EP0358508A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Novel immunosuppressant compound
Assignee: Merck and Co Inc
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Filing: 1989-09-07
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Granted: —
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Expires: 2009-09-07
Abstract
Abstract Described is a new immunosuppressant, "Tsukubamycin A" (I), being the C-9 dihydro analog of FK-506, and a new process for preparing the immunosuppressant, "Tsukubamycin B" (II), being the C-21 propyl analog of FK-506, produced as by-products under fermentation conditions for producing FK-506 utilizing the microorganism, Streptomyces tsukubaensis No. 9993 (FERM BP-927). The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants. <CHEM> r
Inventors
- 👤 Robert P. Borris
- 👤 Linda S. Wicker
- 👤 Deborah L. Zink
- 👤 Thoai Hung Lien
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-07 15:29
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/01; A; A61; A61P; A61P31/00; A61P31/04; A61P37/00; A61P37/02; A61P37/06
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
41 words
An immunosuppressant, "Tsukubamycin A", which exhibits positive inhibition of T-cell activation by the T-cell proliferation assay, and exhibits a high resolution mass spectral molecular ion of (m/z) 1093.6556, as the tetra-(trimethylsilyl) derivative, with characteristic fragment ions at m/z 673 and 481.
Claim 2
Dependent Claim
41 words
An immunosuppressant, "Tsukubamycin A", which exhibits positive inhibition of T-cell activation by the T-cell proliferation assay, and exhibits a high resolution mass spectral molecular ion of (m/z) 1093.6556, as the tetra-(trimethylsilyl) derivative, with characteristic fragment ions at m/z 673 and 481.
Claim 3
Dependent Claim
22 words
A pharmaceutical composition containing a therapeutically effective amount of "Tsukubamycin A" in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 4
Dependent Claim
22 words
A pharmaceutical composition containing a therapeutically effective amount of "Tsukubamycin A" in combination with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 5
Dependent Claim
24 words
The use of "Tsukubamycin A", for the preparation of a medicament useful for preventing transplantation rejection, or for treating autoimmune disease or infectious disease.
Claim 6
Dependent Claim
24 words
The use of "Tsukubamycin A", for the preparation of a medicament useful for preventing transplantation rejection, or for treating autoimmune disease or infectious disease.
Claim 7
Dependent Claim
93 words
A process for producing the immunosuppressant, "Tsukubamycin B", being the C-21 propyl analog of FK-506, which exhibits positive inhibition of T-cell activation by the T-cell proliferation assay, and exhibits a high resolution mass spectral molecular ion of (m/z) 1021.6169, as the tri-(trimethylsilyl) derivative, with characteristic fragment ions at m/z 675 and 483, comprising the step of fermenting the microorganism Streptomyces tsukubaensis No. 9993. (FERM BP-927) under submerged aerobic conditions in an aqueous carbohydrate medium, containing a nitrogen nutrient, said conditions being conducted at a pH of about 7, and recovering said "Tsukubamycin B".
Claim 8
Dependent Claim
93 words
A process for producing the immunosuppressant, "Tsukubamycin B", being the C-21 propyl analog of FK-506, which exhibits positive inhibition of T-cell activation by the T-cell proliferation assay, and exhibits a high resolution mass spectral molecular ion of (m/z) 1021.6169, as the tri-(trimethylsilyl) derivative, with characteristic fragment ions at m/z 675 and 483, comprising the step of fermenting the microorganism Streptomyces tsukubaensis No. 9993. (FERM BP-927) under submerged aerobic conditions in an aqueous carbohydrate medium, containing a nitrogen nutrient, said conditions being conducted at a pH of about 7, and recovering said "Tsukubamycin B".
References Cited (Backward Citations)
No citation records indexed.
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