Patents Represented by Attorney Bruce Stein

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  • Imidazo[1,5-A]quinoxalines
    Patent number: 5541324
    Abstract: An invention relating to Imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group and which are useful as anxiolytic and sedative/hypnotic agents.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: July 30, 1996
    Assignee: The Upjohn Company
    Inventors: Ruth E. TenBrink, E. Jon Jacobsen, Ronald B. Gammill
  • Imidazolylpiperazinyl steroids
    Patent number: 5506354
    Abstract: Disclosed are amino substituted steroids (XI) which contain an imidazolylpiperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: December 1, 1992
    Date of Patent: April 9, 1996
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
  • Pharmaceutically active bicyclic-heterocyclic amines
    Patent number: 5502187
    Abstract: The pharmaceutically active bicyclic heterocyclic amines (XXX) ##STR1## where W.sub.1 is --N.dbd. or --CH.dbd.; W.sub.3 is --N.dbd. or --CH.dbd.; W.sub.5 is --N.dbd. or --CR.sub.5 -- with the proviso that W.sub.5 is --CR.sub.5 -- when both W.sub.1 and W.sub.3 are --N.dbd. which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.
    Type: Grant
    Filed: October 3, 1994
    Date of Patent: March 26, 1996
    Assignee: The Upjohn Company
    Inventors: Donald E. Ayer, Gordon L. Bundy, Eric J. Jacobsen
  • Anti-aids piperazines
    Patent number: 5489593
    Abstract: The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (V) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: February 6, 1996
    Assignee: The Upjohn Company
    Inventors: John R. Palmer, Paul A. Aristoff, Donna L. Romero
  • Amines to sensitize multidrug-resistant cells
    Patent number: 5436337
    Abstract: The sensitizing amines of the present invention, illustrated by the steroidal amines (I) ##STR1## the alkyl amines (II), bicyclic amines (III), bicyclic ethers (IV), tricyclic compounds (V), indoles (VI) and various species are useful in treating individuals who have cancer has become resistant to cancer chemotherapeutic agents and in preventing the resistance from developing or slowing the rate of resistance to the chemotherapeutic agents.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: July 25, 1995
    Assignee: The Upjohn Company
    Inventors: Irene Abraham, Jackson B. Hester, Jr.
  • 9.alpha.-dehalogenation process
    Patent number: 5426198
    Abstract: The present invention involves improved processes for the dehalogenation of 9.alpha.-halosteroids (I) ##STR1## to produce the corresponding 11.beta.-hydroxy steroids (II) ##STR2## which are known to be useful as pharmaceutical, where the improvements comprise (1) adding the 9.alpha.-halo steroid (I) to the chromium and (2) using catalytic amounts of chromium in the presence of a means of converting chromium (II) to chromium (III).
    Type: Grant
    Filed: January 31, 1990
    Date of Patent: June 20, 1995
    Assignee: The Upjohn Company
    Inventors: Joel E. Huber, Jeffrey A. Fleming
  • Bisphosphonic acid derivatives as anti-arthritic agents
    Patent number: 5412141
    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 anti-arthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: May 2, 1995
    Assignee: The Upjohn Company
    Inventor: Richard A. Nugent
  • Oxidative preparation of 3,5-secoandrost-5-one-3,17 .beta.-dioic acid
    Patent number: 5405978
    Abstract: The present invention is an oxidative process for the conversion of 21-unsaturated progesterones (I) ##STR1## to the corresponding 3,5-secoandrost-5-one-3,17.beta.-dioic acids (II) ##STR2## by use of either ozone or an oxidizing agent, which are useful intermediates in the production of .DELTA..sup.5 -4-aza-17-carbonyl steroids (III) which are useful in production of 5.alpha.-4-aza amide (IV) pharmaceuticals. Also disclosed are the novel 21-unsaturated progesterones (I-C) and 3,5-secoandrost-5-one-3,17.beta.-dioic acids (II-C).
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: April 11, 1995
    Assignee: The Upjohn Company
    Inventor: Paul M. Herrinton
  • Microbial degradation of chemical pollutants
    Patent number: 5399495
    Abstract: Disclosed is a biologically pure culture of Aureobasidium pullmans deposited as NRRL 21064. Further disclosed are processes for decreasing the concentration of a type A/B chemical pollutants in an aqueous mixture containing the type A/B chemical pollutant which comprises adding sufficient amount of a fungal cyclic ether degrading microorganism to the aqueous mixture containing the chemical pollutant in the presence of a sufficient amount of cometabolite (type A chemical pollutant; not needed with type B) and a sufficient amount of oxygen.
