Abstract: A new and improved process for the preparation of C-4' etherified anthracycline glycoside derivatives is provided. The new process involves fewer steps than the prior art process and gives the antibiotic end-products in higher yield.
Type:
Grant
Filed:
April 13, 1981
Date of Patent:
November 23, 1982
Assignee:
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
Abstract: A novel peptide antibiotic complex designated herein as Bu-2470 is produced by fermentation of Bacillus circulans strain G493-B6 (ATCC 31,805). Complex Bu-2470 may be separated into four bioactive peptide antibiotics designated as Bu-2470A, B.sub.1, B.sub.2a, and B.sub.2b. The complex and individual bioactive factors possess significant antimicrobial activity.
Abstract: Supra-additive blood platelet antiaggregation activity is observed with anagrelide in combination with those non-steroidal anti-inflammatory agents which are inhibitors of platelet cyclooxygenase. The supra-additive effects of such combinations make possible new compositions and methods for both therapeutic and prophylactic treatment of thrombosis and other disorders associated with blood platelet aggregation.
Type:
Grant
Filed:
July 30, 1981
Date of Patent:
November 2, 1982
Assignee:
Bristol-Myers Company
Inventors:
James S. Fleming, Jr., Joseph P. Buyniski
Abstract: New 4-demethoxy-11-deoxydaunomycin and 4-demethoxy-11-deoxyadriamycin anthracycline derivatives have been prepared and found to be useful antimicrobial and antitumor agents.
Type:
Grant
Filed:
September 11, 1981
Date of Patent:
October 19, 1982
Assignee:
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
Abstract: A novel series of 3,8-dihydroxy-scirpen-4.beta.,15-diol esters is provided for use as antitumor agents. The compounds are also useful as intermediates in the preparation of other trichothecene antitumor agents.
Abstract: A novel peptide antibiotic complex designated herein as Bu-2470 is produced by fermentation of Bacillus circulans strain G493-B6 (ATCC 31,805). Complex Bu-2470 may be separated into four bioactive peptide antibiotics designated as Bu-2470A, B.sub.1, B.sub.2a, and B.sub.2b. The complex and individual bioactive factors possess significant antimicrobial activity.
Abstract: This invention concerns three particular crystalline monolactate salts of the antitumor agent 4'-(9-acridinylamino)methanesulfon-m-anisidide. The salts are characterized in having unexpectedly high water-solubility.
Abstract: Novel mono-, di- and triacylated derivatives of scirpentriol are provided for use as antitumor agents. Also provided are methods for the production of such derivatives.
Type:
Grant
Filed:
March 4, 1981
Date of Patent:
June 1, 1982
Assignee:
Bristol-Myers Company
Inventors:
Henry Schmitz, Takushi Kaneko, John M. Essery, Terrence W. Doyle
Abstract: Novel 3-hydroxyiminoscirpen-4.beta., 15-diol esters and derivatives thereof are provided for use as antitumor agents. Also provided are processes for producing the above compounds and methods for using them to inhibit malignant tumors in mammals.
Type:
Grant
Filed:
January 9, 1981
Date of Patent:
June 1, 1982
Assignee:
Bristol-Myers Company
Inventors:
Takushi Kaneko, John M. Essery, Henry Schmitz, Terrence W. Doyle
Abstract: Disclosed are water-soluble salts of the known coordination compounds 2-hydroxymalonato diammine platinum (II), 2-hydroxymalonato (1,2-diaminocyclohexane)platinum (II) and 2-hydroxymalonato (1,1-diaminomethylcyclohexane)platinum (II). The novel sodium and ammonium salts of the present invention possess high water-solubility, thus allowing intravenous dosage forms to be prepared.
Abstract: The invention concerns a crystalline monogluconate salt of the antitumor agent 4'-(9-acridinylamino)-methanesulfon-m-anisidide and compositions comprising mixtures of such salt with an organic acid selected from gluconic acid, gluconolactone or mixtures thereof. The novel salt and compositions are characterized in having unexpectedly high water-solubility.
