Patents Represented by Attorney Bruce Stein

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  • Debromination
    Patent number: 4325881
    Abstract: A process for 9.alpha.-debromination of 9.alpha.-bromo-11.beta.-hydroxy steroids without eliminating the 11.beta.-hydroxyl group utilizing chromous chloride or chromous sulfate and thioglycolic acid.
    Type: Grant
    Filed: May 15, 1981
    Date of Patent: April 20, 1982
    Assignee: The Upjohn Company
    Inventors: James B. Heather, David R. White
  • 9.beta.,11.beta.-Epoxy-5.beta.-corticoids
    Patent number: 4318853
    Abstract: 17.alpha.-Acyloxy-5.alpha.-pregnanes (I) and 17.alpha.-acyloxy-5.alpha.-pregnanes (IV) have an excellent activity split providing high topical anti-inflammatory activity with very low systemic side effects.
    Type: Grant
    Filed: January 31, 1980
    Date of Patent: March 9, 1982
    Assignee: The Upjohn Company
    Inventors: Donald E. Ayer, Carl A. Schlagel
  • 9.alpha.-Debromination
    Patent number: 4304727
    Abstract: A process for 9.alpha.-debromination of 9.alpha.-bromo-11.beta.-hydroxy steroids without eliminating the 11.beta.-hydroxyl group utilizing chromous chloride or chromous sulfate and thioglycolic acid.
    Type: Grant
    Filed: December 5, 1980
    Date of Patent: December 8, 1981
    Assignee: The Upjohn Company
    Inventors: James B. Heather, David R. White
  • Allylic methyl-hydroxylated novobiocins
    Patent number: 4304855
    Abstract: The present invention relates to a fermentation process for producing allylic methyl-hydroxylated novobiocin and derivatives thereof.
    Type: Grant
    Filed: May 5, 1977
    Date of Patent: December 8, 1981
    Assignee: The Upjohn Company
    Inventors: Oldrich K. Sebek, Lester A. Dolak
  • Male contraceptive steroids and methods of use
    Patent number: 4297350
    Abstract: The steroids of the present invention have been found to be useful as male contraceptives when administered orally. Upon cessation of administration of the male contraceptive steroids of the present invention the male promptly regains normal fertility.
    Type: Grant
    Filed: October 10, 1978
    Date of Patent: October 27, 1981
    Assignee: The Upjohn Company
    Inventors: John C. Babcock, J. Allan Campbell, Thomas J. Lobl
  • Process to prepare metalated olefins
    Patent number: 4284827
    Abstract: Substituted ethanes (I) are reacted with an alkyl metal reagent to form isomeric metalated olefins (IIIA and IIIB) having a trans (IIIB) to cis (IIIA) ratio of greater than 70:30.
    Type: Grant
    Filed: December 17, 1979
    Date of Patent: August 18, 1981
    Assignee: The Upjohn Company
    Inventor: Jerry A. Walker
  • Bisnoraldehyde-22-enamine process
    Patent number: 4257949
    Abstract: A process which produces bisnoraldehyde-22-enamines in high yield and sufficiently high purity for copper-catalyzed oxygenation by the process of U.S. Pat. No. 3,661,942 has been developed.
    Type: Grant
    Filed: October 22, 1979
    Date of Patent: March 24, 1981
    Assignee: The Upjohn Company
    Inventor: John M. Beaton
  • 6-Deoxyneamines
    Patent number: 4252970
    Abstract: 6-Deoxyneamine, 6-deoxy-5-epineamine, their 5-0-glycosyl derivatives, 6-deoxy-5-oxoneamine and the derivatives therefrom are useful as antibacterial agents and/or as intermediates in the synthesis of antibacterially active 6-deoxyneamines.
    Type: Grant
    Filed: March 5, 1979
    Date of Patent: February 24, 1981
    Assignee: The Upjohn Company
    Inventor: Barney J. Magerlein
  • Reversible male contraception
    Patent number: 4252798
    Abstract: Various steroids which have a high affinity for rat ABP (androgen binding protein) and a low affinity for rat AR (androgen receptor) have been found to be useful as male contraceptives. Upon cessation of administration of the steroids of the present invention the male promptly regains normal fertility.
    Type: Grant
    Filed: February 14, 1980
    Date of Patent: February 24, 1981
    Assignee: The Upjohn Company
    Inventor: Donald J. Tindall
  • Piperazinone and piperazine polypeptides
    Patent number: 4251438
    Abstract: Piperazinone polypeptides which are useful as analgesics and psychotherapeutic agents as well as processes to produce them are described.
    Type: Grant
    Filed: June 14, 1979
    Date of Patent: February 17, 1981
    Assignee: The Upjohn Company
    Inventor: Malcolm W. Moon
  • 6-Deoxyneamines
    Patent number: 4232148
    Abstract: 6-Deoxyneamine, 6-deoxy-5-epineamine, their 5-0-glycosyl derivatives, 6-deoxy-5-oxoneamine and the derivatives therefrom are useful as antibacterial agents and/or as intermediates in the synthesis of antibacterially active 6-deoxyneamines.
