Patents Assigned to The Upjohn Company
  • Patent number: 4477684
    Abstract: The present invention provides a process for the preparation of 11.alpha.-alkylprostaglandin E compounds from corresponding prostaglandin A compounds via reaction with alkyllithium complexes, and novel 11-deoxy-11.alpha.-alkylprostaglandin E compounds useful for the same pharmacological purposes as the natural PGE compounds, e.g., antiulcer and antisecretory effects.
    Type: Grant
    Filed: June 23, 1982
    Date of Patent: October 16, 1984
    Assignee: The Upjohn Company
    Inventor: Gordon L. Bundy
  • Patent number: 4477442
    Abstract: A process for treating viral diseases in humans and animals which comprises administering a therapeutic amount of a compound of the formula ##STR1## the compounds are formulated with pharmaceutical carriers for systemic or local means of administration.
    Type: Grant
    Filed: November 5, 1980
    Date of Patent: October 16, 1984
    Assignee: The Upjohn Company
    Inventors: Harvey I. Skulnick, Harold E. Renis
  • Patent number: 4477468
    Abstract: A process for treating Herpes Type II virus by the systemic administration or topical application of flurbiprofen (3-fluoro-4-phenylhydratropic acid) or a salt or ester thereof. Dosage forms are also disclosed.
    Type: Grant
    Filed: December 6, 1982
    Date of Patent: October 16, 1984
    Assignee: The Upjohn Company
    Inventor: Jay W. Heckler
  • Patent number: 4476248
    Abstract: Ibuprofen is crystallized from a .delta.H.gtoreq.8 liquid such as a C.sub.1 to C.sub.3 -alkanol, e.g., methanol, containing solutions thereof to obtain ibuprofen crystals which are equant (cube, sphere or grain) in shape, which ibuprofen crystals have larger average partile size, higher bulk density, lower bulk volume and improved flow properties compared to previously known bulk ibuprofen crystalline materials.
    Type: Grant
    Filed: July 25, 1983
    Date of Patent: October 9, 1984
    Assignee: The Upjohn Company
    Inventors: Roger E. Gordon, Sanjay I. Amin
  • Patent number: 4476134
    Abstract: Therapeutic process for treating panic disorders in humans comprising the systemic administration of a 8-chloro-1-R-oxymethyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine of the formula ##STR1## wherein R is hydrogen, alkyl of from 1 to 3 carbon atoms, inclusive, ##STR2## wherein n is 0 to 16, inclusive, and m is 1 to 16 inclusive, including the N-oxides, esters, and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier.
    Type: Grant
    Filed: August 1, 1983
    Date of Patent: October 9, 1984
    Assignee: The Upjohn Company
    Inventor: James H. Coleman
  • Patent number: 4474966
    Abstract: The present invention provides novel 19-hydroxy-7a-homo-PGI.sub.1 19-hydroxy-19-methyl-7a-homo-PGI.sub.1 compounds which are useful for pharmacological purposes, e.g., anti-asthmatic indications.
    Type: Grant
    Filed: December 31, 1981
    Date of Patent: October 2, 1984
    Assignee: The Upjohn Company
    Inventor: John C. Sih
  • Patent number: 4474791
    Abstract: The present invention provides novel methods of inducing diuresis and/or an antihypertensive effect employing certain 2,6-diaryl-4-pyridinecarboxylic acid derivatives. Also provided are novel compositions to be used in these methods.
    Type: Grant
    Filed: December 13, 1982
    Date of Patent: October 2, 1984
    Assignee: The Upjohn Company
    Inventor: Louis L. Skaletzky
  • Patent number: 4474699
    Abstract: An improved process for preparing a 1-aminomethyl-6-substituted-4H-s-triazolo[4,3-a][1,4]benzodiazepine product, e.g., adinazolam, directly from the corresponding 1-hydrogen-6-substituted-4H-s-triazolo[4,3-a][1,4]benzodiazepine starting material, e.g., from estazolam, by conducting the reaction between the estazolam-type compound and the dimethylaminomethylene salt in the selected solvent in the presence of an alkali metal carbonate, and thereafter extracting the 1-aminomethyl-6-substituted-4H-s-triazolo[4,3-a]-[1,4]benzodiazepine from an aqueous organic solvent mixture thereof into a halogenated C.sub.1 to C.sub.3 -alkane solvent while maintaining the pH of the aqueous phase between pH 3.0 and 4.0, and thereafter recovering the product from the halogenated alkane solvent.