Type:
Grant
Filed:
October 17, 1980
Date of Patent:
March 30, 1982
Assignee:
Bristol-Myers Company
Inventors:
Daniel Bouzard, Claude Perol, Jacques Stemer, Abraham Weber, Edmund S. Granatek
Abstract: Addition of certain amine precursor compounds to the culture medium during fermentation of a tallysomycin-producing strain of Streptoalloteichus hindustanus results in production of new tallysomycin derivatives having advantageous antimicrobial and antitumor properties.
Abstract: New anthracycline derivatives of adriamycin and daunomycin prepared by the etherification of the C-4' and/or C-14 hydroxyl groups of the starting material glycosides are found to be useful antimicrobial and antitumor agents.
Type:
Grant
Filed:
January 31, 1980
Date of Patent:
December 1, 1981
Assignee:
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
Abstract: A known antibiotic substance designated herein as rachelmycin is produced by fermentation of Streptomyces sp. strain C-329, variant 70 (ATCC 31128) or Streptomyces anandii subsp. arraffinosus strain C-22, 437 (ATCC 31431). Rachelmycin exhibits both antibiotic and antitumor properties.
Type:
Grant
Filed:
October 6, 1980
Date of Patent:
November 17, 1981
Assignee:
Bristol-Myers Company
Inventors:
Donald E. Nettleton, Jr., James A. Bush, William T. Bradner
Abstract: Novel mono-, di- and triacylated derivatives of scirpentriol are provided for use as antitumor agents. Also provided are methods for the production of such derivatives.
Type:
Grant
Filed:
April 4, 1980
Date of Patent:
August 18, 1981
Assignee:
Bristol-Myers Company
Inventors:
Henry Schmitz, Takushi Kaneko, John M. Essery, Terrence W. Doyle
Abstract: This invention relates to 2-substituted and 2,6-disubstituted penem compounds of the formula ##STR1## wherein Y is hydrogen, halo or certain organic radicals and X represents certain hetero-interrupted substituted alkyl radicals. Also included in the invention are pharmaceutically acceptable salts of the above compounds and derivatives of the above compounds in which the carboxyl group at the 3-position is protected as by an easily removable ester protecting group. The compounds of the present invention are potent antibacterial agents or are of use as intermediates in the preparation of such agents.
Abstract: This invention relates to 2-substituted and 2,6-disubstituted penem compounds of the formula ##STR1## wherein Y is hydrogen, halo or certain organic substituents and X represents certain organic substituents. Also included in the invention are pharmaceutically acceptable salts of the above compounds and derivatives of the above compounds in which the carboxyl group at the 3-position is protected as by an easily removable ester protecting group. The compounds of the present invention are potent antibacterial agents or are of use as intermediates in the preparation of such agents.
Abstract: Diagnostic method for detecting cancer in humans comprising assaying a serum sample for concentration of a particular DNA-binding protein. The concentration of this serum protein has been found to be significantly different in patients having cancer than in cancer-free patients.
Abstract: Novel 3-oxoscirpen-4.beta.,15-diol esters and derivatives thereof are provided for use as antitumor agents. Also provided are processes for producing the above compounds and methods for using them to inhibit malignant tumors in mammals.
Type:
Grant
Filed:
November 19, 1979
Date of Patent:
May 12, 1981
Assignee:
Bristol-Myers Company
Inventors:
Takushi Kaneko, John M. Essery, Henry Schmitz, Terrence W. Doyle
Abstract: A novel water-soluble basic antibiotic complex designated herein as Bu-2349 is produced by fermentation of Bu-2349-producing strains of the genus Bacillus. Complex Bu-2349 and its bioactive components designated as Bu-2349A and B are found to possess marked inhibitory activity against gram-positive and gram-negative bacteria including various types of aminoglycoside-resistant bacteria.