Patents by Inventor Byron H. Arison

Byron H. Arison has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5250422
    Abstract: Incubation of 13.beta.-hydroxy ivermectin aglycone with a species of Bacillus subtilis or the incubation of 13-deoxy ivermectin aglycone with a mixed culture of a species of Bacillus subtilis and of Streptomyces griseus results in the production of 13-.beta. ivermectin monoglucopyranoside as the major product and of 5-.beta. ivermectin monoglucopyranoside as the minor product.
    Type: Grant
    Filed: May 11, 1992
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Brian R. Petuch, Edward S. Inamine, Shieh-Shung T. Chen, Raymond F. White, Byron H. Arison
  • Patent number: 5225403
    Abstract: Described is a process for producing a new FK-506 antagonist agent, a C-21 hydroxylated analog of FR-900520 under novel fermentation conditions utilizing the novel microorganism, Streptomyces hygroscopicus (Merck Culture Collection MA 6832) ATCC No. 55166. The macrolide antagonist is useful in preventing and/or counteracting accidental or inadvertent FK-506 overdosage in an FK-506 therapeutic program designed to prevent autoimmune diseases or human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
    Type: Grant
    Filed: June 25, 1991
    Date of Patent: July 6, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Laszlo R. Treiber, Georgette Dezeny, Lawrence F. Colwell, Jr., Byron H. Arison, Francis Dumont
  • Patent number: 5221625
    Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6963) ATCC No. 55230. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
    Type: Grant
    Filed: January 10, 1992
    Date of Patent: June 22, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Raymond F. White, Georgette Dezeny, Brian R. Petuch, George M. Garrity, Byron H. Arison, Amy M. Bernick
  • Patent number: 5219985
    Abstract: A compound having the formula ##STR1## and a method of obtaining said compound is described. The compound has antifungal properties.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: June 15, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Brian R. Petuch, Byron H. Arison
  • Patent number: 5215894
    Abstract: The present invention is concerned with a novel biotransformation process for producing 17.beta.-N-monosubstituted carbamoyl-11-oxo-4-aza-5-.alpha.-androst-3-ones of the formula: ##STR1## These compounds are testosterone 5-.alpha. reductase inhibitors and are produced via a claimed novel biotransformation process using the green algae, Selenastrum capricornutum.
    Type: Grant
    Filed: February 25, 1992
    Date of Patent: June 1, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Josephine R. Carlin, Edamanal S. Venkataramani
  • Patent number: 5210030
    Abstract: Described is a new process for selectively acylating FK-506 type immunosuppressant macrolides, including immunomycin (FK-520), in the C-32 position, under novel conditions utilizing an immobilized lipase enzyme, an acyl donor, and a dry, non hydroxylic organic solvent. The enzyme is absorbed onto a solid support and the enzyme/support catalyzes the C-32 acylation. The enzyme/support complex can then be filtered from the reaction mixture and, recycled for use.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: May 11, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Brian R. Petuch, Shieh-shung T. Chen, Byron H. Arison
  • Patent number: 5202258
    Abstract: Described is a new microorganism, Actinoplanacete sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The microorganism acts as a demethylating agent and can produce the new immunosuppressants, "demethomycin" (L-682,993) a C-31 demethylated analog of L-679,934, and "demethimmunomycin" (L-683,742) a C-31 demethylated analog of L-683,590, under novel fermentation conditions. These macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: April 13, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Byron H. Arison, George M. Garrity, Edward S. Inamine, Sagrario Mochales, Linda S. Wicker
  • Patent number: 5192671
    Abstract: Avermectin compounds are glycosylated the 4' and 4"-positions by adding the avermectin compounds to the fermentation medium of Saccharapolyspora erythrea. The outer oleandrose sugar group of the avermectin compound is glycosylated with a glycosyl moiety, specifically a glucose group. In addition, other changes are effected in the avermectin moiety such as selective hydroxylation, epimerization at the 2-carbon and migration of the .DELTA. 3-double bond to a .DELTA. 2-position.
