Patents Represented by Attorney Sidney B. Williams
  • Patent number: 6531139
    Abstract: The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a lipophilic, pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 by weight (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di- unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic compounds.
    Type: Grant
    Filed: July 27, 1998
    Date of Patent: March 11, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: Ping Gao, Walter Morozowich
  • Patent number: 6331636
    Abstract: This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.
    Type: Grant
    Filed: March 12, 1992
    Date of Patent: December 18, 2001
    Assignee: The Upjohn Company
    Inventors: Arthur G. Romero, William H. Darlington
  • Patent number: 5552152
    Abstract: A chewable taste-masked ibuprofen tablet having controlled release characteristics.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 3, 1996
    Assignee: The Upjohn Company
    Inventor: Robert W. Shen
  • Patent number: 5486611
    Abstract: This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula I: ##STR1## wherein X is --(CH.sub.2).sub.n -- or --C(R.sub.1)(H)--; R is C.sub.1 -C.sub.8 alkyl; and R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8) alkynyl, aryl and benzyl.These compounds are useful to treat central nervous system disorders and are unexpectedly resistant to metabolism by the liver and have superior oral plasma bioavailability.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: January 23, 1996
    Assignee: The Upjohn Company
    Inventors: Chiu-Hong Lin, Susanne R. Haadsma-Svensson, Robert B. McCall, Arthur G. Romero, William H. Darlington, Michael D. Ennis
  • Patent number: 5349128
    Abstract: The coat protein gene of cucumber mosaic virus strain WL (CMV-WL), the method of preparing it, its use to prepare transgenic plants and transgenic plants containing it are provided.
    Type: Grant
    Filed: January 28, 1993
    Date of Patent: September 20, 1994
    Assignee: The Upjohn Company
    Inventors: Hector D. Quemada, Jerry L. Slightom, Dennis Gonsalves, Chris Kearney
  • Patent number: 5324664
    Abstract: Methods for isolating thymidine kinase-encoding DNA of a herpes virus are described. These methods utilize degenerate primers based on regions of relatively conserved amino acid sequence in herpes virus thymidine kinase proteins to initiate a polymerase chain reaction which yields large amounts of the thymidine kinase-encoding DNA. The methods are illustrated in the isolation of the thymidine kinase gene of feline herpes virus, which can be used to construct recombinant thymidine kinase-negative feline herpes viruses for purposes of constructing live vaccines and expression vectors. In addition, the regulatory elements of the feline herpes virus thymidine kinase gene are useful in the construction of recombinant DNA vectors.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: June 28, 1994
    Assignee: The Upjohn Company
    Inventors: Jack H. Nunberg, Leonard E. Post, Teresa Compton, Erik A. Petrovskis
  • Patent number: 5268284
    Abstract: Provided are ribosome binding sites having an increased number of adenine (A) and thymidine (T) residues as compared to the naturally occurring ribosome binding sites from which they are derived or to which they are related, which allow high level expression of genes encoding heterologous polypeptides, particularly somatotropins, operatively linked thereto.
    Type: Grant
    Filed: August 27, 1990
    Date of Patent: December 7, 1993
    Assignee: The Upjohn Company
    Inventors: Che-Shen C. Tomich, Mary K. Olsen
  • Patent number: 5250711
    Abstract: Amine salts of alkane-1,n-dicarboxylic acid mono-(2-sulfatoethyl)amides of the Formula IHOC(O)--(CH.sub.2).sub.n --C(O)--N(R.sub.1)--CH.sub.2 CH.sub.2 SO.sub.3.sup.--+ HN(R.sub.2).sub.3 Iwherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.8 alkyl and phenyl, R.sub.2 is C.sub.1 -C.sub.8 alkyl or (R.sub.2).sub.3 when taken together with the nitrogen atom is pyridinyl; and n is an integer from 4 to 20, their preparation and use to prepare water-soluble esters of corticosteroids.
    Type: Grant
    Filed: January 12, 1990
    Date of Patent: October 5, 1993
    Assignee: The Upjohn Company
    Inventor: Bruce A. Pearlman
  • Patent number: 5245046
    Abstract: Provided are novel .alpha.-aminoindole-3-acetic acid derivatives having the formula ##STR1## wherein R through R9 are as defined in the specification, and pharmacologically acceptable salts of compounds wherein R.sub.9 is not OM, which are useful as anti-diabetic, anti-obesity and anti-atherosclerotic agents.
    Type: Grant
    Filed: May 8, 1991
    Date of Patent: September 14, 1993
    Assignee: The Upjohn Company
    Inventors: Gilbert A. Youngdale, John C. Sih, Steven P. Tanis, Chiu-Hong Lin
  • Patent number: 5220034
    Abstract: Process for alkylating protected spectinomycin enone derivatives in the gamma position in order to produce intermediates useful in the synthesis of 6'alkylspectinomycins. The intermediate have the formula ##STR1## which comprises reacting a compound having the formula ##STR2## with a strong base and an alkenyl halide, wherein R.sub.1 is selected from the group consisting of alkoxycarbonyl, halogenated alkoxycarbonyl, aralkoxycarbonyl, and arylsulfone; R.sub.2 is selected from the group consisting of hydrogen, trimethylsilyl (TMS), tetrahydropyran (THP), and triethylsilyl (TES); A is selected from the group consisting of oxygen and sulfur; M is selected from the group consisting of lithium and potassium; and n is an integer from 1 to 3.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: June 15, 1993
    Assignee: The Upjohn Company
    Inventor: Paul M. Herrinton
  • Patent number: 5132424
    Abstract: New pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of formula (I), ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4 and m are as defined in the specification, e.g., 4-(benzoylmethyl)-6-cyclohexyl-6,7-dihydro-2-phenyl-4H-pyrazolo[1,5-a]pyrr olo[3,4-d]pyrimidine-5,8-dione, have been found to be potentially useful to treat warm-blooded animal patients suffering from the symptoms of atherosclerosis and cholesterol buildup to relieve the same and for favorably altering the high density lipoprotein (HDL) to low density lipoprotein (LDL) ratio in blood samples of such patients.
