Patents Examined by Ba K. Trinh
  • Patent number: 6136999
    Abstract: A chemical compound having the formula: ##STR1## wherein P.sub.1 is a hydroxyl protecting group, R.sub.1 may be H or electron withdrawing group, R.sub.2 may be H or electron withdrawing group, R.sub.3 may be H or electron withdrawing group, R.sub.4 may be H or electron withdrawing group, R.sub.5 may be H or electron withdrawing group, R.sub.6 may be an alkyl group, an olefinic group, an aromatic group, Ph, PhCH.sub.2, an O-alkyl group, an O-olefinic group, an O-aromatic group, O--Ph, or O--CH.sub.2 Ph.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: October 24, 2000
    Assignee: NaPro BioTherapeutics, Inc.
    Inventors: Madhavi C. Chander, James D. McChesney, Jan Zygmunt
  • Patent number: 6136988
    Abstract: An antitumor compound of formula (5) ##STR1## and also provided by the present invention is a method of preparing a compound of formula (5) whereby diesterification of the alcohol groups located at the 2' and 7 positions of paclitaxel is followed by the hydrolysis of the 2' hexanoate group resulting in 7-hexanoyltaxol.
    Type: Grant
    Filed: April 10, 1998
    Date of Patent: October 24, 2000
    Assignee: Hauser, Inc.
    Inventors: Christopher K. Murray, Qun Y. Zheng, Sagar R. Shakya
  • Patent number: 6136989
    Abstract: A method of isolating paclitaxel from pactitaxel-containing material that includes the steps of obtaining an acetone mixture of the paclitaxel-containing material, then mixing the acetone mixture with an aqueous solvent to form an aqueous supernatant and a precipitate, wherein the precipitate contains at least 3-times higher paclitaxel content than the paclitaxel extract. The acetone/water precipitation step provides a high yield of highly pure paclitaxel that is suitable for industrial scale isolation using conventional normal-phase silica chromatography steps, and the preparation of pharmaceutical compositions containing paclitaxel.
    Type: Grant
    Filed: December 30, 1998
    Date of Patent: October 24, 2000
    Assignee: Phytogen Life Sciences, Incorporated
    Inventors: Samuel Siang Kiang Foo, Yili Bai, Martin Ehlert
  • Patent number: 6136991
    Abstract: The invention provides for a purified glycidyl ester product prepared from neo acids wherein said ester product is recovered as a light fraction from a glycidyl ester reaction product composition that has been subjected to conditions of temperature and vacuum in a thin film, short pass distillation evaporator, said purified glycidyl ester product further characterized that its polymerizable reaction product with methacrylic acid has a higher effective glass transition temperature as compared with the polymerizable reaction product with methacrylic acid of said glycidyl ester reaction product composition prior to purification.
    Type: Grant
    Filed: November 10, 1997
    Date of Patent: October 24, 2000
    Assignee: Exxon Chemical Patents Inc.
    Inventors: Richard William Ryan, Gerald G. McGlamery, Jr., Ralph Martin Kowalik, Michael J. Keenan
  • Patent number: 6133462
    Abstract: A compound for use in the production of taxanes and intermediates therefor having the formula: ##STR1## wherein R is an alkyl group.
    Type: Grant
    Filed: September 2, 1997
    Date of Patent: October 17, 2000
    Assignees: NaPro BioTherapeutics, Inc., Bryn Mawr College
    Inventors: Nicholas J. Sisti, Charles S. Swindell
  • Patent number: 6133457
    Abstract: A compound of formula IV ##STR1## wherein G is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl or Ar;Ar is an aromatic or heteroaromatic group or a substituted aromatic or heteroaromatic group;R.sup.1 is halo, SR, OR, amino, mono or di-(C.sub.1 -C.sub.6 -alkyl)amino, tri (C.sub.1 -C.sub.6 -alkyl)ammonium, C.sub.1 -C.sub.6 -alkylthio, di(C.sub.1 -C.sub.6 -alkyl)sulfonium, C.sub.1 -C.sub.6 -alkylsulfonyl, or C.sub.1 -C.sub.6 -alkylphosphonyl;R.sup.2 is OH or SH; orR.sup.1 and R.sup.2 taken together form a second bond or together form an epoxide, aziridine, episulfide, or cyclopropyl ring;R is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl or Ar;R.sup.3 is C.sub.1 -C.sub.6 alkyl;R.sup.4 and R.sup.5 are H; orR.sup.4 and R.sup.5 taken together form a second bond;R.sup.24 is a leaving group; andR.sup.26 is an alcohol protecting group;X is O, NH or (C1-C3 alkyl)N--.
    Type: Grant
    Filed: July 2, 1999
    Date of Patent: October 17, 2000
    Assignees: Eli Lilly and Company, Wayne State University, University of Hawaii
    Inventor: Vinod F Patel
  • Patent number: 6130240
    Abstract: Described is a novel compound and method, useful for treatment of cardiac arrhythmias, especially useful in patients with congestive heart failure (CHF). A process for synthesizing the novel compound is also described.
    Type: Grant
    Filed: December 14, 1998
    Date of Patent: October 10, 2000
    Assignee: Aryx Therapeutics, Inc.
    Inventor: Pascal Druzgala
  • Patent number: 6127355
    Abstract: The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;(n) is zero (0) or a positive integer, preferably from 1 to about 12;R.sub.1 and R.sub.2 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls;R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted alkyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## R.sub.4 and R.sub.5 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C.sub.1-6 alkyls or jointly form a cyclic C.sub.5 -C.sub.7 ring.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: October 3, 2000
    Assignee: Enzon, Inc.
    Inventors: Richard B. Greenwald, Annapurna Pendri, Hong Zhao
  • Patent number: 6127558
    Abstract: Epoxy resins which are diglycidyl ethers of tetrabromobisphenol A having a crystalline structure and in particulate form have an epoxy equivalent weight between 320 and 380 g/eq and a chlorine content that is smaller than 0.3%.
    Type: Grant
    Filed: May 5, 1998
    Date of Patent: October 3, 2000
    Assignee: Bromine Compounds Ltd.
    Inventors: Yoav Bar-Yaakov, Daniel Plewinski
  • Patent number: 6127557
    Abstract: A method for producing silasesquioxane metal complexes of the formula (II)((R.sup.1 SiO.sub.1,5).sub.n (R.sup.2a SiO.sub.1,5).sub.m ((B).sub.q (O).sub.r)).sub.u (M).sub.v (Y).sub.win which R.sup.1 represents C.sub.5 -C.sub.10 -cycloalkyl, norbornyl or adamantyl; R.sup.2a represents oxygen; B represents H, OH, halogen, alkoxy, SiR.sup.3.sub.y in which R.sup.3 can be C.sub.1 -C.sub.4 alkyl, aryl or substituted silyl groups, and y represents 2 or 3, and R.sup.1 and R.sup.3 can be functionalized; M represents metals of the 4.sup.th to 7.sup.th subgroups of the periodic system of elements; Y represents C.sub.1 -C.sub.20 alkyl or aryl groups devoid of beta-hydrogen, silyl, alkoxy, OH, halogen, oxo, imido, fluorenyl, indenyl, cyclopentadienyl, in which the individual ligands can be substituted; n=6 or 7; m=0 or 1; q=0-2; r=0-2; u=1-4; v=1-4; w=0-12, in which a metal compound of the 4.sup.th to 7.sup.th subgroups of the periodic system of elements and at least one silasesquioxane compound of the formula (I)(R.sup.
    Type: Grant
    Filed: October 18, 1999
    Date of Patent: October 3, 2000
    Assignee: Solvay Deutschland GmbH
    Inventors: Rutger Anthony Van Santen, Hendrikus Cornesis Louis Abbenhuis, Martinus Lambertus Wilhelmus Vorstenbosch
  • Patent number: 6127555
    Abstract: A process for selective monoacylation of 10-deacetylbaccatin III, or a derivative thereof in positions C-2 and C-4 possessing free hydroxyl groups in positions C-7 and C-10, using a methyleneiminium salt.
    Type: Grant
    Filed: May 5, 1999
    Date of Patent: October 3, 2000
    Assignee: Aventis Pharma S.A.
    Inventors: Eric Didier, Pascal Pecquet
  • Patent number: 6127556
    Abstract: In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80.degree. C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0.degree. C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: October 3, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Chin Liu, John S. Ng, James R. Behling, Arthur L. Campbell
  • Patent number: 6124481
    Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal or an ammonium alkoxide is reacted with a .beta.-lactam.
