Abstract: The novel antitumor antibiotic designated herein as BU-3420T is produced by fermentation of Micromonospora chersina strain M956-1 (ATCC 53710). BU-3420T and its triacetate derivative possess antibacterial and antifungal activity and also inhibit the growth of mammalian tumors such as P388 leukemia in mice.
Abstract: There is disclosed a drug-monoclonal antibody conjugate wherein the antibody is linked to a antitumor drug using disulfide benzyl carbamate or carbonate as the linker. Also disclosed is a method of delivering an active antitumor drug to the site of tumor cells in a mammal by administering the drug-monoclonal antibody conjugate.
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: This invention provides novel tetrazole intermediates of the formula ##STR1## wherein R.sup.1 and R.sup.4 each are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl;R.sup.2, R.sup.3, R.sup.5 and R.sup.6 each are independently hydrogen, halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;B is hydrogen, C.sub.1-4 alkoxycarbonyl, CH.sub.2 Y or CH.sub.2 Z;Y is hydrogen, hydroxyl or X;Z is ##STR2## X is bromo, chloro or iodo; R.sup.10 is C.sub.1-4 alkyl; andR.sup.11 is phenyl which is unsubstituted or substituted by one or two C.sub.1-4 alkyl or chloro substituents.and processes thereof which are useful for the preparation of antihypercholesterolemic agents.
Type:
Grant
Filed:
November 1, 1989
Date of Patent:
July 3, 1990
Assignee:
Bristol-Myers Company
Inventors:
John J. Wright, Sing-Yuen Sit, Neelakantan Balasubramanian, Peter J. Brown
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: A process for the selective formation of oximino o-protected derivatives of lower alkyl 2-(2-aminothiazol-4-yl)-2-oximinoacetates, and their use in the acylation of 7-amino-cephalosporin compounds is disclosed.
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 new antitumor antibiotic designated herein as BMY-28121 is produced by fermentation of Streptomyces albus strain K7331-113 (ATCC 39897). BMY-28121, which may be recovered from the fermentation broth in either its natural free hydroxy form (BMY-28121A) or methyl ether form (BMY-28121B), inhibits gram-positive bacteria and anaerobes and inhibits the growth of mammalian tumors such as P-388 leukemia, L-1210 leukemia and B16 melanoma.
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: The present invention relates to novel intermediates of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl and R is ##STR2## --CH.sub.2 OH or --CH.sub.2 X in which X is a conventional leaving group and Y is lower alkyl and the use thereof in a process for the preparation of certain histamine H.sub.2 -antagonists.
Abstract: The present invention provides novel mitomycin analogs containing a disulfide group and processes for the preparation thereof. These compounds are mitomycin A analogs in which the 7-alkoxy group bears an organic substituent incorporating a disulfide group. Mitomycin A is an antibiotic of established utility, and the 7-O-substituted mitosane analogs thereof have similar utility.
Type:
Grant
Filed:
November 7, 1988
Date of Patent:
May 22, 1990
Assignee:
Bristol-Myers Company
Inventors:
Dolatrai M. Vyas, Terrence W. Doyle, Richard A. Partyka
Abstract: A new antibiotic having the chromophore structure of the pluramycin family of antibiotics is produced by fermentation of Streptomyces ciolaceus ATCC 53807. The new antibiotic designated BU-3839T, exhibits potent antibacterial activity and also inhibits the growth of tumors in experimental animal systems.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl;A is ##STR2## and R.sup.5 is hydrogen, a hydrolyzable ester group or a cation to form a non-toxic pharmaceutically acceptable salt,are novel antihypercholesterolemic agents which inhibit cholesterol biosynthesis. Intermediates and processes for their preparation are disclosed.
Abstract: The present invention relates to novel intermediates of the formula ##STR1## wherein R is lower alkyl or cyclohexyl, and X is hydroxy or a conventional leaving group, and the use thereof in a process for the preparation of certain histamine H.sub.2 -antagonists.
Type:
Grant
Filed:
April 11, 1988
Date of Patent:
May 22, 1990
Assignee:
Bristol-Myers Company
Inventors:
James L. Douglas, Guy Fabre, Claude Demosthene
Abstract: There is provided new antitumor antibiotic substances designated herein as BBM-1675C and BBM-1675D, said substances being produced by selective chemical hydrolysis of the bioactive components BBM-1675A.sub.1 (esperamicin A.sub.1) or BBM-1675A.sub.2 (esperamicin A.sub.2). The new antitumor antibiotics exhibit both antimicrobial activity and antitumor activity.
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: The novel antitumor antibiotic designated herein as BU-3420T is produced by fermentation of Micromonospora chersina strain M956-1 (ATCC 53710). BU-3420T and its triacetate derivative possess antibacterial and antifungal activity and also inhibit the growth of mammalian tumors such as P388 leukemia in mice.
Abstract: Novel peptide antibiotics designated herein as BU-2867T F and G are produced by fermentation of Polyangium brachysporum strain K481-B101 (ATCCC 53080). The new antibiotics are found to have antifungal activity and to inhibit P388 lymphatic leukemia in rodents.