    Type: Grant
    Filed: January 21, 1991
    Date of Patent: July 21, 1992
    Assignee: The Upjohn Company
    Inventors: Scott D. Larsen, Frank P. Bell
  • Patent number: 5087639
    Abstract: A method for the prevention of central nervous system toxicity of acivicin which comprises the concomitant administration of acivicin and an amino acid solution consisting essentially of large neutral amino acids.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: February 11, 1992
    Assignee: The Upjohn Company
    Inventors: J. Patrick McGovren, Marta G. Williams, Robert H. Earhart
  • Patent number: 5079007
    Abstract: An controlled release implant antibiotic formulation comprising (a) a crystalline salt of the antibiotic; (b) an amorphous salt of the antibiotic; and (c) excipients; whereas the excipients comprise from 0% to 10% of the tablet by weight.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: January 7, 1992
    Assignee: The Upjohn Company
    Inventor: Michael L. Putnam
  • Patent number: 4978753
    Abstract: A 7-phenylpyrimido[1,2-a][1,4]benzodiazepin-3(5H)-ones of the formula II: ##STR1## wherein R.sub.o is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, --COOR in which R is alkyl defined as above, ##STR2## in which n is a number of 1 to 4, R.sub.6 and R.sub.7 are hydrogen or alkyl defined as above or together ##STR3## is selected from the group consisting of pyrrolidino, piperidino, morpholino, and 4-methylpiperazino, and --CH.sub.2 OH; wherein R.sub.1 is selected from the group consisting of hydrogen, hydroxy, acetoxy, propionoxy, succinyloxy, and alkyl esters thereof; wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.
    Type: Grant
    Filed: November 2, 1989
    Date of Patent: December 18, 1990
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4902794
    Abstract: 1-Substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula (III): ##STR1## wherein R is selected from the group consisting of hydroxy, esters thereof, and alkoxy, in which the alkyl group is of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoylamino, and dialkylamino in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, are produced by condensing a 1,3-dihydro-5-phenyl-2H-1,4-benzodiazepine-2-thione of the formula (I): ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.
    Type: Grant
    Filed: July 20, 1983
    Date of Patent: February 20, 1990
    Assignee: The Upjohn Company
    Inventor: Jackson B. Hester, Jr.
  • Patent number: 4891382
    Abstract: A method for the prevention of pancreatitis utilizing cis- and trans-N-(3-aminocycloaliphatic)-2-arylacetamide derivative compounds of the formula ##STR1## e.g., N-[2-(n',N'-dimethylamino)cyclohexyl]-N-methyl-2-(4-bromophenyl)acetamide and trans-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]acetamide, 2-(3,4-dichlorophenyl) and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: April 22, 1988
    Date of Patent: January 2, 1990
    Assignee: The Upjohn Company
    Inventors: Cleo Lancaster, Andre Robert
  • Patent number: 4810700
    Abstract: An estrogen sulfotransferase inhibitor composition comprises a compound of the formula ##STR1## wherein R.sub.1 is F, Br, NO.sub.2, or H; R.sub.2 is F, Br, NO.sub.2, NH.sub.2, or H; R is H or alkyl of 1-4 carbon atoms; R.sub.3 is O or H.sub.2 ; and R.sub.4 is H.sub.2, O, or .alpha.-H, .beta.-OH; R.sub.5 is H.sub.2, .alpha.-H and .beta.-OH or B-H and .alpha.-OH in admixture with a pharmaceutically acceptable carrier with the proviso that R.sub.1, R.sub.2 and R.sub.3 cannot all be hydrogen and one of R.sub.1 and R.sub.2 is F.
    Type: Grant
    Filed: May 18, 1983
    Date of Patent: March 7, 1989
    Assignee: Wayne State University
    Inventor: Samuel C. Brooks
  • Patent number: 4767847
    Abstract: The invention concerns a novel nogamycin having a heretofore unknown configuration and novel analogs which are active against various microorganisms. The invention also includes novel methods of making substituted and unsubstituted nogamycin having an essentially pure isomeric form of a preferred configuration.
    Type: Grant
    Filed: May 11, 1981
    Date of Patent: August 30, 1988
    Assignee: The Upjohn Company
    Inventors: Paul F. Wiley, David W. Elrod
  • Patent number: 4711960
    Abstract: Isochromans, isothiochromans, 2-benzoxepins and 2-benzothiepins are described. The compounds possess hypotensive and anti-psychotic properties; methods and compositions using them are described.
    Type: Grant
    Filed: January 28, 1986
    Date of Patent: December 8, 1987
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4710565
    Abstract: Process for preparing clindamycin and analogs thereof by reacting lincomycin or an analog thereof with a dimethylformamide and an excess of thionyl halide.
    Type: Grant
    Filed: January 24, 1986
    Date of Patent: December 1, 1987
    Assignee: The Upjohn Company
    Inventors: Douglas A. Livingston, Janet E. Petre