Patents Represented by Attorney Bruce Stein

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  • Alkyl substituted piperadinyl and piperazinyl anti-AIDS compounds
    Patent number: 5866589
    Abstract: Anti-AIDS compounds of formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are as defined in the specification and R.sub.8 is alkyl of substituted alkyl.
    Type: Grant
    Filed: June 9, 1997
    Date of Patent: February 2, 1999
    Assignee: Pharmacia & Upjohn Company
    Inventors: Donna L. Romero, Richard C. Thomas, Paul D. May, Toni-Jo Poel
  • Cosolvent parenteral formulation of tirilazad
    Patent number: 5858999
    Abstract: The invention is a cosolvent parenteral pharmaceutical formulation of a lazaroid and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: February 4, 1997
    Date of Patent: January 12, 1999
    Assignee: Pharmacia & Upjohn Company
    Inventors: Ching-Chiang Su, David S. Baker, Susan M. Machkovech
  • Process to prepare oxazolidinones
    Patent number: 5837870
    Abstract: The present invention includes processes for producing 5-hydroxymethyl substituted oxazolidinone alcohols (III) from carbamates (IIA) or a trifluoroacetamide (IIB) using a dihydroxy compound (I) or glycidol (IV) starting material and for the transformation of the hydroxymethyl substituted oxazolidinone alcohols (III) to the corresponding amino compounds, 5-aminomethyl substituted oxazolidinone amines (VII) which are acylated to form commercially useful antibacterial 5-acylamidomethyl substituted oxazolidinone (VIII).
    Type: Grant
    Filed: March 28, 1997
    Date of Patent: November 17, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Bruce A. Pearlman, William R. Perrault, Michael R. Barbachyn, Peter R. Manninen, Dana S. Toops, David J. Houser, Thomas J. Fleck
  • Process to produce midazolam
    Patent number: 5831089
    Abstract: The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.
    Type: Grant
    Filed: May 28, 1997
    Date of Patent: November 3, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventor: Joel E. Huber
  • Substituted heteroarylphenyloxazolidinones
    Patent number: 5801246
    Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 1, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Pyrimido?4,5-B!indoles
    Patent number: 5795986
    Abstract: The pyrimido?4,5-b!indoles (I) ##STR1## and lactams (XIII) of the invention are useful as pharmaceutical agents for a number of different indications.
    Type: Grant
    Filed: July 25, 1997
    Date of Patent: August 18, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Gordon L. Bundy, John R. Palmer
  • Substituted heteroarylphenyloxazolidinones
    Patent number: 5756732
    Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 26, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Antiparasitic paraherquamides
    Patent number: 5750695
    Abstract: The present invention includes various substituted and paraherquamides, exemplified by the 14-hydroxy-2-deoxoparaherquamide B of formula (XXV) which are useful as antiparasitic agents.
    Type: Grant
    Filed: March 21, 1997
    Date of Patent: May 12, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Byung H. Lee, Michael F. Clothier
  • Finely divided solid crystalline powders via precipitation into an anti-solvent
    Patent number: 5707634
    Abstract: The present invention is a process for producing a finely divided solid which comprises(1) dissolving the solid to be finely divided in a liquid carrier solvent to form an injection solution and(2) adding the injection solution of step (1) to a volume of anti-solvent sufficient to precipitate or crystallize the solid.The solid can be a pharmaceutical, agricultural chemical, commercial chemical, fine chemical, food item, photographic chemical, dye, explosive, paint, polymer or cosmetic.
    Type: Grant
    Filed: June 8, 1995
    Date of Patent: January 13, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventor: William J. Schmitt
  • Pyridyl piperazine compound
    Patent number: 5686610
    Abstract: Substituted indoles of formula (I) ##STR1## are useful anti-AIDS pharmaceuticals.
    Type: Grant
    Filed: September 10, 1996
    Date of Patent: November 11, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventor: John R. Palmer
  • 4,5-cyclicimidazo[1,5-A]quinoxalines
    Patent number: 5668282
    Abstract: The invention discloses imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group that are useful as anxiolytic and sedative/hypnotic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 16, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventor: Ruth E. TenBrink
  • Substituted heteroarylphenyloxazolidinones
    Patent number: 5654428
    Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difluorophenyl]-2-oxazolid inone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Substituted arylphenyloxazolindinones
    Patent number: 5654435
    Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difluorophenyl]-2-oxazolid inone.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Bisphosphonic acid derivatives as anti-arthritic agents
    Patent number: 5602115
    Abstract: The bisphosphonates of formula (III)R.sub.2 --X--(CW).sub.m1 --CR.sub.3 R.sub.4 --CH.sub.2 --CM[PO--(OR.sub.1).sub.2 ].sub.2 (III)bicyclic bisphosphonates (V), and cyclic bisphosphonates (VII) are useful as antiarthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.
    Type: Grant
    Filed: November 28, 1994
    Date of Patent: February 11, 1997
    Assignee: The Upjohn Company
    Inventor: Richard A. Nugent
  • Substituted indoles as anti-AIDS pharmaceuticals
    Patent number: 5599930
    Abstract: Substituted indoles of formula (I) ##STR1## are useful anti-AIDS pharmaceuticals.
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: February 4, 1997
    Assignee: The Upjohn Company
    Inventors: Donna L. Romero, Richard C. Thomas
  • Imidazo[1,5-A]quinolines for treatment of anxiety and sleep disorders
    Patent number: 5594140
    Abstract: Imidazo[1,5-a]quinolines of formula (I) which are useful pharmaceutical agents for the treatment of anxiety, sleep disorders, panic states, convulsions and muscle disorders.
    Type: Grant
    Filed: May 13, 1996
    Date of Patent: January 14, 1997
    Assignee: The Upjohn Company
    Inventors: Eric J. Jacobsen, Ruth E. TenBrink
  • 5,6-cyclicimidazo [1,5-a] Quinoxalines
    Patent number: 5574038
    Abstract: The invention discloses imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group that are useful as anxiolytic and sedative/hypnotic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 12, 1996
    Assignee: The Upjohn Company
    Inventor: E. Jon Jacobsen
  • Substituted aryl- and heteroaryl-phenyloxazolidinones
    Patent number: 5565571
    Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difiuorophenyl]-2-oxazolid inone.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: October 15, 1996
    Assignee: The Upjohn Company
    Inventors: Michael R. Barbachyn, Steven J. Brickner
  • Diaromatic substituted compounds as anti-HIV-1 agents
    Patent number: 5563142
    Abstract: The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: October 8, 1996
    Assignee: The Upjohn Company
    Inventors: John R. Palmer, Donna L. Romero, Paul A. Aristoff, Richard C. Thomas, Herman W. Smith
  • Imidazo?1,5-a!quinolines for treatment of anxiety and sleep disorders
    Patent number: RE35840
    Abstract: The present invention is to imidazo?1,5-a!quinolines (I) which are useful pharmaceutical agents for the treatment of anxiety, sleep disorders, panic states, convulsions and muscle disorders.
    Type: Grant
    Filed: June 17, 1997
    Date of Patent: July 7, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Eric Jon Jacobsen, Ruth Elizabeth TenBrink