method of inhibiting the growth of neoplastic cells from a person having neoplastic disease comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 13
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the breast comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 14
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the breast comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 15
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the bladder comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 16
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the bladder comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 17
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the liver comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 18
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the liver comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 19
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the lung comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 20
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the lung comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 21
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the kidney comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 22
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the kidney comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 23
Independent Claim
35 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the primary tract comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 24
Independent Claim
35 words
A method of inhibiting the growth of neoplastic cells from a person having neoplasia of the primary tract comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 25
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having primary malignant brain tumor comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
Claim 26
Independent Claim
34 words
A method of inhibiting the growth of neoplastic cells from a person having primary malignant brain tumor comprising the administration to said person a therapeutically effective amount of 3-[N-phenylacetylaminopiperidine]-2,6-dion dispersed in a pharmaceutical carrier.
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) | 1988-12-09 | 1989-06-10 | 1989-12-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-12-09 | 1993-06-10 | 1993-12-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-12-09 | 1997-06-10 | 1997-12-10 | $7700.00 | Window Closed / Lapsed |