Patent US1977819A successfully refreshed from Google Patents.
US3929992A
Expired / Lapsed
US
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Rapamycin and process of preparation
Assignee: Wyeth Canada Inc
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Filing: 1974-04-12
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Granted: 1975-12-30
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Expires: 1994-04-12
Abstract
Abstract Antibiotic rapamycin is producible by culturing Streptomyces hygroscopicus NRRL 5491 in an aqueous nutrient medium. Rapamycin has antifungal properties. Methods for its preparation and use are disclosed.
Inventors
- 👤 Surendra N Sehgal
- 👤 Teodora M Blazekovic
- 👤 Claude Vezina
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 19:54
CPC Classifications
C; C12; C12P; C12P17/00; C12P17/18; C12P17/188; Y; Y10; Y10S; Y10S435/00; Y10S435/8215; Y10S435/822; Y10S435/886; Y10S435/898
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
158 words
RAPAMYCIN, AN ANTIBIOTIC WHICH A. IS A LOLOURLESS, CRYSTALLINE COMPOUND WITH A MELTING POINT OF 183* TO 185*C, AFTER RECRYSTALLIZATION FROM ETHER; B. IS SOLUBLE IN ETHER, CHLOROFORM, ACETONE, METHANOL AND DIMETHYLFORMAMIDE, VERY SPARINGLY SOLUBLE IN HEXANE AND PETROLEUM ETHER AND SUBSTANTIALLY INSOLUBLE IN WATER; C. SHOWS A UNIFORM SPOT ON THIN LAYER PLATES OF SILICA GEL; D. HAS A CHARACTERISTIC ELEMENTAL ANALYSIS OF ABOUT C. 66.84%, H, 8.84%; N, 1.37%, E. EXHIBITS THE FOLLOWING CHARACTERISTIC ABSORPTION MAXIMA IN ITS ULTRAVIOLET ABSORPTION SPECTRUM (95% ETHANOL) 267 NM (E1CM1% 417), 277 NM (E1CM1% 541) AND 288 NM (E1CM1% 416); F. HAS A CHARACTERISTIC INFRARED ABSORPTION SPECTRUM SHOWN IN ACCOMPANYING FIG. 1; G. HAS A CHARACTERISTIC NUCLEAR MAGNETIC RESONANCE SPECTRUM AS SHOWN IN ACCOMPANYING FIG. 2; H. HAS A MINIMUM INHIBITORY CONCENTRATION OF 0.002 TO 0.1 UG/ML AGAINST CANDIDA ALBICANS; AND I. EXHIBITS A LD50 (I.P., MICE) OF 597.3 $ 28.1 MG/KG AND A LD50 (P.O., MICE) OF >2,500 MG/KG.
Claim 2
Dependent Claim
158 words
RAPAMYCIN, AN ANTIBIOTIC WHICH A. IS A LOLOURLESS, CRYSTALLINE COMPOUND WITH A MELTING POINT OF 183* TO 185*C, AFTER RECRYSTALLIZATION FROM ETHER; B. IS SOLUBLE IN ETHER, CHLOROFORM, ACETONE, METHANOL AND DIMETHYLFORMAMIDE, VERY SPARINGLY SOLUBLE IN HEXANE AND PETROLEUM ETHER AND SUBSTANTIALLY INSOLUBLE IN WATER; C. SHOWS A UNIFORM SPOT ON THIN LAYER PLATES OF SILICA GEL; D. HAS A CHARACTERISTIC ELEMENTAL ANALYSIS OF ABOUT C. 66.84%, H, 8.84%; N, 1.37%, E. EXHIBITS THE FOLLOWING CHARACTERISTIC ABSORPTION MAXIMA IN ITS ULTRAVIOLET ABSORPTION SPECTRUM (95% ETHANOL) 267 NM (E1CM1% 417), 277 NM (E1CM1% 541) AND 288 NM (E1CM1% 416); F. HAS A CHARACTERISTIC INFRARED ABSORPTION SPECTRUM SHOWN IN ACCOMPANYING FIG. 1; G. HAS A CHARACTERISTIC NUCLEAR MAGNETIC RESONANCE SPECTRUM AS SHOWN IN ACCOMPANYING FIG. 2; H. HAS A MINIMUM INHIBITORY CONCENTRATION OF 0.002 TO 0.1 UG/ML AGAINST CANDIDA ALBICANS; AND I. EXHIBITS A LD50 (I.P., MICE) OF 597.3 $ 28.1 MG/KG AND A LD50 (P.O., MICE) OF >2,500 MG/KG.
Claim 3
Dependent Claim
55 words
A process for the production of rapamycin which comprises cultivating Streptomyces hygroscopicus NRRL 5491 in an aqueous nutrient medium containing a source of assimilable carbon and nitrogen and mineral salts under aerobic conditions until substantial antifungal activity is present in the fermentation mixture by the production of rapamycin, and isolating rapamycin from said fermentation mixture.
Claim 4
Dependent Claim
55 words
A process for the production of rapamycin which comprises cultivating Streptomyces hygroscopicus NRRL 5491 in an aqueous nutrient medium containing a source of assimilable carbon and nitrogen and mineral salts under aerobic conditions until substantial antifungal activity is present in the fermentation mixture by the production of rapamycin, and isolating rapamycin from said fermentation mixture.
Claim 5
Dependent Claim
32 words
A process as claimed in claim 2 in which the cultivation is carried out at a temperature ranging from 20* to 35*C and at an initial pH of between 6.5 and 7.5.
Claim 6
Dependent Claim
34 words
A process according to claim 2 in which the isolation comprises filtering the fermentation mixture, extracting the filter cake with methanol or ethanol to produce an extract, and separating the rapamycin from the extract.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1978-12-29 | 1979-06-30 | 1979-12-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1982-12-29 | 1983-06-30 | 1983-12-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1986-12-29 | 1987-06-30 | 1987-12-30 | $7700.00 | Window Closed / Lapsed |