Nova Patents
EP0378317A2

Microbial transformation product of L-679,934.

Abstract

Described is a new immunosuppressant, L-683,519, a monodemethylated rearranged derivative of L-679,934, produced under fermentation conditions utilizing the microorganism, unidentified Actinomycete (Merck Culture Collection MA 6474) ATCC No. 53828. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

EP0378317A2, drawing sheet 1
Sheet 1 of 3

Term

Term ended

Projected expiry passed 5 January 2010, 16.7 years ago.

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7 claims: 5 independent, 2 dependent

  1. 1
    An immunosuppressant, designated as L-683,519, which exhibits:positive inhibition of T-cell activation by the T-cell proliferation assay, a proton nuclear magnetic spectrogram as depicted in Figure 1, and a molecular weight of 789 as determined by FAB mass spectroscopy.
  2. 2
    An immunosuppressant, L-683,519, which has a molecular structure as depicted in Figure 1.
  3. 3
    A pharmaceutical composition containing a therapeutically effective amount of L-683,519 in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
  4. 4
    A process for producing an immunosuppressant, identified as L-683,519, comprising the step of culturing a strain of Actinomycete , ATCC No. 53828 under submerged aerobic fermentation conditions in an aqueous carbohydrate medium containing a nitrogen nutrient at a pH below 8.0 for a sufficient time to produce L-683,519.
  5. 5
    The broth produced by the process of Claim 4, containing L-683,519, said broth exhibiting a positive inhibition of T-cell activation by the T-cell proliferation assay.
  6. 6
    The immunosuppressant product produced by the above-described process of Claim 4.
  7. 7
    The use of L-683,519 for the preparation of a medicament useful for treating a human host to prevent transplantation rejection, or for treating autoimmune disease or infectious disease.
Independent claims7