Abstract: The present invention relates to a novel and efficient process for the preparation of 8-hydroxybicyclo[7.3.1]tridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring system. The present invention also provides a method for treating mammalian malignant tumors by administering to an animal in need of such treatment an antitumor effective amount of a compound of the present invention.
Abstract: The present invention relates to a fermentation process for producing BMY-28960 and desxylosyl BMY-28960, and to a novel BMY-28960-producing organism belonging to the genus Actinomadura and designated as strain AB 1236 (ATCC 55208).
Abstract: Disclosed are antibiotics BU-3608 FA-1 and FA-2 and alkyl derivatives thereof. These compounds are useful as antifungal agents. BU-3608 FA-1 and FA-2 are produced from Actinomadura hibisca in a medium containing a source of D-serine.
Abstract: The invention relates to anthracycline conjugates comprising at least one anthracycline molecule linked to a molecule that is reactive with a cell population to be eliminated such as antibody, bombesin, EGF and transferrin. Each anthracycline molecule, having a keto group at the C-13 position, is conjugated to the antibody via a linker arm and is bound to that linker arm via an acid-sensitive acylhydrazone bond at the 13-keto position of the anthracycline. The linker additionally contains a disulfide or thioether linkage as part of the antibody or ligand attachment to the immunoconjugate. The novel anthracycline acylhydrazone derivatives are useful in the preparation of the conjugates of this invention. The acid-sensitive hydrazone bond of the conjugates of this invention allows the release of free anthracycline from the conjugates in the acidic external or internal environment of the target cell.
Type:
Grant
Filed:
May 17, 1989
Date of Patent:
June 16, 1992
Assignee:
Bristol-Myers Squibb Company
Inventors:
Robert S. Greenfield, Gary R. Braslawsky, Lee J. Olech, Takushi Kaneko, Peter A, Kiener
Abstract: Disclosed are antibiotics BU-3608 FA-1 and FA-2 and alkyl derivatives thereof. These compounds are useful as antifungal agents. BU-3608 FA-1 and FA-2 are produced from Actinomadura hibisca in a medium containing a source of D-serine.
Abstract: Novel antibiotic herein designated as BU-3608, BU-3608 B, and BU-3608 C are produced by fermentation of Actinomadura hibisca Strain No. P157-2, ATCC 53557, and Strain No. Q278-4, ATCC 53646. The antibiotics possess antifungal and antiviral activities.
Abstract: Production of an antiviral antibiotic complex, BU-3889V and its bioactive components A.sub.1, A.sub.2, A.sub.3, D.sub.1, D.sub.2 and D.sub.3, by fermentation of a BU-3889V producing strain of the new microorganism Amycolatopsis orientalis ATCC-53884 is disclosed. Complex BU-3889V is recovered and the components separated by the use of ion exchange chromatography techniques. The bioactive components are characterized by their physico-chemical characterizing properties. The products have been found to be effective to inhibit viruses including herpes simplex virus, human immunodeficiency virus (HIV) and influenza virus.
Abstract: Glidobactin PF-1 of the formula ##STR1## having antitumor activity is prepared by cultivation of Polyangium brachysporum in a nutient medium containing a suitable fatty acid ester, such linolenate, together with other assimilable sources of carbon and nitrogen.
Abstract: The present invention relates to a novel .alpha.-glucosidase inhibitor, pradimicin Q, having the following formula ##STR1## and its pharmaceutically acceptable base salts.
Abstract: A new antibiotic designated BMY-42448 is produced by fermentation of Micromonospora narashinoensis strain C39217-R109-7 (ATCC-53791). BMY-42448 exhibits both in vitro and in vivo antitumor activity.
Type:
Grant
Filed:
January 10, 1990
Date of Patent:
January 21, 1992
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Daniel R. Schroeder, Kin S. Lam, Grace A. Hesler, Donald R. Gustavson, Koji Tomita, Ronald L. Berry
Abstract: The present invention relates to antitumor 4'-demethylepipodophyllotoxin glycosides having the formula ##STR1## wherein R is a pentose selected from the group consisting of .beta.-D-ribopyranosyl, peracyl .beta.-D-ribopyranosyl, .beta.-D-xylopyranosyl, peracyl .beta.-D-xylopyranosyl, .alpha.-D-xylopyranosyl, peracyl .alpha.-D-xylopyranosyl, .alpha.-D-arabinopyranosyl, 3,4-O-(C.sub.1-4)alkylidene-D-ribopyranosyl, 2-O-acyl-3,4-O-(C.sub.1-4)alkylidene-D-ribopyranosyl, and .beta.-D-ribofuranosyl; P is hydrogen, or --PO.sub.3 H.sub.2 or a pharmaceutically acceptable salt thereof.
Abstract: An antitumor antibiotic designated BMY-41950 is produced by fermentation of Streptomyces staurosporeus ATCC 55006 or Streptomyces hygroscopicus ATCC 53730. The BMY-41950 antibiotic exhibits both antimicrobial and antitumor activities.
Type:
Grant
Filed:
November 5, 1990
Date of Patent:
December 17, 1991
Assignee:
Bristol-Myers Company
Inventors:
Daniel Schroeder, Kin S. Lam, Jacqueline Mattei, Grace A. Hesler
Abstract: The antibiotic designated BU-4061T is produced by fermentation of actinomycete strain Q996-17 (ATCC-53904). The BU-4061T antibiotic exhibits both in vitro and in vivo antitumor activity.
Abstract: The present invention provides antitumor 4'-Demethylepipodophyllotoxin glycosides characterized by the fact that the glycoside moiety is altrose.
Abstract: Disclosed are antibiotics BU-3608 FA-1 and FA-2 and alkyl derivatives thereof. These compounds are useful as antifungal agents. BU-3608 FA-1 and FA-2 are produced from Actinomadura hibisca in a medium containing a source of D-serine.
Abstract: Cephalosporin intermediates having a replacable organosulfonylyoxy or heterocyclothio group in the 3-position undergo a carbon alkylation process with organocopper reagents to provide 3-hydrocarbon substituted cephalosporin antibiotics.
Abstract: Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility.
Type:
Grant
Filed:
December 14, 1989
Date of Patent:
August 20, 1991
Assignee:
Bristol-Myers Company
Inventors:
Mark G. Saulnier, Peter D. Senter, John F. Kadow
Abstract: The epipodophyllotoxin glucosides disclosed are acylated at herein one or both sugar hydroxyl groups. These compounds exhibit significant activity against P388 murine leukemia.