Patents Represented by Attorney H. G. Jackson
  • Patent number: 5877296
    Abstract: This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: March 2, 1999
    Assignee: American Cyanamid Company
    Inventors: Philip Ross Hamann, Lois Hinman, Irwin Hollander, Ryan Holcomb, William Hallett, Hwei-Ru Tsou, Martin J. Weiss
  • Patent number: 5773001
    Abstract: This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: June 30, 1998
    Assignee: American Cyanamid Company
    Inventors: Philip Ross Hamann, Lois Hinman, Irwin Hollander, Ryan Holcomb, William Hallett, Hwei-Ru Tsou, Martin J. Weiss
  • Patent number: 5767285
    Abstract: This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: June 16, 1998
    Assignee: American Cyanamid Company
    Inventors: Philip Ross Hamann, Lois Hinman, Irwin Hollander, Ryan Holcomb, William Hallett, Hwei-Ru Tsou, Martin J. Weiss
  • Patent number: 5606040
    Abstract: This disclosure describes disulfide analogs of the family of antibacterial and antitumor agents known collectively as the LL-E33288 complex.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: February 25, 1997
    Assignee: American Cyanamid Company
    Inventors: William J. McGahren, Martin L. Sassiver, George A. Ellestad
  • Patent number: 5461163
    Abstract: The invention relates to a process improvement for making [R-(R*,R*)]-5-[2-[5-(3-chlorophenyl)-2-oxo-3-oxazolidinyl]propyl]-1,3-benz odioxole-2,2-dicarboxylic acid dimethyl ester an intermediate used in the synthesis of beta-3 agonist, [R-(R*,R*)]-5-[2-[5-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benz odioxole-2,2-dicarboxylic acid disodium salt.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: October 24, 1995
    Assignee: American Cyanamid Company
    Inventors: Christine P. Bellon, David M. Blum, William T. Cain
  • Patent number: 5438148
    Abstract: The invention is the simultaneous addition of boron tribromide and a solution of [R-(R*,R*)]-5-(3-chlorophenyl-3-[2-(3,4-dimethoxyphenyl)-1-methylethyl]-2- oxazolidinone in methylene chloride to methylene chloride while maintaining a constant ratio of 2.10:1.00 of boron tribromide to the substrate [R-(R*,R*)]-5-(3-chlorophenyl-3-[2-(3,4-dimethoxyphenyl)-1-methylethyl]-2- oxazolidinone at a temperature of -5.degree. C. to 10.degree. C. gives [R-(R*,R*)]-5-(3-chlorophenyl-3-[2-(3,4-hydroxyoxyphenyl)-1-methylethyl]-2 -oxazolidinone in an isolated yield of 86.7% and a purity of 98.7%.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: August 1, 1995
    Assignee: American Cyanamid Company
    Inventors: Arthur G. Mohan, David M. Blum
  • Patent number: 5426108
    Abstract: This invention relates to antibiotic 31F508.alpha..sub.1 of the formula ##STR1## 31F508.alpha..sub.2, 31F508.beta..sub.1 and 31F508.beta..sub.2, derived from the microorganism Streptomyces viridodiastaticus subsp. "littus" which are useful as anti-bacterial agents.
    Type: Grant
    Filed: November 10, 1993
    Date of Patent: June 20, 1995
    Assignee: American Cyanamid Company
    Inventor: Joseph A. Zaccardi
  • Patent number: 5420291
    Abstract: The invention is a process improvement for producing [R-(R*, R*)]-5-(3-chlorophenyl)-3-[2-(3,4-dihydroxyphenyl)-1-methylethyl]-2-oxazol idinone which is an intermediate useful in making compounds that have antidiabetic and/or antihyperglycemic and/or antiobesity properties in mammals.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: May 30, 1995
    Assignee: American Cyanamid Company
    Inventors: William T. Cain, Kelvin Cruz, Kevin M. McCoy
  • Patent number: 5411983
    Abstract: The invention is a compound of R or S enantiomers or racemic mixtures of compounds of the formula: ##STR1## wherein: (A) X, Y, and R.sub.3 are as defined in the specification.