    Type: Grant
    Filed: April 28, 1993
    Date of Patent: March 21, 1995
    Assignee: The Upjohn Company
    Inventors: Tom E. Patt, Haile M. Abebe
  • Pyrazinylpiperazinyl steroids
    Patent number: 5382661
    Abstract: Disclosed are amino substituted steroids (XI) which contain a pyrazinylpiperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: December 1, 1992
    Date of Patent: January 17, 1995
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Pyridinylpiperazinyl steroids
    Patent number: 5380841
    Abstract: Disclosed are amino substituted steroids (XI) which contain a pyridinylpiperazinyl group group attached to the terminal carbon atom of the C.sub.17 -side chain of the steroid which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: December 1, 1992
    Date of Patent: January 10, 1995
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
  • Triazinylpiperazinyl steroids
    Patent number: 5380840
    Abstract: Disclosed are amino substituted steroids (XI) which contain 4-[1,3,5-triazin-2-yl]- or 4-[1,2,4-triazin-3-yl]- 1-piperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: December 1, 1992
    Date of Patent: January 10, 1995
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. Van Doornik, John R. Palmer, Harold A. Karnes
  • Phenylpiperazinyl steroids
    Patent number: 5380839
    Abstract: Disclosed are amino substituted steroids (XI) which contain a phenylpiperazinyl group attached to the terminal carbon atoms of the C.sub.17 -side chain, which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: December 1, 1992
    Date of Patent: January 10, 1995
    Assignee: The Upjohn Company
    Inventors: John M. McCall, E. Jon Jacobsen, Frederick J. VanDoornik
  • Piperazine compounds which are substituted
    Patent number: 5322943
    Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: August 26, 1991
    Date of Patent: June 21, 1994
    Assignee: The Upjohn Company
    Inventors: John M. McCall, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Triazinylpiperazinyl amine intermediates
    Patent number: 5268477
    Abstract: The claimed invention is to triazin-2-yl and triazin-3-yl piperazines which are useful intermediates in the preparation of amino substituted steroid (XI) which are useful pharmaceutical agents.
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: December 7, 1993
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
  • Method for rapid in vivo assessment of intravenous irritation of pharmaceutical compositions
    Patent number: 5266301
    Abstract: The present invention is a method for rapid in vivo assessment of intravenous irritation of pharmaceutical compositions. The assessment of the vascular irritability of new pharmaceutical agents, vehicles and their pharmaceutical compositions has traditionally been limited to histological characterization of postinfusion damage. These studies utilized about 15 conscious animals and required about two weeks to complete. The method of the present invention in contrast utilizes fewer animals and can be completed in as short as only about 2-4 hr. In addition the direct observation is contemporaneous with the infusion and utilized a central vein.
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: November 30, 1993
    Assignee: The Upjohn Company
    Inventors: Ricardo Ochoa, Bruce C. Graves
  • Tricyclic [6,6,5]-fused oxazolidinone antibacterial agents
    Patent number: 5247090
    Abstract: The present invention involves tricyclic-fused 6-member ring oxazolidinones ##STR1## which are useful as antibacterial agents.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: September 21, 1993
    Assignee: The Upjohn Company
    Inventor: Steven J. Brickner
  • Tricyclic [6.5.51]-fused oxazolidinone antibacterial agents
    Patent number: 5231188
    Abstract: The present invention involves tricyclic-fused 6-member ring oxazolidinones ##STR1## and tricyclic-fused 5-member ring oxazolidinones ##STR2## which are useful as antibacterial agents.
    Type: Grant
    Filed: May 13, 1992
    Date of Patent: July 27, 1993
    Assignee: The Upjohn Company
    Inventor: Steven J. Brickner
  • 1,2-dehydrogenation of steroidal 21-esters with Arthrobacter simplex or Bacterium cyclooxydans
    Patent number: 5225335
    Abstract: The present invention involves processes for 1,2-dehydrogenation of .DELTA..sup.4 -3-keto C.sub.21 -hemiester steroids of formula (I) ##STR1## with Arthrobacter simplex or Bacterium cyclooxydans to produce the corresponding .DELTA..sup.1,4 -3-keto C.sub.21 hemiester of formula (II) ##STR2## or free alcohol thereof with improved yields. The advantage is that the processes utilize higher substrate concentrations and give shorter reaction times than previously were known.
    Type: Grant
    Filed: September 12, 1989
    Date of Patent: July 6, 1993
    Assignee: The Upjohn Company
    Inventors: Leo A. Kominek, Holly J. Wolf, Paula S. Steiert
  • Amines useful in producing pharmaceutically active CNS compounds
    Patent number: RE35053
    Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: October 10, 1995
    Assignee: The Upjohn Company
    Inventors: John M. McCall, E. Jon Jacobsen