    Type: Grant
    Filed: March 5, 1979
    Date of Patent: November 4, 1980
    Assignee: The Upjohn Company
    Inventor: Barney J. Magerlein
  • Synthesis of 16-unsaturated pregnanes from 17-keto steroids
    Patent number: 4216159
    Abstract: 17-Keto steroids (I) in their protected form (IIa or IIb) are reacted with a metalated olefin (VI) to give a 21-aldehyde (IV) which is readily transformed to a 16-unsaturated pregnane (V) which is useful in the production of commercially important substituted corticoids.
    Type: Grant
    Filed: May 25, 1978
    Date of Patent: August 5, 1980
    Assignee: The Upjohn Company
    Inventors: Edward J. Hessler, Verlan H. VanRheenen
  • Spironolactone process
    Patent number: 4211701
    Abstract: Spironolactone (VIII) is produced from ethisterone (I) by formation of the lactone (IV), a halo lactone (VI) and a .DELTA.4,6-lactone (VII).
    Type: Grant
    Filed: April 13, 1979
    Date of Patent: July 8, 1980
    Assignee: The Upjohn Company
    Inventor: Joseph M. Timko
  • Epoxide process
    Patent number: 4189430
    Abstract: 11.beta.,21-Dihydroxypregna-1,4,17(20)-triene-3-one 21-acetate (0) is epoxidized, followed by ring opening and hydrolysis to give 11.beta.,20,21-trihydroxypregna-1,4,16-triene-3-one 21-acetate (III), an intermediate in the synthesis of betamethasone, in improved yields.
    Type: Grant
    Filed: July 31, 1978
    Date of Patent: February 19, 1980
    Assignee: The Upjohn Company
    Inventor: Kenneth P. Shephard
  • Chemical oxidation of novobiocin and products obtained therefrom
    Patent number: 4169940
    Abstract: The present invention relates to processes for the chemical oxidation of novobiocin-type compounds (I) to their corresponding hydroxy derivative (II) or aldehyde (III) and formation of novobiocin derivatives from these oxidation products. The oxidation products and derivatives have antibacterial activity.
    Type: Grant
    Filed: February 15, 1978
    Date of Patent: October 2, 1979
    Assignee: The Upjohn Company
    Inventor: Lester A. Dolak
  • 6-Deoxyneamines aminoglycoside compounds
    Patent number: 4169197
    Abstract: 6-Deoxyneamine, 6-deoxy-5-epineamine, their 5-O-glycosyl derivatives, 6-deoxy-5-oxoneamine and the derivatives therefrom are useful as antibacterial agents and/or as intermediates in the synthesis of antibacterially active 6-deoxyneamines.
    Type: Grant
    Filed: March 13, 1978
    Date of Patent: September 25, 1979
    Assignee: The Upjohn Company
    Inventor: Barney J. Magerlein
  • Phosphate catalyzed acylation of steroidal tertiary alcohols
    Patent number: 4154748
    Abstract: The process of the invention permits acylation of hindered steroidal tertiary alcohols without the undesirable side reactions which accompany previously known acylation reactions.
    Type: Grant
    Filed: January 20, 1978
    Date of Patent: May 15, 1979
    Assignee: The Upjohn Company
    Inventors: Verlan H. Van Rheenen, James B. Heather
  • Allylic methyl-hydroxylated novobiocins
    Patent number: 4148992
    Abstract: The present invention relates to a fermentation process for producing allylic methyl-hydroxylated novobiocin and derivatives thereof. These hydroxy novobiocins (II) are useful as antibiotics.
    Type: Grant
    Filed: February 15, 1978
    Date of Patent: April 10, 1979
    Assignee: The Upjohn Company
    Inventors: Oldrich K. Sebek, Lester A. Dolak
  • Derivatives of novobiocin
    Patent number: 4147704
    Abstract: The present invention relates to processes for the chemical oxidation of novobiocin-type compounds (I) to their corresponding hydroxy derivative (II) or aldehyde (III) and formation of novobiocin derivatives from these oxidation products. The oxidation products and derivatives have antibacterial activity.
    Type: Grant
    Filed: February 15, 1978
    Date of Patent: April 3, 1979
    Assignee: The Upjohn Company
    Inventor: Lester A. Dolak
  • Allylic methyl-hydroxylated novobiocins
    Patent number: 4128563
    Abstract: The present invention relates to a fermentation process for producing allylic methyl-hydroxylated novobiocin and derivatives thereof.
    Type: Grant
    Filed: February 15, 1978
    Date of Patent: December 5, 1978
    Assignee: The Upjohn Company
    Inventors: Oldrich K. Sebek, Lester A. Dolak