    Type: Grant
    Filed: May 25, 1983
    Date of Patent: October 2, 1984
    Assignee: The Upjohn Company
    Inventors: Donald J. Cram, Martin Gall, Michael F. Lipton
  • Patent number: 4474968
    Abstract: Racemic mixtures and optically active isomers of (.alpha.S-5S)-.alpha.-amino-3-chloro-.alpha.-isoxazoline-5-acetic acid (AT-125). Provides process for preparing AT-125 and its analogs and intermediates used in the process.
    Type: Grant
    Filed: November 14, 1980
    Date of Patent: October 2, 1984
    Assignee: The Upjohn Company
    Inventor: Robert C. Kelly
  • Patent number: 4473584
    Abstract: A process for treating Herpes Type I virus by the systemic administration or topical application of flurbiprofen (3-fluoro-4-phenylhydratropic acid) or a salt or ester thereof. Dosage forms are also disclosed.
    Type: Grant
    Filed: December 6, 1982
    Date of Patent: September 25, 1984
    Assignee: The Upjohn Company
    Inventor: Jay W. Heckler
  • Patent number: 4473649
    Abstract: Novel antibiotic U-64,864 producible in a fermentation under controlled conditions using a biologically pure culture of the microorganism Streptomyces braegensis Dietz sp.n., NRRL 12567. This antibiotic is active against various Gram-positive bacteria, for example, Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae. Thus, antibiotic U-64,864 can be used in various environments to eradicate or control such bacteria.
    Type: Grant
    Filed: September 2, 1982
    Date of Patent: September 25, 1984
    Assignee: The Upjohn Company
    Inventors: Lester A. Dolak, Fritz Reusser, Thomas M. Castle, Betty R. Hannon, Alice L. Laborde, Charles K. Marschke
  • Patent number: 4473580
    Abstract: This invention pertains to some new organic compounds, to a process for preparing them, and to formulations of them suitable for pesticidal use. The invention is more particularly directed to imidic acid derivatives of N-thio(methyl)carbamates.
    Type: Grant
    Filed: October 25, 1982
    Date of Patent: September 25, 1984
    Assignee: The Upjohn Company
    Inventors: Fred E. Dutton, Stephen J. Nelson
  • Patent number: 4472392
    Abstract: Novel solution stable ester prodrugs of corticosteroids of the formula ##STR1## and their salts.
    Type: Grant
    Filed: January 21, 1983
    Date of Patent: September 18, 1984
    Assignee: The Upjohn Company
    Inventors: Bradley D. Anderson, Robert A. Conradi
  • Patent number: 4472341
    Abstract: Disclosed is an improved process for the production of organic polyisocyanate based molded polymers prepared from at least one organic polyisocyanate and at least one polyol in the presence of an internal release agent wherein the improvement comprises employing as said agent a polysiloxane having at least one unit of the formula ##STR1## wherein R is selected from the group consisting of lower-alkyl and aryl, R.sup.1 is a divalent hydrocarbon radical, and R.sup.2 is selected from the group consisting of lower-alkoxy, aryloxy, particular hydroxyalkyleneoxy, alkoxyalkyleneoxy, amino, and hydroxyalkylamino radicals.The molding process can be repeated in many cycles before the molds require cleaning or treatment with release agent. The ease and rapidity with which the present process can be carried out makes it particularly suited to RIM production methods.
