Process for preparing macrocin derivatives

Patent 4559301 Issued on December 17, 1985. Estimated Expiration Date:

March 3, 2003. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Abstract Claims Description Full Text

Patent References

3326759

Tylosin derivatives and their manufacturing process
Patent #: 4092473
Issued on: 05/30/1978
Inventor: Okamoto, et al.

Tylosin derivatives
Patent #: 4205163
Issued on: 05/27/1980
Inventor: Mori , et al.

Derivatives of antibiotic tylosin Patent #: 4268665
Issued on: 05/19/1981
Inventor: Sakakibara , et al.

Inventors

Assignee

Eli Lilly and Company

Application

No. 06/471628 filed on 03/03/1983

US Classes:

435/76, The hetero ring has eight or more ring members and only oxygen as ring hetero atoms (e.g., erythromycin, spiramycin, nystatin, etc.)435/193, Transferase other than ribonuclease (2.)435/886, Streptomyces536/7.1Oxygen containing hetero ring having 12-19 members (e.g., methymycin, carbomycin, spiramycin, etc.)

Examiners

Primary: Tanenholtz, Alvin E.

Attorney, Agent or Firm

International Classes

C12P 19/00 (20060101)
C12P 19/62 (20060101)
C07H 17/00 (20060101)
C07H 17/08 (20060101)

Abstract

New macrocin and lactenocin ester derivatives of the formula: ##STR1## wherein R is formyl or hydroxymethyl; R1 is hydrogen, acetyl or propionyl; R2 is hydrogen or ##STR2## and R3 is hydrogen, acetyl, propionyl, n-butyryl or isovaleryl; provided that one of R1 or R3 must be other than hydrogen; and the acid addition salts thereof; prepared by bioconversion of macrocin or lactenocin with an acylating enzyme system produced by Streptomyces thermotolerans strains, have improved activity against Mycoplasma species.

Other References

Derwent Abstract No. 66634C/38 of Japanese Unexamined Patent J5 5043-013, 3-26-80 (Sanraku Ocean)
Derwent Abstract No. 17437C/10 of Japanese Unexamined Patent J5 5011-558, 1-26-80 (Toyo Jozo)
Derwent Abstract No. 79659C/45 of Japanese Unexamined Patent J5 5122-798, 9-20-80 (Toyo Jozo)
Derwent Abstract No. 74422C/42 of Japanese Unexamined Patent J5 5115-899, 9-6-80 (Toyo Jozo)
Okamoto et al., "The Activity of 4"-Acylated Tylosin Derivatives Against Macrolide-Resistant Gram-Positive Bacteria", J. Antibiotics 32, 542-544 (1979)
Okamoto et al., "Physico-Chemical Properties of New Acyl Derivatives of Tylosin Produced by Microbial Transformation", J. Antibiotics 33, 1300-1308 (1980)
Okamoto et al., "Biological Properties of New Acyl Derivatives of Tylosin", J. Antibiotics 33, 1309-1315, (1980)
Okamoto et al., "Studies on the Effects of 3-Acetyl-4"-Isovaleryltylosin Against Multiple-Drug Resistant Strains of Staphylococcus aureus", J. Antibiotics 34, 305-312 (1981)
Tsuchiya et al., "Studies of Tylosin Derivatives Effective Against Macrolide-Resistant Strains: Synthesis and Structure Activity Relationships", J. Antibiotics 35, 661-672 (1982)
Derwent Abstract No. 27592A/15 of Japanese Unexamined Patent J5 3021-182, 2-27-78 (Sanraku Ocean)