Patents Represented by Attorney, Agent or Law Firm Aldo A. Algieri
  • Patent number: 4866189
    Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodoplyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)-alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.
    Type: Grant
    Filed: September 16, 1988
    Date of Patent: September 12, 1989
    Assignee: Bristol-Myers Company
    Inventors: Dolatrai M. Vyas, Paul M. Skonezny
  • Patent number: 4845248
    Abstract: There are disclosed intermediate which can be converted into podophyllotoxin and related compounds, which are known antineoplastic agents. There are also disclosed processes for the preparation of such intermediates, and processes for the conversion of the intermediates into known intermediates which are readily converted into podophyllotoxin and related compounds.
    Type: Grant
    Filed: December 7, 1987
    Date of Patent: July 4, 1989
    Assignee: Bristol-Myers Company
    Inventors: Takushi Kaneko, Henry S. L. Wong
  • Patent number: 4829073
    Abstract: The present invention provides a method for treating gastrointestinal motility disorders and thiadiazole oxide compounds for use in the method.
    Type: Grant
    Filed: May 12, 1988
    Date of Patent: May 9, 1989
    Assignee: Bristol-Myers Company
    Inventors: Jaswant S. Gidda, Ivo Monkovic
  • Patent number: 4824959
    Abstract: This invention provides novel intermediates of the formula ##STR1## in substantially the cis or cis-(4R,6S) form wherein R.sup.9 and R.sup.10 each are C.sub.1-4 alkyl or R.sup.9 and R.sup.10, taken together with the carbon atom to which they are attached, is cyclopentyl, cyclohexyl or cycloheptyl; andR.sup.12 is hydrogen, C.sub.1-4 alkyl or a metal cationand processes thereof which are useful for the preparation of antihypercholesterolemic agents.
    Type: Grant
    Filed: February 18, 1988
    Date of Patent: April 25, 1989
    Assignee: Bristol-Myers Company
    Inventors: William T. Han, John J. Wright
  • Patent number: 4814445
    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: February 25, 1988
    Date of Patent: March 21, 1989
    Assignee: Bristol-Myers Company
    Inventors: Dolatrai M. Vyas, Terrence W. Doyle, Richard A. Partyka
  • Patent number: 4795819
    Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.
    Type: Grant
    Filed: July 22, 1987
    Date of Patent: January 3, 1989
    Assignee: Bristol-Myers Company
    Inventors: Dolatrai M. Vyas, Paul M. Skonezny
  • Patent number: 4788184
    Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.
    Type: Grant
    Filed: November 13, 1987
    Date of Patent: November 29, 1988
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • Patent number: 4772704
    Abstract: Histamine H.sub.2 -antagonists of the formula: ##STR1## wherein m is an integer of from zero to 2, inclusive;n is an integer of from 2 to 5 inclusive;Z is sulfur, oxygen or methylene;R.sup.1 is NO.sub.2 or NR.sup.2 R.sup.3 ;R.sup.2 and R.sup.3 each are independently hydrogen or (lower)alkyl, or, when R.sup.2 is hydrogen, R.sup.3 also may be formyl, carboalkoxy, alkanoyl or benzoyl;A is phenyl, furyl, thienyl, pyridyl, thiazolyl, imidazolyl, oxazolyl, oxadiazolyl, thiadiazolyl, triazolyl, isoxazolyl, isothiazolyl, pyrimidinyl, pyrazolyl, pyridazinyl or pyrazinyl; provided that A contains one or two substituents, the first substituent being selected from ##STR2## and the second substituent being selected from (lower)alkyl, hydroxy, trifluoromethyl, halogen, amino, hydroxymethyl and (lower)alkoxy;q is an integer of from 0 to 6, inclusive;R.sup.
    Type: Grant
    Filed: September 21, 1983
    Date of Patent: September 20, 1988
    Assignee: Bristol-Myers Company
    Inventor: Aldo A. Algieri
  • Patent number: 4751295
    Abstract: 7-[2-(5-Amino-1,2,4-thiadiazol-3-yl)-2-(substituted)-iminoacetamido]-3-[3-( quaternaryammonio)-1-propen-1-yl]-3-cephem-4-carboxylates of the formula ##STR1## in which R.sup.1 and R.sup.2 are defined herein and --.sup..sym. N.tbd.Q is a quaternary ammonio group as defined herein, and salts, solvates, hydrates and esters thereof, are potent antibacterial agents. Processes for their preparation and intermediates in such processes are described.
