Patents Represented by Attorney David M. Morse

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  • In-vial deposition of 7-(dimethylaminomethylene)amino-9.alpha.-methoxymitosane
    Patent number: 4792566
    Abstract: There is disclosed a process for the in-vial deposition of 7-(dimethylaminomethylene)amino-9a-methoxymitosane in sterile unit dosage form. A solution of this compound is introduced into a sterile vial in a solution of tertiary-butanol. The tertiary-butanol is then removed, e.g., by evaporation or lyophilization, and the vial is closed by appropriate means. The thus deposited material can contain up to 0.5 mole equivalent of tertiary-butanol as a hemi-solvate and is very stable to heat.
    Type: Grant
    Filed: May 14, 1986
    Date of Patent: December 20, 1988
    Assignee: Bristol-Myers Company
    Inventors: Murray A. Kaplan, Dolatrai M. Vyas, Nagaswara R. Palepu, Chih-Ming J. Chen
  • Crystalline upsilon-form bestatin and processes for its preparation
    Patent number: 4786754
    Abstract: A stable, non-hygroscopic, crystalline .gamma.-form of bestatin is prepared from the .alpha.- or .beta.-form of bestatin by heating at a temperature of from about 148.degree. C. to the melting point of bestatin, or by suspending or kneading in certan specified solvents.
    Type: Grant
    Filed: July 13, 1987
    Date of Patent: November 22, 1988
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Hai
    Inventors: Takashi Terada, Tetsushi Saino, Terukatsu Sakurai, Hamao Umezawa, Masaaki Ishizuka
  • Rebeccamycin analogs
    Patent number: 4785085
    Abstract: There are disclosed analogs of the antitumor agent, rebeccamycin, which possess antineoplastic properties against mammalian, particularly experimental animal, tumor systems. The compounds of the invention are aminoalkylated derivatives of rebeccamycin produced by first reacting rebeccamycin with a strong base to obtain a reactive intermediate and then reacting the reactive intermediate with an aminoalkyl compound.
    Type: Grant
    Filed: November 21, 1986
    Date of Patent: November 15, 1988
    Assignee: Bristol-Myers Company
    Inventors: Takushi Kaneko, Henry S. Wong, Jacob J. Utzig
  • Crystalline gamma-form bestatin and processes for its preparation
    Patent number: 4769490
    Abstract: A stable, non-hygroscopic, crystalline .gamma.-form of bestatin is prepared from the .alpha.- or .beta.-form of bestatin by heating at a temperature of from about 148.degree. C. to the melting point of bestatin, or by suspending or kneading in certain specified solvents.
    Type: Grant
    Filed: April 2, 1987
    Date of Patent: September 6, 1988
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Takashi Terada, Tetsushi Saino, Terukatsu Sakurai, Hamao Umezawa, Masaaki Ishizuka
  • Isoxazoline intermediates
    Patent number: 4767863
    Abstract: New and more efficient chemical processes are provided for preparing (.alpha.S, 5S)-.alpha.-amino-3-chloro-2-isoxazoline-5-acetic acid (AT-125), (.alpha.S, 5S)-.alpha.-amino-3-bromo-2-isoxazoline-5-acetic acid (bromo AT-125) and the C-5 epimers thereof. The disclosed processes allow the above-mentioned antitumor agents to be produced in high yield and purity with substantially fewer steps than prior art chemical procedures.
    Type: Grant
    Filed: June 25, 1987
    Date of Patent: August 30, 1988
    Assignee: Bristol-Myers Company
    Inventors: Dolatrai M. Vyas, Terrence W. Doyle, Yulin Chiang
  • Pad dispenser
    Patent number: 4765482
    Abstract: A pad dispenser for moistened treatment pads includes a wide mouth container and a pad elevator which is receivable within the container. The pad elevator has a generally planar pad support platform to whose periphery are joined a plurality of spaced, resilient collets. A generally vertically directed grasping stem is formed in the middle of the platform. A plurality of treatment pads or disks are positionable in a generally on edge array on the pad elevator's platform. Access to these pads is afforded by raising of the pad elevator within the container. Once raised, the pad elevator will be maintained in its elevated position by a sliding interference fit between the elevator collets and the container sidewall.
