Patents Examined by John Peabody
  • Patent number: 5462968
    Abstract: The invention relates to (.+-.) trans-2-[-4(1-hydroxyhexyl) phenyl]-5-oxocyclopentaneheptanoic acid, and ester and unsaturated derivatives thereof, prostaglandin derivatives. More particularly, the present invention concerns compounds of the formula I ##STR1## wherein the wavy bonds indicate that .alpha. or .beta. configuration, the dashed bond represents either a single or double bond, which double bond may be a cis or trans double bond and R is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.1 wherein m is 0-10, and R.sub.1 is an aliphatic ring having from about 3 to about 7 carbon atoms, or an aryl or heteroaryl ring having from about 4 to about 10 carbon atoms and wherein the heteroatom is selected from the group consisting of N, O and S. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
    Type: Grant
    Filed: January 19, 1994
    Date of Patent: October 31, 1995
    Assignee: Allergan, Inc.
    Inventor: David F. Woodward
  • Patent number: 5459160
    Abstract: Iridoid derivatives synthesized using genipin, which is an aglycon of geniposide, as the starting material are useful as an anti-hyperlipemia agent and as a cholagogue.
    Type: Grant
    Filed: June 23, 1994
    Date of Patent: October 17, 1995
    Assignee: Tsumura & Co.
    Inventors: Yuuichi Fujii, Ichiro Arai, Akira Hatta, Akemi Tatsugi, Hiroshi Mitsuhashi, deceased, by Mieko Mitsuhashi, legal representative, by Hiroyuki Mitsuhashi, legal representative, by Tomoaki Mitsuhashi, legal representative, Masaharu Kigawa
  • Patent number: 5457242
    Abstract: A process for preparing the novel compound 2-bromo, 1', 2'-dichloroperfluoro diethyl ether of formula:BrCFhd 2--CF.sub.2 --O--CFCl--CF.sub.2 Clwhere BrCF.sub.2 --CF.sub.2 OF is reacted with the olefin CFCl.dbd.CFCl, with bromohypofluorite being introduced into the reaction mixture in the form of a solution in an inert solvent based on chlorofluorohydrocarbon.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: October 10, 1995
    Assignee: Ausimont S.r.l.
    Inventors: Pierangelo Calini, Guglielmo Gregorio, Giorgio Guglielmo
  • Patent number: 5457106
    Abstract: There is disclosed a pharmaceutical composition for providing antiinflammatory, antipyretic, analgesic, antiallergic, immunosuppressing or immunomodulating activity which comprises a pyridine derivative of the formula (I): ##STR1## wherein R is an optionally substituted pyridine ring, X is a oxygen atom or --S(O).sub.n --, wherein n is 0, 1 or 2, A is a bivalent C.sub.1-15 hydrocarbon residue whose branched moiety may have a substituent, Y is an oxygen or sulfur atom, R.sub.3 is a hydrogen atom or an optionally substituted hydrocarbon residue, R.sub.4 is an optionally substituted hydrocarbon residue or an optionally substituted monocyclic or bicyclic heterocyclic group, R.sub.3 and R.sub.4 may be joined together with the carbamoyl group or the thiocarbamoyl group to which they are attached to form an optionally substituted heterocyclic group, or R.sub.3 or R.sub.
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: October 10, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Muneo Takatani, Taketoshi Saijo, Kiminori Tomimatsu
  • Patent number: 5453544
    Abstract: A process for making t-butylthiol by reacting hydrogen sulfide and an olefin having a carbon number of 3 to 15 in the presence of a HZSM-5, HZSM-12, or MCM-22 zeolite catalyst. The reaction takes place under autogenous pressure conditions and a temperature of about 70.degree. C. to about 160.degree. C.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: September 26, 1995
    Assignee: Mobil Oil Corporation
    Inventor: Thomas J. Giacobbe
  • Patent number: 5453550
    Abstract: A process for the production of alkyl tert alkyl ether, comprising the steps of providing a liquid hydrocarbon feedstock containing diolefin in an amount greater than or equal to about 2% wt, mixing said feedstock with an alcohol selected from the group consisting of methanol, ethanol, propanol and mixtures thereof and with hydrogen so as to provide a mixture of said feedstock, alcohol and hydrogen and contacting said mixture with an etherification catalyst under etherification process conditions including a pressure sufficient to maintain said hydrogen in a liquid phase, and a space velocity (LHSV) of less than or equal to about 1 h.sup.-1 so as to provide said alkyl tert alkyl ether without poisoning said catalyst.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: September 26, 1995
    Assignee: Intevep, S.A.
    Inventors: Marco Marquez, Raul Navarro
  • Patent number: 5449779
    Abstract: A process for preparing a compound of the formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen, R.sub.2 is e.g. C.sub.2 -C.sub.12 alkylene and R.sub.3 is e.g. C.sub.1 -C.sub.18 alkyl;which process comprises reacting, in water, in the absence of an organic solvent, a compound of the formula (II)Cl--COOR.sub.3 (II)wherein R.sub.3 is as defined above with a compound of the formula (III) ##STR2## where R.sub.1 is e.g. as defined above and R.sub.2 ' is e.g. as defined above for R.sub.2, at a temperature of from 0.degree. to 60.degree. C., 1 to 1.5 mol of the compound of the formula (II) being used per mol --NH-- group in the compound of the formula (III); and neutralizing the hydrochloric acid formed with an inorganic base.
    Type: Grant
    Filed: May 11, 1994
    Date of Patent: September 12, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Primo Carrozza, Giovanni Da Roit, Valerio Borzatta
  • Patent number: 5449837
    Abstract: A process is disclosed for producing a fluorinated ether of the formula R.sub.2 CHOCF.sub.2 A, where A is Cl or F, and each R is H, (CF.sub.2).sub.n Cl, (CF.sub.2).sub.n F or (CF.sub.2).sub.n H (n is an integer from 1 to 10) by reacting a first reactant of the formula R.sub.2 CHOY where Y is H, COF, COCl or COOCHR.sub.2 (R is as defined above), a second reactant selected of the formula CZ.sub.2 Cl.sub.2 or COZ.sub.2 where each Z is independently Cl or F (provided that when A is Cl, the second reactant is CZ.sub.2 Cl.sub.2), and HF; and recovering the fluorinated ether from the reaction products. Also disclosed are bis-ethers of the formula (CF.sub.3 (CF.sub.2).sub.m).sub.2 CHOCF.sub.2 OCH (CF.sub.2).sub.m CF.sub.3).sub.2, where m is an integer of 0 to 3, which can also be produced by the process.
    Type: Grant
    Filed: September 2, 1994
    Date of Patent: September 12, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Carl G. Krespan, V. N. Mallikarjuna Rao
  • Patent number: 5449839
    Abstract: Disclosed is an improved process for preparing ethyl t-butyl ether in one step which comprises reacting tertiary butanol and ethanol in the presence of a catalyst selected from zeolite beta and zeolite beta modified with multimetals selected from the group consisting of Groups IB, VB, VIB, VIIB or VIII of the Periodic Table at a temperature of about 20.degree. C. to 250.degree. C. and atmospheric pressure to about 1000 psig, wherein when the temperature is in the operating range above about 140.degree. C., the product comprises a two-phase mix of an ETBE-isobutylene and, optionally, diisobutylene product-rich phase and a heavier aqueous ethanol-rich phase.
    Type: Grant
    Filed: July 22, 1994
    Date of Patent: September 12, 1995
    Assignee: Texaco Chemical Inc.
    Inventors: John F. Knifton, Pei-Shing E. Dai
  • Patent number: 5449681
    Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: September 12, 1995
    Assignee: Eli Lilly and Company
    Inventor: David I. Wickiser
  • Patent number: 5446208
    Abstract: A process for the production of an ether alcohol is disclosed, which comprises subjecting a cyclic ketal to hydrogenolysis in the presence of a catalyst containing palladium in an amount of from 50 to 100% by weight, based on the total active catalytic component present. According to the inventive process, ether alcohols which are useful as perfumes or raw materials for perfumes can be produced easily with low cost and high yield.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: August 29, 1995
    Assignee: Kao Corporation
    Inventors: Junji Koshino, Hajime Miyabe, Yoshiaki Fujikura
  • Patent number: 5446152
    Abstract: This invention refers to heterocyclic compounds of general formula ##STR1## and their pharmacologically accepted salts. The derivatives described in this invention are active in the gastro-intestinal apparatus; in particular, they have prokinetic effects, in other words they create specific stimulation on gastro-intestinal motility, facilitating the passage of the contents of the alimentary tract, and possess anti-emetic qualities, without side effects involving the central nervous system.
    Type: Grant
    Filed: April 6, 1994
    Date of Patent: August 29, 1995
    Assignee: Alfa Wassermann S.p.A.