    Type: Grant
    Filed: October 17, 1986
    Date of Patent: June 14, 1988
    Assignee: Bristol-Myers Company
    Inventors: Masahisa Oka, Haruhiro Yamashita, Jun Okumura, Takayuki Naito
  • Patent number: 4734512
    Abstract: There are disclosed intermediates which can be converted into podophyllotoxin and related compounds, which are known antineoplastic agents. There are also disclosed processes for the preparation of such intermediates, and processes for the conversion of the intermediates into known intermediates which are readily converted into podophyllotoxin and related compounds.
    Type: Grant
    Filed: December 5, 1985
    Date of Patent: March 29, 1988
    Assignee: Bristol-Myers Company
    Inventors: Takushi Kaneko, Henry S. L. Wong
  • Patent number: 4728740
    Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.
    Type: Grant
    Filed: September 15, 1986
    Date of Patent: March 1, 1988
    Assignee: Bristol-Myers Company
    Inventors: Dolatrai M. Vyas, Paul M. Skonezny
  • Patent number: 4714760
    Abstract: Stable, crystalline cephalosporin intermediates of the formula ##STR1## wherein X is HI or HCl and Nu and Nu.sup..sym. are certain N-containing heterocyclic rings attached via a sulfur atom or a ring nitrogen atom, respectively, which are substantially free of the .DELTA..sup.2 isomer; processes for, and intermediates in, the preparation of the above compounds; and processes for the preparation of broad-spectrum cephalosporin antibiotics.
    Type: Grant
    Filed: July 11, 1986
    Date of Patent: December 22, 1987
    Assignee: Bristol-Myers Company
    Inventors: Steven P. Brundidge, Paul R. Brodfuehrer, Chet Sapino, Jr., Kun M. Shih, Donald G. Walker
  • Patent number: 4692531
    Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.
    Type: Grant
    Filed: September 25, 1986
    Date of Patent: September 8, 1987
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • Patent number: 4659812
    Abstract: Temperature stable crystalline mono-hydrochloric and sulfuric acid addition salts of 7-amino-3-(1-methylpyrrolidinio)methyl-3-cephem-4-carboxylate substantially free of .DELTA..sup.2 isomer are intermediates for the preparation of broad spectrum 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(Z)-methoxyiminoacetamido]-3-[(1- methyl-1-pyrrolidinio)methyl]-3-cephem-4-carboxylates.
    Type: Grant
    Filed: August 20, 1985
    Date of Patent: April 21, 1987
    Assignee: Bristol-Myers Company
    Inventors: Shimpei Aburaki, Yukio Narita, Jun Okumura, Takayuki Naito, Donald G. Walker
  • Patent number: 4644006
    Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.
    Type: Grant
    Filed: June 22, 1984
    Date of Patent: February 17, 1987
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • Patent number: 4644072
    Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.
    Type: Grant
    Filed: April 12, 1985
    Date of Patent: February 17, 1987
    Assignee: Bristol-Myers Company
    Inventors: Dolatrai M. Vyas, Paul M. Skonezny
  • Patent number: 4599310
    Abstract: A new cyclic depsipeptide antitumor antibiotic designated herein as sandramycin is produced by fermentation of a new microorganism, Nocardioides sp. strain C49,009, ATCC 39419. Sandramycin possesses antibacterial activity and inhibits the growth of tumors in experimental animals.
    Type: Grant
    Filed: September 25, 1985
    Date of Patent: July 8, 1986
    Assignee: Bristol-Myers Company
    Inventors: James A. Matson, James A. Bush
  • Patent number: 4582639
    Abstract: A new cyclic depsipeptide antitumor antibiotic designated herein as sandramycin is produced by fermentation of a new microorganism, Nocardioides sp. strain C49,009, ATCC 39419. Sandramycin possesses antibacterial activity and inhibits the growth of tumors in experimental animals.
    Type: Grant
    Filed: June 18, 1984
    Date of Patent: April 15, 1986
    Assignee: Bristol-Myers Company
    Inventors: James A. Matson, James A. Bush
  • Patent number: 4546188
    Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers.
    Type: Grant
    Filed: October 3, 1984
    Date of Patent: October 8, 1985
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw