Claims
- 1. A pharmaceutically acceptable di-basic salt of MM 4550 A which is at least 70% pure wherein MM 4550 A is a solid carboxylic acid of the molecular formula C.sub.13 H.sub.16 O.sub.9 N.sub.2 S.sub.2 which in the form of a substantially pure sodium salt has the following characteristics:
- (a) in aqueous solution, it has a characteristic ultraviolet spectrum with absorption maxima at about 238 nm and at about 287 nm;
- (b) when present at 0.4% w/w in a freshly prepared KBr disc, it has a characteristic infra-red spectrum substantially as shown in FIG. 2 and has absorption maxima at, inter alia, about 3450, 2950, 1765, 1695, 1510, 1390 and 1260 cm.sup.-1 ;
- (c) it has a characteristic n.m.r. spectrum which when taken in D.sub.2 O is substantially as shown in FIG. 3, which spectrum possesses, inter alia, (i) a pair of low field doublets centered approximately at 2.45.tau. and 3.65.tau. with coupling constants of approximately 15 Hz; (ii) a doublet centered at approximately 8.55.tau.; and (iii) a sharp singlet at approximately 7.95.tau.;
- (d) it possesses antibacterial activity against various species including, inter alia, strains of Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Klebsiella aerogenes, Proteus mirabilis, Acinetobacter anitratus, Serratia marcescens and Shigella sonnei;
- (e) it synergizes the antibacterial activity of ampicillin against certain .beta.-lactamase producing bacteria including strains of Escherichia coli, Klebsiella aerogenes, Proteus mirabilis, Proteus morganii and Staphylococcus aureus Russell; and
- (f) it is not a polypeptide or protein.
- 2. A pharmaceutically acceptable di-basic salt of MM 4550 A according to claim 1 in the form of an alkali metal salt.
- 3. A pharmaceutically acceptable di-basic salt of MM 4550 A according to claim 1 in the form of the sodium, potassium, calcium, magnesium, aluminium or ammonium salt.
- 4. A pharmaceutically acceptable di-basic salt of MM 4550 A according to claim 1 in the form of the di-sodium salt.
- 5. A pharmaceutically acceptable di-basic salt of MM 4550 A according to claim 1 in the form of the di-potassium salt.
- 6. A pharmaceutically acceptable di-basic salt of MM 4550 A according to claim 1 which is at least 80% pure.
- 7. A pharmaceutically acceptable di-basic salt of MM 4550 A according to claim 1 which is 90% to 100% pure.
- 8. A process for the preparation of substantially pure MM 4550 A in the form of a pharmaceutically acceptable di-basic salt wherein MM 4550 A is a solid carboxylic acid of the molecular formula C.sub.13 H.sub.16 O.sub.9 N.sub.2 S.sub.2 which in the form of a substantially pure sodium salt has the following characteristics:
- (a) in aqueous solution, it has a characteristic ultraviolet spectrum with absorption maxima at about 238 nm and at about 287 nm;
- (b) when present at 0.4% w/w in a freshly prepared KBr disc, it has a characteristic infrared spectrum substantially as shown in FIG. 2 and has absorption maxima at, inter alia, about 3450, 2950, 1765, 1695, 1510, 1390 and 1260 cm.sup.-1 ;
- (c) it has a characteristic n.m.r. spectrum which when taken in D.sub.2 O is substantially as shown in FIG. 3, which spectrum possesses, inter alia, (i) a pair of low field doublets centered approximately at 2.45.tau. and 3.65.tau. with coupling constants of approximately 15 Hz; (ii) a doublet centered at approximately 8.55.tau.; and (iii) a sharp singlet at approximately 7.95.tau.;
- (d) it possesses antibacterial activity against various species including, inter alia, strains of Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Klebsiella aerogenes, Proteus mirabilis, Acinetobacter anitratus, Serratia marcescens and Shigella sonnei;
- (e) it synergizes the antibacterial activity of ampicillin against certain .beta.-lactamase producing bacteria including strains of Escherichia coli, Klebsiella aerogenes, Proteus mirabilis, Proteus morganii and Staphylococcus aureus Russell; and
- (f) it is not a polypeptide or protein;
- which comprises cultivating a MM 4550 A producing strain of Streptomyces olivaceus having the same identifying characteristics as ATCC 31126 in a suitable medium containing an assimilable source of carbon, hydrogen, sulphur and nitrogen until a significant amount of antibiotic activity has been imparted to said medium and recovering a substantially pure, pharmaceutically acceptable di-basic salt of MM 4550 A from the culture medium.
- 9. A process according to claim 8 for the preparation of substantially pure MM 4550 A in the form of a pharmaceutically acceptable di-sodium or di-potassium salt wherein MM 4550 A is recovered in the form of a substantially pure, pharmaceutically acceptable di-sodium or di-potassium salt.
Priority Claims (1)
Number |
Date |
Country |
Kind |
13855/74 |
Mar 1974 |
GBX |
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CROSS REFERENCE
This application is a continuation-in-part of U.S. patent application Ser. No. 559,973 filed Mar. 19, 1975 now abandoned.
US Referenced Citations (3)
Number |
Name |
Date |
Kind |
3919415 |
Butterworth et al. |
Nov 1975 |
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3928569 |
Umezawa et al. |
Dec 1975 |
|
3950357 |
Kahan et al. |
Apr 1976 |
|
Non-Patent Literature Citations (1)
Entry |
Maeda et al., J. of Antibiotics, Sep. 1977, pp. 770-772. |
Continuation in Parts (1)
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Number |
Date |
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Parent |
559973 |
Mar 1975 |
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