    Type: Grant
    Filed: July 5, 1983
    Date of Patent: September 18, 1984
    Assignee: The Upjohn Company
    Inventors: Louis M. Alberino, Dale F. Regelman, George H. Temme
  • Patent number: 4472397
    Abstract: Certain 1-(Nitrogen-containing group)-triazolo-benzodiazepines, e.g., adinazolam, are useful for treating psychotic, including schizophrenic, conditions in human patients.
    Type: Grant
    Filed: February 18, 1983
    Date of Patent: September 18, 1984
    Assignee: The Upjohn Company
    Inventors: Robert Lahti, Robert E. Pyke
  • Patent number: 4469689
    Abstract: Novel solution stable ester prodrugs of corticosteroids of the formula ##STR1## and their salts.
    Type: Grant
    Filed: March 30, 1983
    Date of Patent: September 4, 1984
    Assignee: The Upjohn Company
    Inventors: Bradley D. Anderson, Robert A. Conradi
  • Patent number: 4466977
    Abstract: Cis- and trans-N-[2-amino(oxy- or thia group-substituted-cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., 3,4-dichloro-N-[4,4-dimethoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzen eacetamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.
    Type: Grant
    Filed: November 4, 1982
    Date of Patent: August 21, 1984
    Assignee: The Upjohn Company
    Inventors: Moses W. McMillan, Jacob Szmuszkovicz
  • Patent number: 4467103
    Abstract: The present invention relates to novel methods of preparing a wide variety of spectinomycin analogs and biologically acceptable salts thereof. Further, the invention relates both to novel intermediates and novel products therein. The novel products are spectinomycin analogs which can be used for the same biological purposes as spectinomycin. The processes of the invention provide for novel intermediates that are versatile and highly reactive exocyclic enones.
    Type: Grant
    Filed: May 24, 1982
    Date of Patent: August 21, 1984
    Assignee: The Upjohn Company
    Inventors: David R. White, Clarence J. Maring
  • Patent number: RE31671
    Abstract: Polyurethane polyether-based elastomers are described which are thermoplastic, recyclable and have increased high temperature resistance which permits fabrication by injection molding. The elastomers are the product of reaction of 4,4'-methylenebis(phenyl isocyanate), a particular group of polypropylene oxide-polyethylene oxide block copolymers and an extender [straight chain aliphatic diols C.sub.2-6 or the bis(2-hydroxyethyl ether) of hydroquinone or resorcinol]. The block copolymers have at least 50 percent primary hydroxyl groups, a pH in the range of 4.5 to 9, a content of alkali metal ion less than 25 ppm and a molecular weight of 1000 to 3000. The minimum ethylene oxide (E.O.) residue content (percent by weight) of the polyether for any molecular weight (M.W.) is governed by the equation: ##EQU1## In a particularly preferred embodiment the elastomers are prepared by replacing up to 25 percent by equivalents of the extender by certain diols (polyethylene glycols up to 1500 M.W. preferred).
    Type: Grant
    Filed: February 26, 1981
    Date of Patent: September 11, 1984
    Assignee: The Upjohn Company
    Inventors: Henry W. Bonk, Tilak M. Shah
  • Patent number: RE31703
    Abstract: A process is disclosed for the preparation of liquid, storage-stable, polyisocyanate compositions containing a release agent formed in situ which compositions are useful, for example, as binder resins in the formation of particle boards which latter, because of the presence of the release agent, show no tendency to adhere to the face of metal platens used in their formation. The process comprises heating an organic polyisocyanate (polymethylene polyphenyl polyisocyanate preferred) with an acid phosphate (e.g. a mixture of mono- and di-alkyl acid phosphates) under conditions controlled as to time and temperature so as to yield a product which is storage stable and shows no tendency to deposit solid or to separate into two liquid phases.
    Type: Grant
    Filed: August 2, 1982
    Date of Patent: October 9, 1984
    Assignee: The Upjohn Company
    Inventors: Richard A. Prather, David L. Williams, Robert M. Partin, Warren J. Rabourn, deceased