US4981792A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Immunosuppressant compound
Assignee: Merck and Co Inc
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Filing: 1988-06-29
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Granted: 1991-01-01
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Expires: 2008-06-29
Abstract
Abstract Described is a process for producing a new immunosuppressant, "demethomycin" (L-682,993) a C-31 demethylated analog of L-679,934 under novel fermentation conditions utilizing the microorganism, Actinoplanacete sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in prevent human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
Inventors
- 👤 Edward S. Inamine
- 👤 Byron H. Arison
- 👤 Shieh-Shung T. Chen
- 👤 Linda S. Wicker
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 19:32
CPC Classifications
C; C07; C07D; C07D493/00; C07D493/12; C07D493/18; A; A61; A61P; A61P37/00; A61P37/02; A61P37/06; C07H; C07H19/00; C07H19/01; C12; C12P; C12P17/00; C12P17/18; Y; Y10; Y10S; Y10S435/00; Y10S435/8215; Y10S435/822; Y10S435/827
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
43 words
A process for producing an immunosuppressant, identified as "demethomycin", comprising the step of culturing a strain of Actinoplanacete sp., together with L-679,934 under submerged aerobic fermentation conditions in an aqueous carbohydrate medium containing a nitrogen nutrient for a sufficient time to produce "demethomycin".
Claim 2
Dependent Claim
43 words
A process for producing an immunosuppressant, identified as "demethomycin", comprising the step of culturing a strain of Actinoplanacete sp., together with L-679,934 under submerged aerobic fermentation conditions in an aqueous carbohydrate medium containing a nitrogen nutrient for a sufficient time to produce "demethomycin".
Claim 3
Dependent Claim
12 words
The process of claim 1 wherein said microorganism is ATCC No. 53771.
Claim 4
Dependent Claim
23 words
The process of claim 1 wherein said medium is "Medium B" fermentation medium comprising glucose, Hycase HF, beef extract and corn steep liquor.
Claim 5
Dependent Claim
24 words
The process of claim 1 wherein said medium is "Medium C" fermentation medium comprising mannitol, glycerol, Hycase Sf, beef extract and corn steep liquor.
Claim 6
Dependent Claim
11 words
The broth produced by the process of claim 1, containing "demethomycin".
Claim 7
Dependent Claim
11 words
The immunosuppressant product produced by the above-described process of claim 1.
Claim 8
Dependent Claim
35 words
An immunosuppressant, "demethomycin", which exhibits positive inhibition IC 50 of about 0.6 to 1.2×10 -9 molar) of T-cell activation by the T-cell proliferation assay and a proton nuclear magnetic spectrogram as depicted in FIG. 1.
Claim 9
Dependent Claim
35 words
An immunosuppressant, "demethomycin", which exhibits positive inhibition IC 50 of about 0.6 to 1.2×10 -9 molar) of T-cell activation by the T-cell proliferation assay and a proton nuclear magnetic spectrogram as depicted in FIG. 1.
Claim 10
Dependent Claim
12 words
An immunosuppressant, "demethomycin", having a molecular structure as depicted in FIG. 3.
Claim 11
Dependent Claim
12 words
An immunosuppressant, "demethomycin", having a molecular structure as depicted in FIG. 3.
Claim 12
Dependent Claim
21 words
A pharmaceutical composition containing a therapeutically effective amount of "demethomycin" in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 13
Dependent Claim
21 words
A pharmaceutical composition containing a therapeutically effective amount of "demethomycin" in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 14
Independent Claim
32 words
A method of use for treating a human host to prevent transplantation rejection, or for treating autoimmune disease or infectious disease comprising administering to said host a therapeutically effective amount of "demethomycin".
Claim 15
Independent Claim
32 words
A method of use for treating a human host to prevent transplantation rejection, or for treating autoimmune disease or infectious disease comprising administering to said host a therapeutically effective amount of "demethomycin".
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) | 1993-12-31 | 1994-07-02 | 1995-01-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-12-31 | 1998-07-02 | 1999-01-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-12-31 | 2002-07-02 | 2003-01-01 | $7700.00 | Window Closed / Lapsed |