    Type: Grant
    Filed: June 26, 1991
    Date of Patent: March 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Marvin D. Schulman, Patrick J. Doherty
  • Patent number: 5192668
    Abstract: A dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: February 27, 1992
    Date of Patent: March 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Laszlo R. Treiber, Lawrence F. Colwell, Jr., Byron H. Arison, Georgette Dezeny, Russell B. Lingham, Wayne J. Thompson, Suresh K. Balani
  • Patent number: 5187074
    Abstract: A novel dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: February 20, 1992
    Date of Patent: February 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Laszlo R. Treiber, Russell B. Lingham, Byron H. Arison, Lawrence F. Colwell, Jr., Georgette Dezeny, Nancy E. Kohl
  • Patent number: 5169769
    Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation products the 6-hydroxymethyl and 5-(1-hydroxy)ethyl anologs. These products are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.
    Type: Grant
    Filed: June 7, 1991
    Date of Patent: December 8, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Suresh K. Balani, Byron H. Arison, Harri G. Ramjit, Anthony D. Theoharides, Laura R. Kauffman
  • Patent number: 5149701
    Abstract: Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated devivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
    Type: Grant
    Filed: August 1, 1991
    Date of Patent: September 22, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Ali Shafiee, Louis Kaplan, Shieh-Shung T. Chen, Byron H. Arison, Lawrence F. Colwell, Jr., Francis Dumont
  • Patent number: 5140042
    Abstract: Fermentation of S. erythraea produces the novel avermectin, 28-hydroxy ivermectin aglycone.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: August 18, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Marvin D. Schulman, Patrick J. Doherty
  • Patent number: 5138052
    Abstract: Described is a new L-679,934 (FK-506) antagonist, L-686,292, a C-15, C-31 bisdemethylated, derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide reverses the immunosuppressant action of L-679,934 (FK-506), and can be used diagnostically as a tool to determine the presence of FK-506 macrolide type immunosuppressants in natural product broths, distinguishing such immunosuppressants from other chemical families such as the cycloporins.
    Type: Grant
    Filed: March 5, 1991
    Date of Patent: August 11, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Linda S. Wicker, Byron H. Arison
  • Patent number: 5124258
    Abstract: Fermentation of S. erythraea produces the novel avermectin, 28-hydroxy ivermectin aglycone.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: June 23, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Patrick J. Doherty, Marvin D. Schulman
  • Patent number: 5087702
    Abstract: Fermentation of the microorganism Streptomyces sp. (MA6750) ATCC No. 55042 in the presence of the Angiotensin II (A II) receptor antagonist of the following structure: ##STR1## yields an analog having a shikimate sugar-like moiety attached to the tetrazole, the said analog which is also an A II antagonist useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II angatonists.
    Type: Grant
    Filed: January 30, 1991
    Date of Patent: February 11, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Byron H. Arison, Raymond F. White, Edward S. Inamine
  • Patent number: 5068323
    Abstract: Ring-expanded macrolides related to FK-506 have immunosuppressive activity.
    Type: Grant
    Filed: April 10, 1990
    Date of Patent: November 26, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Matthew J. Wyvratt, Jr., Thomas R. Beattie, Hyun Ok, Byron H. Arison, Michael H. Fisher
  • Patent number: 5057608
    Abstract: Ring-expanded, immunosuppressive macrolides, are produced by heating and rearranging FK-506 and related compounds.
    Type: Grant
    Filed: April 10, 1990
    Date of Patent: October 15, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Matthew J. Wyvratt, Jr., Thomas R. Beattie, Hyun O. Ok, Byron H. Arison, Michael H. Fisher
  • Patent number: 5053329
    Abstract: Novel biotransformation compounds I and II are prepared by fermenting 3-[(2'-tetrazol-5-yl-biphenyl-4-yl)methyl]-7-methyl-2-propyl-3H-imidazo[4, 5-b]pyridine in a culture of Actinoplanacete sp., Accession No. ATCC 53771.
    Type: Grant
    Filed: April 1, 1991
    Date of Patent: October 1, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Byron H. Arison
  • Patent number: 5049565
    Abstract: Fermentation of the microorganism Streptomyces sp. (MA6750) ATTC No. 55042 in the presence of the Angiotensin II (A II) receptor antagonist ##STR1## yields three analogs, each having a shikimate sugar-like moiety attached to the tetrazole, which are also A II antagonists useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.
    Type: Grant
    Filed: December 7, 1990
    Date of Patent: September 17, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Raymond F. White, Byron H. Arison