Patents Represented by Attorney Bruce Stein

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  • Rubradirin treatment of methicillin-resistant staph
    Patent number: 4749568
    Abstract: It has been discovered that rubradirin can be used to treat rubradirin-sensitive, methicillin-resistant staphylococcal infections.
    Type: Grant
    Filed: January 23, 1987
    Date of Patent: June 7, 1988
    Assignee: The Upjohn Company
    Inventors: Fritz Reusser, Gary E. Zurenko, John H. Coats
  • 6'-thiomethylsubstituted spectinomycins
    Patent number: 4730059
    Abstract: Disclosed are 6'-thiomethylsubstituted spectinomycins (XII) which are useful in the same way as other spectinomycin pharmaceutical agents.6'-Thiomethylsubstituted (XIV) and protected spectinomycin (XIII) intermediates useful in the production of 6'-thiomethylsubstituted spectinomycins (XII) and 6'-alkenylspectinomycins (IX) are also disclosed.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: March 8, 1988
    Assignee: The Upjohn Company
    Inventor: David R. White
  • 16.alpha.-methylated.DELTA.17(20)-corticoids
    Patent number: 4704455
    Abstract: C.sub.16 -unsaturated corticoids are readily transformed to the corresponding 16.alpha.-methyl-17.alpha.-hydroxy corticoids by use of a .DELTA..sup.17 (.sup.20)-20-silyl ether.
    Type: Grant
    Filed: April 18, 1985
    Date of Patent: November 3, 1987
    Assignee: The Upjohn Company
    Inventors: Verlan H. VanRheenen, Joel E. Huber
  • .DELTA..sup.1 -dehydrogenation with heat or air-dried B. cyclooxidans
    Patent number: 4704358
    Abstract: Disclosed and claimed is an improved microbial bioconversion to produce 1,2-dehydro steroids from their corresponding 1,2-saturated derivatives.
    Type: Grant
    Filed: April 8, 1985
    Date of Patent: November 3, 1987
    Assignee: The Upjohn Company
    Inventors: Leo A. Kominek, Holly J. Wolf
  • Process for converting 1,2-saturated steroids to 1,2-dehydro steroids
    Patent number: 4684610
    Abstract: Disclosed and claimed is an improved microbial bioconversion to produce 1,2-dehydro steroids from their corresponding 1,2-saturated derivatives by use of a water-immiscible solvent comprising an aromatic hydrocarbon in the reaction procedure.
    Type: Grant
    Filed: April 17, 1985
    Date of Patent: August 4, 1987
    Assignee: The Upjohn Company
    Inventor: Timothy W. Evans
  • Process to prepare .alpha.-chloroalprazolam
    Patent number: 4663454
    Abstract: .alpha.-Halomethylbenzodiazepines (II) are produced by direct halogenation of methylbenzodiazepines (I) using sulfuryl halide.
    Type: Grant
    Filed: April 17, 1985
    Date of Patent: May 5, 1987
    Assignee: The Upjohn Company
    Inventor: Joel E. Huber
  • Ethynylation of 16-methyl-17-keto steroids
    Patent number: 4618456
    Abstract: The process of the present invention transforms 16.alpha.- or 16.beta.-methyl-17-keto steroids (I) to the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-16.alpha.- or 16.beta.-methyl steroids (II) without epimerization and loss of stereochemistry of the 16.alpha.- or 16.beta.-methyl group.
    Type: Grant
    Filed: April 26, 1984
    Date of Patent: October 21, 1986
    Assignee: The Upjohn Company
    Inventor: Joseph M. Timko
  • Ethynylation of 16-methylene-17-keto steroids
    Patent number: 4614621
    Abstract: The process of the present invention transforms 16-methylene-17-keto steroids (I) to the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-16-methylene steroids (II).
    Type: Grant
    Filed: April 20, 1984
    Date of Patent: September 30, 1986
    Assignee: The Upjohn Company
    Inventor: Verlan H. VanRheenen
  • Corticosteroids from 17-keto steroids via 20-cyano-.DELTA..sup.17 (.sup.20)-pregnanes
    Patent number: 4600538
    Abstract: The process of the present invention transforms 17-keto steroids (I) to the corresponding corticoids (IV) in three steps.
    Type: Grant
    Filed: August 2, 1984
    Date of Patent: July 15, 1986
    Assignee: The Upjohn Company
    Inventor: Jerry A. Walker
  • Piperazinone and piperazine polypeptides
    Patent number: 4593098
    Abstract: Piperazinone polypeptides which are useful as analgesics and psychotherapeutic agents as well as processes to produce them are described.
    Type: Grant
    Filed: May 27, 1980
    Date of Patent: June 3, 1986
    Assignee: The Upjohn Company
    Inventor: Malcolm W. Moon
  • Cyanohydrin process
    Patent number: 4585590
    Abstract: Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17.alpha.-acyl progesterones.
