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EP0349061A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Immunosuppressant agent

Assignee: Merck and Co Inc
•
Filing: 1989-06-22
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Granted: —
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Expires: 2009-06-22
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Abstract

Abstract Described is a process for producing a new immunosuppressant, "demethimmunomycin" (L-683,742) a C-31 demethylated analog of L-683,590 under novel fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosup­pressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Inventors

  • 👤 Edward S. Inamine
  • 👤 Linda S. Wicker
  • 👤 Shieh-Shung T. Chen
  • 👤 Byron H. Arison

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-01 23:58
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/01; A; A61; A61P; A61P37/00; A61P37/02; A61P37/06; C12; C12N; C12N1/00; C12N1/20; C12N1/205; C12P; C12P17/00; C12P17/18; C12P17/188; C12R; C12R2001/00; C12R2001/01

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 44 words
A process for producing an immunosup­pressant, identified as "demethimmunomycin", comprising the step of culturing a strain of Actinoplanacete sp. , together with L-683,590 under submerged aerobic fermentation conditions in an aqueous carbohydrate medium containing a nitrogen nutrient for a sufficient time to produce "demethimmunomycin".
Claim 2
Dependent Claim 44 words
A process for producing an immunosup­pressant, identified as "demethimmunomycin", comprising the step of culturing a strain of Actinoplanacete sp. , together with L-683,590 under submerged aerobic fermentation conditions in an aqueous carbohydrate medium containing a nitrogen nutrient for a sufficient time to produce "demethimmunomycin".
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 "demethimmunomycin".
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, "demethimmuno­mycin", which exhibits positive inhibition (IC₅₀ of about 1.6 to 1.9 x 10⁻⁹ molar) of T-cell activation by the T-cell proliferation assay and a proton nuclear magnetic spectrogram as depicted in Figure 1.
Claim 9
Dependent Claim 35 words
An immunosuppressant, "demethimmuno­mycin", which exhibits positive inhibition (IC₅₀ of about 1.6 to 1.9 x 10⁻⁹ molar) of T-cell activation by the T-cell proliferation assay and a proton nuclear magnetic spectrogram as depicted in Figure 1.
Claim 10
Dependent Claim 12 words
An immunosuppressant, "demethimmuno­mycin", having a molecular structure as depicted in Figure 3.
Claim 11
Dependent Claim 12 words
An immunosuppressant, "demethimmuno­mycin", having a molecular structure as depicted in Figure 3.
Claim 12
Dependent Claim 21 words
A pharmaceutical composition containing a therapeutically effective amount of "demethimmuno­mycin" 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 "demethimmuno­mycin" in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 14
Dependent Claim 28 words
The use of "demethimmunomycin" for the preparation of a medicament useful for treating a human host to prevent transplantation rejection, or for treating autoimmune disease or infectious disease.
Claim 15
Dependent Claim 28 words
The use of "demethimmunomycin" for the preparation of a medicament useful for treating a human host to prevent transplantation rejection, or for treating autoimmune disease or infectious disease.

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