    Type: Grant
    Filed: July 28, 1993
    Date of Patent: May 2, 1995
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Robert E. Schaub, Phaik-Eng Sum
  • Patent number: 5373020
    Abstract: The present invention discloses substituted 1,3-benzodioxoles which possess anti-diabetic and/or anti-hyperglycemic and/or anti-obesity properties in humans and other animals.
    Type: Grant
    Filed: June 3, 1993
    Date of Patent: December 13, 1994
    Assignee: American Cyanamid Company
    Inventors: Jonathan D. Bloom, Thomas H. Claus, Vern G. DeVries, Jo A. Dolan, Minu D. Dutia
  • Patent number: 5366733
    Abstract: Oral compositions for the local administration of a therapeutic agent to a periodontal pocket of a patient for alleviating dental disease comprise a plurality of dry, discrete microparticles each of which comprise an effective amount of at least one therapeutic agent dispersed in a matrix comprising a biocompatible and biodegradable polymer. Apparatus and methods are also provided for the dispensing of the dry microparticles to the periodontal pocket whereby they become tacky and adhere to the involved tissue so as to induce long term therapeutic benefits.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: November 22, 1994
    Assignee: American Cyanamid Company
    Inventors: Nancy S. Brizzolara, Michael G. Lanzilotti, James R. Lawter
  • Patent number: 5328921
    Abstract: The invention is aryl, amide, imide and carbamate pyridine antagonists of platelet activating factor.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: July 12, 1994
    Assignee: American Cyanamid Company
    Inventors: Michael P. Trova, Allan Wissner
  • Patent number: 5328901
    Abstract: The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.
    Type: Grant
    Filed: June 1, 1993
    Date of Patent: July 12, 1994
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Kenneth Green, Robert E. Schaub
  • Patent number: 5283065
    Abstract: A controlled release pharmaceutical composition in oral dosage unit form comprising a tablet comprising a therapeutically effective number of active spherical granules comprising an effective amount of active medicament, a pharmaceutically acceptable normally solid diluent adapted to form a diffusable matrix for the active medicament and an optional pharmaceutically acceptable excipient; and a number of compressible spherical granules comprising a mono- or di-saccharide, an optional pharmaceutically acceptable normally solid diluent adapted to form a diffusable matrix, an optional active medicament and/or an optional pharmaceutically acceptable excipient wherein the average compressive yield of the compressible spherical granules is less than the average compressive yield of the active spherical granules is provided. A method for the preparation and for the administration of the above defined composition is provided as well.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: February 1, 1994
    Assignee: American Cyanamid Company
    Inventors: Daniel J. Doyon, Madurai G. Ganesan, Wendy A. Preston, Nitin V. Sheth
  • Patent number: 5245053
    Abstract: A process is disclosed for obtaining the R,R isomer of: ##STR1## wherein R.sub.1 and R.sub.2 may be one or more groups which may be the same or different and are selected from the group consisting of hydrogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, hydroxy, halogen, trifluoromethyl, carboxy, hydroxyalkyl, alkoxycarbonyl, C.sub.1 to C.sub.4 thioalkyl, sulfonyl and sulfinyl; X is a divalent radical consisting of ##STR2## wherein R' is hydrogen; R.sub.2 and R.sub.3 may be the same or different and are selected from the group consisting of hydrogen and C.sub.1 to C.sub.4 alkyl; R.sub.5 and R.sub.6 are selected from the group consisting of hydrogen, carboxy, alkoxycarbonyl, hydroxymethyl, --CH.sub.2 OCH.sub.2 COOR.sub.7 and --CH.sub.2 OCH.sub.2 CH.sub.2 OR.sub.7 where R.sub.7 is hydrogen or C.sub.1 to .sub.4 alkyl; except that R.sub.5 and R.sub.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: September 14, 1993
    Assignee: American Cyanamid Company
    Inventors: Jonathan D. Bloom, Thomas H. Claus, Vern G. Devries, Jo A. Dolan, Minu D. Dutia
  • Patent number: 5236355
    Abstract: Oral compositions for the local administration of a therapeutic agent to a periodontal pocket of a patient for alleviating dental disease comprise a plurality of dry, discrete microparticles each of which comprise an effective amount of at least one therapeutic agent dispersed in a matrix comprising a biocompatible and biodegradable polymer. Apparatus and methods are also provided for the dispensing of the dry microparticles to the periodontal pocket whereby they become tacky and adhere to the involved tissue so as to induce long term therapeutic benefits.
