Abstract: Novel cyclic orthoesters and orthocarbonates of 4'-demethylepipodophyllotoxin glucoside are disclosed in the present invention. These compounds are active against experimental murine P388 leukemia.
Abstract: Kedarcidin is a protein antitumor antibiotic produced by Streptoalloteichus sp. nov. strain L585-6, ATCC 53650. The antibiotic comprises a non-protein chromophore and a single chain polypeptide having 114 amino acid residues.
Type:
Grant
Filed:
March 17, 1989
Date of Patent:
March 19, 1991
Assignee:
Bristol-Myers Company
Inventors:
Sandra J. Hofstead, James A. Matson, Kin S. Lam, Salvatore Forenza, James A. Bush, Koji Tomita
Abstract: The present invention relates to novel antitumor compounds which are 4'-demethylepipodophylloxtoxin derivatives. More particularly, the novel compounds are 4'-demethylepipodophyllotoxin allopyranosides, allofuranosides, and mannopyranosides.
Abstract: Disclosed herein are novel .alpha.-arylcarbamoyl cyanoacetic esters, thioesters, and amides which exhibit anti-inflammatory/antiarthritic activities.
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 present invention provides novel dimers of epipodophyllotoxin glucosides wherein the two units are connected via a diacyl linker. These compounds have useful property as tumor inhibiting agents.
Abstract: Disclosed herein are N-alkyl derivatives of antibiotics BU-3608, BU-3608 B, C, D and E as well as the corresponding desxylosyl compounds. These novel compounds are useful as antifungal agents.
Abstract: Novel antitumor epipodophyllotoxin glucoside lactam derivatives are prepared by first converting the lactone ring of the parent compound to the open-chain trans-hydroxy hydrazide, condensing the hydrazide with a carbonyl compound to form the corresponding hydrazone, and finally cyclizing the trans-hydroxy hydrazone using diethylazodicarboxylate and triphenylphosphine.
Abstract: The invention relates to chemically stable, concentrated solutions of cis-diamminedinitratoplatinum which are pH-stabilized with nitric acid and are readily convertible to parenteral cisplatin solutions by addition of sources of chloride ion.
Type:
Grant
Filed:
November 23, 1988
Date of Patent:
August 7, 1990
Assignee:
Bristol-Myers Company
Inventors:
Murray A. Kaplan, Robert K. Perrone, Joseph B. Bogardus, Kenneth W. Douglas, Sr.
Abstract: Novel 4'-esters, 4'-carbonates and 4'-carbamates of 4'-demethylepipodophyllotoxin glucosides are disclosed. These agents exhibit antitumor activity in animals.
Type:
Grant
Filed:
December 2, 1988
Date of Patent:
June 19, 1990
Assignee:
Bristol-Myers Company
Inventors:
Mark G. Saulnier, Dolatrai M. Vyas, David R. Langley
Abstract: Disclosed herein are isoxazole-4-carboxamides having the formula ##STR1## wherein R.sup.1 is C.sub.3-6 cycloalkyl and R.sup.2 is selected from the group consisting of C.sub.1-5 alkyl, C.sub.2-5 alkenyl, C.sub.2-5 alkynyl, C.sub.3-6 cycloalkyl, phenyl, and phenyl substituted with at least one group selected from C.sub.1-5 alkyl, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, and halo-substituted C.sub.1-5 alkyl; with the proviso that when R.sup.1 is cyclopropyl, R.sup.2 is not methyl, ethyl, or cyclobutyl; or R.sup.1 is C.sub.1-5 alkyl and R.sup.2 is phenylmethyl wherein the ring portion is opt. substituted with a halo-substituted C.sub.1-5 alkyl group. These compounds have antiinflammatory and antiarthritic activities and are also useful as intermediates in the preparation of .beta.-ketonitriles.
Abstract: A solution of etoposide in dimethylisosorbide is disclosed. The solution is useful for filling gelatin capsules and may also be formulated into parenteral dosage forms.
Type:
Grant
Filed:
September 12, 1988
Date of Patent:
May 22, 1990
Assignee:
Bristol-Myers Company
Inventors:
Gururaj Bykadi, Murray A. Kaplan, Richard G. Corrao, Edward J. Bara, Ismat Ullah, Shreeram N. Agharkar
Abstract: Etoposide-3',4'-quinone is converted into a phosphorane or phosphate ester by reaction with an organic phosphine or phosphite. The resulting phosphoranes and phosphates have anti-tumor activity in animals.
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:
May 27, 1988
Date of Patent:
February 27, 1990
Assignee:
Bristol-Myers Company
Inventors:
Mark G. Saulnier, Peter D. Senter, John F. Kadow
Abstract: This invention relates to novel 3'-demethoxy epipodophyllotoxin glucosides, their use as anti-tumor agents, and pharmaceutical compositions thereof.
Abstract: Disclosed herein are N.sup.7 -alkylphosphate derivatives of mitomycin C and porfiromycin showing antitumor activity against transplanted human tumor and reduced toxicity relative to the parent N.sup.7 -alkanol mitomycin compounds.