    Type: Grant
    Filed: December 18, 1987
    Date of Patent: August 23, 1988
    Assignee: Bristol-Myers Company
    Inventor: Anthony D. Delia
  • Carbapenem antibiotics
    Patent number: 4746736
    Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents a C.sub.1 -C.sub.6 straight or branched chain alkylene group; R.sup.5 represents an optionally substituted aliphatic cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical and ##STR2## represents a nitrogen-containing aromatic heterocycle attached to the alkylene group A at a ring carbon atom and quaternized by substituent R.sup.5. Such derivatives are useful as potent antibacterial agents.
    Type: Grant
    Filed: October 24, 1986
    Date of Patent: May 24, 1988
    Assignee: Bristol-Myers Company
    Inventor: Choung U. Kim
  • Semi-synthetic peptide antibiotics
    Patent number: 4742047
    Abstract: Semi-synthetic derivatives of the BU-2867T antibotics are disclosed. These derivatives are active against experimental mammalian tumors, and may be prepared from enzymatic degradation product(s) of BU-2867T A.
    Type: Grant
    Filed: October 10, 1986
    Date of Patent: May 3, 1988
    Assignee: Bristol-Myers Company
    Inventors: Masahisa Oka, Keiichi Numata, Masataka Konishi
  • Antineoplastic platinum complexes
    Patent number: 4739087
    Abstract: Novel platinum(II) complexes of 1,2-diaminocyclohexane, 2,2'-bipiperidine, 1,2-diamino-2,4-dimethylpentane, 1,2-diaminocyclooctane, 3,4-diamino-2,5-dimethylhexane and 1-aminomethylcyclooctylamine are provided: such complexes are of use in inhibiting the growth of certain mammalian tumors.
    Type: Grant
    Filed: January 10, 1985
    Date of Patent: April 19, 1988
    Assignee: Bristol-Myers Company
    Inventors: Robert J. Speer, David P. Stewart
  • Carbapenem antibiotics
    Patent number: 4732977
    Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents a C.sub.1 -C.sub.6 straight or branched chain alkylene group; R.sup.5 represents an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical and ##STR2## represents a nitrogen-containing aromatic heterocycle attached to the alkylene group A at a ring carbon atom and quaternized by substituent R.sup.5. Such derivatives are useful as potent antibacterial agents.
    Type: Grant
    Filed: November 10, 1986
    Date of Patent: March 22, 1988
    Assignee: Bristol Myers Company
    Inventor: Choung U. Kim
  • 3,3-neotrehalosadiamine antibiotic and producing it with novel microorganism
    Patent number: 4732976
    Abstract: 3,3'-Neotrehalosadiamine antibiotic is prepared by fermentation of B. pumilus K169-B91 (ATCC No. 53206) in a nutrient medium preferably comprising soybean meal, corn starch, calcium carbonate and magnesium sulfate. The antibiotic and pharmaceutically acceptable salts and hydrates thereof and compositions containing these are useful to treat bacterial infections in mammals.
    Type: Grant
    Filed: December 9, 1985
    Date of Patent: March 22, 1988
    Assignee: Bristol-Myers Company
    Inventors: Takashi Tsuno, Masataka Konishi
  • Lipoxygenase inhibitory phenylalkanohydroxamic acids
    Patent number: 4731382
    Abstract: Compounds of the formula ##STR1## where n=6-11 and M is hydrogen or a pharmaceutically acceptable cation are potent inhibitors of 5-lipoxygenase.
    Type: Grant
    Filed: December 29, 1986
    Date of Patent: March 15, 1988
    Assignee: Bristol-Myers Company
    Inventors: Fred C. Zusi, Suresh A. Marathe, Kenneth M. Tramposch
  • Boxazomycin A and B, new antibiotics containing benzoxazole nucleus
    Patent number: 4728612
    Abstract: The novel antibiotics boxazomycin A and B, which have the formula: ##STR1## wherein R is --CH.sub.2 OH for boxazomycin A; and R is --CH.sub.3 for boxazomycin B. These new antibiotics, which are produced by cultivating a novel strain of Pseudonocardia (ATCC 53205), inhibit growth of aerobic Gram-positive bacteria and anaerobes with enhanced activity observed in acidic medium.
    Type: Grant
    Filed: July 25, 1986
    Date of Patent: March 1, 1988
    Assignee: Bristol Myers Company
    Inventors: Kyoichiro Saitoh, Masataka Konishi, Koji Tomita
  • Carbapenem antibiotics
    Patent number: 4710568
    Abstract: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups and ##STR2## represents a quaternized nitrogen-containing aromatic heterocycle. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives and novel intermediates utilized in these processes.
