Patent US5149701A successfully refreshed from Google Patents.
US5149701A
Expired / Lapsed
US
⏱️ 0.0 years remaining
C-31 methylated FR-900520 cyclic hemiketal immunosuppressant agents
Assignee: Merck and Co Inc
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Filing: 1991-08-01
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Granted: 1992-09-22
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Expires: 2011-08-01
Abstract
Abstract Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated devivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
Inventors
- 👤 Ali Shafiee
- 👤 Louis Kaplan
- 👤 Shieh-Shung T. Chen
- 👤 Byron H. Arison
- 👤 Lawrence F. Colwell, Jr.
- 👤 Francis Dumont
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 13:12
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/22
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
27 words
An immunosuppressant, Compound II, which exhibits positive inhibition of T-cell activation by the T-cell proliferation assay and a proton nuclear magnetic spectrogram as depicted in FIG. 2.
Claim 2
Dependent Claim
27 words
An immunosuppressant, Compound II, which exhibits positive inhibition of T-cell activation by the T-cell proliferation assay and a proton nuclear magnetic spectrogram as depicted in FIG. 2.
Claim 3
Dependent Claim
14 words
The immunosuppressant of claim 1, having a molecular structure as depicted in FIG. 2.
Claim 4
Dependent Claim
22 words
A pharmaceutical composition containing a therapeutically effective amount of Compound II in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 5
Dependent Claim
22 words
A pharmaceutical composition containing a therapeutically effective amount of Compound II in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 6
Independent Claim
30 words
A method of use for treating a human host to prevent transplantation rejection, or for treating autoimmune disease comprising administering to said host a therapeutically effective amount of Compound II.
Claim 7
Independent Claim
30 words
A method of use for treating a human host to prevent transplantation rejection, or for treating autoimmune disease comprising administering to said host a therapeutically effective amount of Compound II.
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) | 1995-09-22 | 1996-03-23 | 1996-09-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-09-22 | 2000-03-23 | 2000-09-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-09-22 | 2004-03-23 | 2004-09-22 | $7700.00 | Window Closed / Lapsed |