    Inventors: Claudia Baldazzi, Silvano Piani, Maria Barbanti, Egidio Marchi
  • Patent number: 5444063
    Abstract: A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
    Type: Grant
    Filed: October 28, 1992
    Date of Patent: August 22, 1995
    Assignee: Emory University
    Inventor: Raymond F. Schinazi
  • Patent number: 5442106
    Abstract: Described are preferred processes for hydrolyzing activated esters using, as catalysts, siloxanes having 4-dialkylaminopyridyl groups incorporated into their polymer backbones. The preferred siloxane catalyst materials demonstrate unexpected catalytic efficacy in the hydrolysis as well as enzyme-like selectivity for ester substrates.
    Type: Grant
    Filed: April 15, 1994
    Date of Patent: August 15, 1995
    Assignee: Indiana University Foundation
    Inventors: Martel Zeldin, Wilmer K. Fife, Slawomir Rubinsztajn
  • Patent number: 5440056
    Abstract: Compounds having the formula ##STR1## wherein --OR.sup.1 comprises alkanoyl or the C-13 side-chain of taxol; R.sup.2, R.sup.3, and R.sup.6 can be oxygenated or hydrogen in various combinations; and R.sup.4 and R.sup.5 are acyl groups,as well as a process for the preparation thereof, pharmaceutical compositions containing the above compounds, and a method for their use in inhibiting tumor growth.
    Type: Grant
    Filed: March 9, 1994
    Date of Patent: August 8, 1995
    Assignee: Abbott Laboratories
    Inventors: Larry L. Klein, Clinton M. Yeung, Leping Li
  • Patent number: 5440057
    Abstract: Transformations of taxol, baccatin III and of 10-deacetyl baccatin III provide access to novel taxol analogs and key intermediates thereto.
    Type: Grant
    Filed: August 20, 1993
    Date of Patent: August 8, 1995
    Assignee: The Scripps Research Institute
    Inventors: K. C. Nicolaou, Philippe G. Nantermet, Rodney K. Guy, Hiroaki Ueno
  • Patent number: 5436238
    Abstract: Novel chemical compounds that can be used to synthesize halichondrin B and norhalichondrin B, and related derivatives. The total synthesis of halichondrin B and norhalichondrin B is also disclosed.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: July 25, 1995
    Assignee: President and Fellows of Harvard College
    Inventors: Yoshito Kishi, Francis G. Fang, Craig J. Forsyth, Paul M. Scola, Suk K. Yoon
  • Patent number: 5436359
    Abstract: There are disclosed novel hydroquinone derivatives of the formulas: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments, and the derivatives of the formula (II) are intermediates for the production thereof.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: July 25, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirotomo Masuya, Masayoshi Yamaoka
  • Patent number: 5436246
    Abstract: The present invention is directed to a new class of 2-optionally substituted-4-piperazine-benzothiophene derivatives of the formula ##STR1## in which Y is represented by hydrogen or C.sub.1-3 alkyl; R is represented by a substituent selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, --CF.sub.3, --OCF.sub.3, and --OH; R.sub.1 is represented by hydrogen, cycloalkyl, C.sub.1-6 alkyl, phenyl optionally substituted, phenylalkyl, or phenylamidoalkyl; X is represented by hydrogen, --(CH.sub.2).sub.n X.sub.1, CH=CHX.sub.1 or CHX.sub.2 --(CH.sub.2).sub.q --CH.sub.3 ; n is an integer from 0-2; q is either the integer 0 or 1; X.sub.1 is represented by --OH--,--OR.sub.2, --NR.sub.2 R.sub.3, --CO.sub.2 R.sub.2, --CONR.sub.2 R.sub.3, --CN, or --COR.sub.2 ; R.sub.2 and R.sub.3 are each independently represented by hydrogen, C.sub.1-4 alkyl, phenyl optionally substituted, phenylalkyl, or R.sub.2 and R.sub.3 together form a (CH.sub.2).sub.m cycloalkyl, where m=2- 6; X.sub.2 is --OR.
    Type: Grant
    Filed: September 15, 1993
    Date of Patent: July 25, 1995
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Ronald C. Bernotas, Jeffrey S. Sprouse, Hsien C. Cheng
  • Patent number: 5434287
    Abstract: The subject matter of the present invention relates to bifunctional cyclohexyl DPTA ligands and methods for utilizing these compounds.
    Type: Grant
    Filed: November 4, 1993
    Date of Patent: July 18, 1995
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Otto A. Gansow, Martin W. Brechbiel