    Type: Grant
    Filed: October 30, 1986
    Date of Patent: December 1, 1987
    Assignee: Bristol-Myers Company
    Inventors: Choung Un. Kim, Peter F. Misco, Jr.
  • Antitumor antibiotic complex
    Patent number: 4708872
    Abstract: A novel antibiotic complex designated herein as BBM-1675 complex is produced by fermentation of certain novel strains of Actinomadura verrucosospora. The complex may be separated into two major components, BBM-1675 A.sub.1 and A.sub.2, and four minor components, BBM-1675 A.sub.3, A.sub.4, B.sub.1 and B.sub.2, and such components exhibit both antimicrobial activity and antitumor activity.
    Type: Grant
    Filed: December 23, 1985
    Date of Patent: November 24, 1987
    Assignee: Bristol-Meyers Company
    Inventors: Masataka Konishi, Kyoichiro Saitoh, Hiroaki Ohkuma, Hiroshi Kawaguchi
  • Trichloroethanimidic acid esters
    Patent number: 4692538
    Abstract: New and more efficient chemical processes are provided for preparing (.alpha.S, 5S)-.alpha.-amino-3-chloro-2-isoxazoline-5-acetic acid (AT-125), (.alpha.S, 5S)-.alpha.-amino-3-bromo-2-isoxazoline-5-acetic acid (bromo AT-125) and the C-5 epimers thereof. The disclosed processes allow the above-mentioned antitumor agents to be produced in high yield and purity with substantially fewer steps than prior art chemical procedures.
    Type: Grant
    Filed: May 28, 1985
    Date of Patent: September 8, 1987
    Assignee: Bristol-Myers Company
    Inventors: Dolatrai M. Vyas, Terrence W. Doyle, Yulin Chiang
  • Peptide antibiotics
    Patent number: 4692510
    Abstract: Novel peptides of the formula ##STR1## wherein R is CH.sub.3 --(CH.sub.2).sub.6, CH.sub.3 --(CH.sub.2).sub.4 --CH.dbd.CH--(CH.sub.2).sub.2 and CH.sub.3 (CH.sub.2).sub.8 having antibiotic and antitumor activity are prepared by cultivation of the novel microorganism Polyangium brachysporum. Enzymatic hydrolysis of those peptides gives other peptides useful as intermediates in the preparation of peptides having activity as antibiotics and/or antitumor agents.
    Type: Grant
    Filed: April 25, 1986
    Date of Patent: September 8, 1987
    Assignee: Bristol-Myers Company
    Inventors: Masataka Konishi, Koji Tomita, Masahisa Oka, Ken-ichi Numata
  • Boxazomycin A and B, new antibiotics containing benzoxazole nucleus
    Patent number: 4690926
    Abstract: The novel antibiotics boxazomycin A and B, which have the formula: ##STR1## wherein R is --CH.sub.2 OH for boxazomycin A; and R is --CH.sub.3 for boxazomycin B. These new antibiotics, which are produced by cultivating a novel strain of Pseudonocardia (ATCC 53205), inhibit growth of aerobic Gram-positive bacteria and anaerobes with enhanced activity observed in acidic medium.
    Type: Grant
    Filed: February 3, 1986
    Date of Patent: September 1, 1987
    Assignee: Bristol-Myers Company
    Inventors: Kyoichiro Saitoh, Masataka Konishi, Koji Tomita
  • Carbapenem intermediates
    Patent number: 4683296
    Abstract: A new process is provided for preparing the key carbapenem intermediates of the formula ##STR1## wherein R.sup.5 and R.sup.6 each independently represent hydrogen or methyl and R.sub.1 represents a conventional carboxyl-protecting group.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: July 28, 1987
    Assignee: Bristol-Myers Company
    Inventors: Yasutsugu Ueda, Guy Roberge
  • BMY-28121, a new antitumor antibiotic
    Patent number: 4683230
    Abstract: A new antitumor antibiotic designated herein as BMY-28121 is produced by fermentation of Streptomyces albus strain K731-113 (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.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: July 28, 1987
    Assignee: Bristol-Myers Company
    Inventors: Mitsuaki Tsunakawa, Masataka Konishi, Takeo Miyaki