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: September 26, 2000
    Assignee: Florida State University
    Inventor: Robert A. Holton
  • Patent number: 6121465
    Abstract: Process for the production of drospirenone (6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-3-oxo-17.alpha.-pregn-4-ene-21, 17-carbolactone, DRSP) (1) and 7.alpha.-(3-hydroxy-1-propyl)-6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-5.beta.-androstane-3.beta., 5, 17.beta.-triol (ZK 92836) and 6.beta., 7.beta.; 15.beta., 16.beta.-dimethylene-5.beta.-hydroxy-3-oxo-17.alpha.-androstane-21, 17-carbolactone (ZK 90965) as intermediate products of the process.
    Type: Grant
    Filed: February 11, 1999
    Date of Patent: September 19, 2000
    Assignee: Schering Aktiengesellschaft
    Inventors: Jorg-Thorsten Mohr, Klaus Nickisch
  • Patent number: 6121467
    Abstract: The invention relates to a method for separating a gaseous mixture comprising formaldehyde and trioxane, wherein at least some of the formaldehyde and the trioxane are dissolved from the mixture in a alcohol-containing liquid and the trioxane is crystallized from the solution thus obtained and is separated.
    Type: Grant
    Filed: July 23, 1999
    Date of Patent: September 19, 2000
    Assignee: Ticona GmbH
    Inventors: Hagen Kniep, Christine Meister, Elke Schweers, Ioannis Nicolaou, Dirk Scheid
  • Patent number: 6118011
    Abstract: This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.
    Type: Grant
    Filed: November 27, 1996
    Date of Patent: September 12, 2000
    Assignee: The Liposome Company, Inc.
    Inventors: Eric Mayhew, J. Craig Franklin, Suresh Bhatia, Paul A. Harmon, Andrew S. Janoff
  • Patent number: 6114550
    Abstract: A .beta.-phenylisoserine derivative of general formula (I): ##STR1## in the form of a salt or an ester, in which Ar represent an aryl radical, R represents a phenyl or naphthyl or a O--R.sub.1 radical and G.sub.1 represents --CH.sub.2 --Ph radical; and a method of using the same for making taxane derivatives.
    Type: Grant
    Filed: November 10, 1997
    Date of Patent: September 5, 2000
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Jean-Noel Denis, Andrew-Elliot Greene, Alice Kanazawa
  • Patent number: 6114552
    Abstract: Highly active and selective epoxidation catalysts are prepared by combining high surface area silica support or the like, having surface area greater than 1100 m.sup.2 /g, with a titanium source. The titanium source is a non-oxygenated hydrocarbon solution of a titanium halide or a vapor stream of titanium tetrachloride. The impregnated support it then calcined at an elevated temperature (preferably, in a substantially oxygen-free atmosphere), and, optionally, reacted with water and/or silylated. The resulting materials are highly active heterogeneous epoxidation catalysts for the reaction of olefins to with organic hydroperoxides.
    Type: Grant
    Filed: September 28, 1999
    Date of Patent: September 5, 2000
    Assignee: Arco Chemical Technology, L.P.
    Inventors: Yuan-Zhang Han, Edrick Morales, Robert G. Gastinger, Kevin M. Carroll
  • Patent number: 6114545
    Abstract: The present invention provides novel haloenol lactones that are effective as active site inhibitors of cholesterol esterase. By inhibiting cholesterol esterase the inhibitors of the present invention provide a new approach to the treatment of hypercholesterolemia through limiting the bioavailability of dietary cholesterol.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: September 5, 2000
    Assignee: University of New Mexico
    Inventors: Lorraine Deck, David L. Vander Jagt
  • Patent number: 6114553
    Abstract: A catalyst for the production of ethylene oxide by the vapor phase oxidation of ethylene under specific conditions such that an amount of chlorine suffered to adhere thereto is not more than 2 mol % per mol of silver after the duration of the reaction caused under the specific conditions has totalled 240 hours from the start of the reaction, a silver catalyst for the production of ethylene oxide which incorporates therein an organic nitrogen compound, methods for the production of the catalysts mentioned above, and a method for the production of ethylene oxide by the gaseous-phase oxidation of ethylene with a molecular oxygen-containing gas in the presence of such a catalyst.
    Type: Grant
    Filed: December 15, 1998
    Date of Patent: September 5, 2000
    Assignee: Nippon Shokubai Co., Ltd.
    Inventors: Masaharu Kiriki, Hitoshi Takada