    Type: Grant
    Filed: October 5, 1990
    Date of Patent: August 17, 1993
    Assignee: American Cyanamid Company
    Inventors: Nancy S. Brizzolara, Michael G. Lanzilotti, James R. Lawter
  • Patent number: 5234918
    Abstract: The invention is a compound of R or S enantiomers or racemic mixtures of compounds of the formula: ##STR1## wherein: (A) is ##STR2## Y is (i) C.sub.1 -C.sub.24(ii) C.sub.1 -C.sub.24 alkoxy;(iii) C.sub.1 -C.sub.24 carboamoyloxy;Y is the divalent radical ##STR3## which are PAF inhibitors.
    Type: Grant
    Filed: September 23, 1991
    Date of Patent: August 10, 1993
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Robert E. Schaub, Phaik-eng Sum
  • Patent number: 5235037
    Abstract: The invention is an improvement in isolating vancomycin from an aqueous solution of pH 5 to 9 which comprises separating the vancomycin from the solution by adding an alkali or alkaline earth metal inorganic salt to the solution.
    Type: Grant
    Filed: August 15, 1991
    Date of Patent: August 10, 1993
    Assignee: American Cyanamid Company
    Inventor: Lalitha Krishnan
  • Patent number: 5231091
    Abstract: The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: July 27, 1993
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Kenneth Green, Robert E. Schaub
  • Patent number: 5219857
    Abstract: Novel compounds of the formula ##STR1## wherein n is an integer from 1 to 4 inclusive; R.sub.1 represents a mono-or disubstituent of hydrogen, lower alkyl(C.sub.1 -C.sub.3), lower alkoxy(C.sub.1 -C.sub.3), halogen, nitro or trifluoromethyl; R.sub.2 is cyano, carboxamido, ethyl carboxylate or halogen; R.sub.3 is hydrogen, straight or branched chain lower alkyl(C.sub.1 -C.sub.3), alkenyl(C.sub.2 -C.sub.3), alkynyl(C.sub.2 -C.sub.3), cycloalkyl(C.sub.3 -C.sub.6), hydroxyalkyl(C.sub.1 -C.sub.3), dimethylaminoalkyl(C.sub.1 -C.sub.3), ethylcarboxylate, alkyl(C.sub.1 -C.sub.13)carbonyl, 1-(methylethyl)acetamide, cyclohexylethyl, phenyl, mono-or disubstituted phenyl (wherein the phenyl substituent is halogen, trifluoromethyl, lower alkyl(C.sub.1 -C.sub.3) or lower alkoxy(C.sub.1 -C.sub.3)), benzyl, mono-or disubstituted benzyl (wherein the benzyl substituent is halogen, lower alkyl(C.sub.1 -C.sub.3), lower alkoxy(C.sub.1 -C.sub.3) or trifluoromethyl), benzoyl, 4-methoxybenzoyl, straight or branched chain alkyl(C.sub.
    Type: Grant
    Filed: April 15, 1992
    Date of Patent: June 15, 1993
    Assignee: American Cyanamid Company
    Inventors: Shin S. Tseng, Herbert J. Brabander, Joseph W. Epstein