Macrocyclic lactone compounds and their production process
AssigneePfizer Inc.
InventorsHiroyuki Nishida, Yuji Yamauchi, Taisuke Inagaki, Yasuhiro Kojima, Nakao Kojima
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Abstract
This invention provides a process for producing a macrocyclic lactone compound, which comprises cultivating Actinoplanes sp. FERM BP-3832, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and then isolating a macrocylic lactone compound from the fermentation broth. The compounds produced by this process include a compound of the following formula: The present invention also relates to a pharmaceutical composition comprising the same, which is useful as immunosuppressive, antimycotic, antitumor agent or the like.
Claims9
A macrocyclic lactone compound designated CJ-13,502, made by cultivating a microorganism having the identifying characteristics of Actinoplanes sp. FERM BP-3832, or a mutant or recombinant form thereof, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and having the characteristics of ESI mass spectrum shown in FIG. 3, with m/z 908 [M+Na]+;
- the UV spectrum shown in FIG. 7, with a UV max at 267, 277 and 288 nm in methanol;
- and a retention time of 12.8 min. on HPLC using a Pegasil ODS column (4.6×150 mm) and eluting with methanol-water (7:3 to 10:0) for 30 min at a flow rate of 0.7 ml/min at 42° C.
A macrocylic lactone compound designated CJ-13,503, made by cultivating a microorganism having the identifying characteristics of Actinoplanes sp. FERM BP-3832, or a mutant or recombinant form thereof, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and having the characteristics of ESI mass spectrum shown in FIG. 4, with m/z 896 [M+Na]+;
- the UV spectrum shown in FIG. 8, with a UV max at 267, 277 and 288 nm in methanol;
- and a retention time of 10.9 min. on HPLC using a Pegasil ODS column (4.6×150 mm) and eluting with methanol-water (7:3 to 10:0) for 30 min at a flow rate of 0.7 ml/min at 42° C.
A macrocylic lactone compound designated CJ-13,504, made by cultivating a microorganism having the identifying characteristics of Actinoplanes sp. FERM BP-3832, or a mutant or recombinant form thereof, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and having the characteristics of ESI mass spectrum shown in FIG. 5, with m/z 908 [M+Na]+;
- the UV spectrum shown in FIG. 9, with a UV max at 267, 277 and 288 nm in methanol;
- and a retention time of 11.9 min. on HPLC using a Pegasil ODS column (4.6×150 mm) and eluting with methanol-water (7:3 to 10:0) for 30 min at a flow rate of 0.7 ml/min at 42° C.
Dependencies are inferred from the claim text.