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EP0388153A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Immunosuppressant agent

Assignee: Merck and Co Inc
•
Filing: 1990-03-13
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Granted: —
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Expires: 2010-03-13
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Abstract

Abstract Described is a new immunosuppressant, L-687,819, a C-31 demethylated derivative of L-683,795 (FK-523), produced under fermentation conditions utilizing the new mutant microorganism, Streptomyces hygroscopicus subsp. ascomyceticus (Merck Culture Collection MA 6646) ATCC No. 53855, being a blocked mutant of Streptomyces hygroscopicus subsp. ascomyceticus (MA 6475) ATCC No. 14891. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Inventors

  • 👤 Louis Kaplan
  • 👤 Robert P. Borris
  • 👤 Kevin M. Byrne
  • 👤 Linda S. Wicker
  • 👤 Deborah L. Zink

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-01 16:03
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/01; A; A61; A61P; A61P37/00; A61P37/02; A61P37/06; C12; C12P; C12P19/00; C12P19/44; C12P19/445; Y; Y10; Y10S; Y10S435/00; Y10S435/8215; Y10S435/822; Y10S435/886; Y10S435/898

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 52 words
An immunosuppressant, designated as L-687,819, which exhibits: positive inhibition of T-cell activation by the T-cell proliferation assay, a proton nuclear magnetic resonance spectrum as depicted in Figure 1, a carbon-13 nuclear magnetic resonance spectrum as depicted in Figure 2, and a molecular formula of C₄₁H₆₅NO₁₂ as determined by electron impact mass spectrometry.
Claim 2
Dependent Claim 52 words
An immunosuppressant, designated as L-687,819, which exhibits: positive inhibition of T-cell activation by the T-cell proliferation assay, a proton nuclear magnetic resonance spectrum as depicted in Figure 1, a carbon-13 nuclear magnetic resonance spectrum as depicted in Figure 2, and a molecular formula of C₄₁H₆₅NO₁₂ as determined by electron impact mass spectrometry.
Claim 3
Dependent Claim 13 words
An immunosuppressant, L-687,819, which has a molecular structure as depicted in Figure 3.
Claim 4
Dependent Claim 13 words
An immunosuppressant, L-687,819, which has a molecular structure as depicted in Figure 3.
Claim 5
Dependent Claim 21 words
A pharmaceutical composition containing a therapeutically effective amount of L-687,819 in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 6
Dependent Claim 21 words
A pharmaceutical composition containing a therapeutically effective amount of L-687,819 in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 7
Dependent Claim 28 words
The use of L-687,819 for the preparation of a composition useful for treating a human host to prevent transplantation rejection, or for treating autoimmune disease or infectious disease.
Claim 8
Dependent Claim 28 words
The use of L-687,819 for the preparation of a composition useful for treating a human host to prevent transplantation rejection, or for treating autoimmune disease or infectious disease.

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