    Type: Grant
    Filed: January 30, 1985
    Date of Patent: April 29, 1986
    Assignee: The Upjohn Company
    Inventor: Verlan H. VanRheenen
  • 17.beta.-hydroxy-17.alpha.-methyl-5.alpha.-androstano[3,2-c]pyrazole 17-methyl ether
    Patent number: 4585765
    Abstract: 17.beta.-Hydroxy-17.alpha.-methyl-5.alpha.-androstano[3,2-c]pyrazole 17-methyl ether is a very potent reversible male contraceptive which has a very low degree of androgenic side effects. Upon cessation of administration fertility promptly returns.
    Type: Grant
    Filed: April 16, 1980
    Date of Patent: April 29, 1986
    Assignee: The Upjohn Company
    Inventors: Donald J. Tindall, Anthony R. Means
  • Epi-ethynylation process
    Patent number: 4582644
    Abstract: Ethynylation of 17-keto steroids (I) by standard means in the presence of a polar amine solvent produces the epi (17.beta.-ethynyl-17.alpha.-hydroxy) configuration at C.sub.17. The epi-ethisterone compounds are useful intermediates in the production of 17.alpha.-hydroxyprogesterones.
    Type: Grant
    Filed: November 21, 1984
    Date of Patent: April 15, 1986
    Assignee: The Upjohn Company
    Inventor: Jean R. Runge
  • .DELTA.16-20-Keto steroid conversion to 17.alpha.-hydroxy-20-keto steroids
    Patent number: 4568492
    Abstract: .DELTA.16-20-keto steroids (I) are converted to 17.alpha.-hydroxy-20-keto steroids (III) in 2 steps, hydrosilylation followed by peracid oxidation.
    Type: Grant
    Filed: September 14, 1984
    Date of Patent: February 4, 1986
    Assignee: The Upjohn Company
    Inventor: Jerry A. Walker
  • 11-Difluoromethylene steroids
    Patent number: 4567000
    Abstract: 11-Difluoromethylene steroids having progestational and anti-progestational properties, useful as anti-fertility agents, are disclosed as well as a process for making the 11-difluoromethylene steroids.
    Type: Grant
    Filed: August 31, 1984
    Date of Patent: January 28, 1986
    Assignee: The Upjohn Company
    Inventor: Donald E. Ayer
  • 16-Methylene-17.alpha.-hydroxy-progesterones
    Patent number: 4567001
    Abstract: 16-Methylene-17-keto steroids (III) are transformed to the corresponding 16-methylene-17.alpha.-hydroxyprogesterones (VII) which are intermediates useful in the production of betamethasone, diflorasone diacetate and melengesterol acetate.
    Type: Grant
    Filed: June 3, 1983
    Date of Patent: January 28, 1986
    Assignee: The Upjohn Company
    Inventor: Verlan H. VanRheenen
  • 11.beta.-Difluoromethyl and (E)- and (Z)-11-fluoromethylene steriods
    Patent number: 4557867
    Abstract: Known reactions are arranged in a novel manner to produce 11.beta.-difluoromethyl and (E)- and (Z)-11-fluoromethylene 19-norandrostenediones and 19-nor-13.beta.-ethylandrostenediones which are useful as contraceptive agents.
    Type: Grant
    Filed: August 8, 1984
    Date of Patent: December 10, 1985
    Assignee: The Upjohn Company
    Inventor: J. Allan Campbell
  • Cyanohydrin process
    Patent number: 4548748
    Abstract: Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17.alpha.-acyl progesterones.
    Type: Grant
    Filed: February 3, 1984
    Date of Patent: October 22, 1985
    Assignee: The Upjohn Company
    Inventor: Verlan H. Van Rheenen
  • Piperazinone, piperazine, 1,4-diazepin-2-one and 1,4-diazepine intermediate compounds
    Patent number: 4534897
    Abstract: The compounds of the following formulas ##STR1## where W is hydrogen, benzyloxycarbonyl, or t-butoxycarbonyl useful as intermediates for preparing piperazine, piperazinone, 1,4-diazepine and 1,4-diazepin-2-one polypeptide compound.
    Type: Grant
    Filed: April 10, 1984
    Date of Patent: August 13, 1985
    Assignee: The Upjohn Company
    Inventor: Malcolm W. Moon
  • Process for preparation of 16 .alpha.-methyl corticoids from .DELTA..sup.16 -steroids
    Patent number: 4530795
    Abstract: This invention discloses a general process for the production of corticoids from respective steroid-type compounds having a double bond from C-16 to C-17. The invention provides a viable alternative synthesis of 17.alpha.-hydroxy-progesterones and like corticoids.
    Type: Grant
    Filed: February 27, 1984
    Date of Patent: July 23, 1985
    Assignee: The Upjohn Company
    Inventor: Joel E. Huber