Patents Examined by Ba K. Trinh
  • 7-hexanoyltaxol and methods for preparing the same
    Patent number: 6469050
    Abstract: An antitumor compound of formula (5): 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: October 16, 2000
    Date of Patent: October 22, 2002
    Inventors: Christopher K. Murray, Qun Y. Zheng, Sagar R. Shakya
  • Total synthesis of antitumor acylfulvenes
    Patent number: 6469184
    Abstract: The present invention provides a method of synthesizing compounds of formula (I): wherein R and R′ are independently (C1-C4)alkyl.
    Type: Grant
    Filed: June 5, 2001
    Date of Patent: October 22, 2002
    Assignee: Regents of the University of California
    Inventor: Trevor C. McMorris
  • Asymmetric 1,4-reductions of and 1,4-additions to enoates and related systems
    Patent number: 6465664
    Abstract: One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: October 15, 2002
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L Buchwald, Daniel H. Appella, Yasunori Moritani, Ryo Shintani, Valdas Jurkauskas
  • Epoxyvibsanin B
    Patent number: 6462078
    Abstract: This invention relates to a new compound, epoxyvibsanin B, which can be used to treat an IL-12 overproduction-related disorder such as an inflammatory disease.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: October 8, 2002
    Assignee: Shionogi Bioresearch Corp.
    Inventors: Mitsunori Ono, Yumiko Wada, Naoto Yamaguchi, Jifeng Duan
  • C7 acyloxy and hydrido taxane derivatives and pharmaceutical compositions containing them
    Patent number: 6462208
    Abstract: Taxane derivatives having alternative C7 substituents.
    Type: Grant
    Filed: October 25, 1999
    Date of Patent: October 8, 2002
    Assignee: Florida State University
    Inventors: Robert A. Holton, Ki-Byung Chai
  • Preparation of substituted isoserine esters using &bgr;-lactams and metal or ammonium alkoxides
    Patent number: 6458977
    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 &bgr;-lactam.
    Type: Grant
    Filed: March 2, 2000
    Date of Patent: October 1, 2002
    Assignee: Florida State University
    Inventor: Robert A. Holton
  • Taxoid anti-tumor agents, pharmaceutical compositions, and treatment methods
    Patent number: 6458976
    Abstract: A taxoid of formula (7), a method for making the taxoid, a pharmaceutical composition containing the taxoid, and a method for treating tumors by administering the taxoid: wherein R1 is a branched or unbranched C3-C5 alkyl or alkenyl radical, CF2H, or (S)-2,2-dimethylcyclopropyl; R8 is a C1-C4 alkyl radical; and R7 is F, Cl, MeO, vinyl, Me, or N3.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: October 1, 2002
    Assignee: The Research Foundation of State University of New York
    Inventor: Iwao Ojima
  • Phosphonooxymethyl ethers of taxane derivatives
    Patent number: 6455575
    Abstract: The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: September 24, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jerzy Golik, Dolatrai Vyas, John J. Wright, Henry Wong, John F. Kadow, John K. Thottathil, Wen-Sen Li, Murray A. Kaplan, Robert K. Perrone, Mark D. Wittman
  • Heat recovery procedure
    Patent number: 6452027
    Abstract: The present invention provides a process treating the cycle gas from an ethylene oxide reactor to avoid heat losses in a carbonate scrubbing system as well as glycol formation in the carbonate scrubbing and catalyst contamination upon cycle gas recycle.
    Type: Grant
    Filed: September 10, 2001
    Date of Patent: September 17, 2002
    Assignee: Scientific Design Company, Inc.
    Inventors: Barry Billig, James Mann
  • Three-step conversion of protected taxane ester to paclitaxel
    Patent number: 6452025
    Abstract: The present invention relates to a method of producing paclitaxel from a protected coupled ester compound having a formula: wherein P1 is a hydrogenatable protecting group, comprising deprotecting the 7-O-position and 3′-N-position of the protected coupled ester compound to form a first intermediate compound, benzoylating the first intermediate compound at the 3′-N-position thereby to form a second intermediate compound, and deprotecting the second intermediate compound by replacing P1 with hydrogen in the presence of an acid. The present invention also provides chemical compounds useful in the production of paclitaxel.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: September 17, 2002
    Assignee: NaPro BioTherapeutics, Inc.
    Inventors: Jan Zygmunt, James D. McChesney
  • Methods and useful intermediates for paclitaxel synthesis from C-7, C-10 di-cbz 10-deacetylbaccatin III
    Patent number: 6448417
    Abstract: The present invention relates to a method of producing paclitaxel or a paclitaxel analog comprising the esterification of C-7, C-10 di-CBZ 10-deacetylbaccatin III with an N-carbamate protected, C-2-protected 3-phenyl isoserine side chain. The C-7, C-10 carbobenzyloxy groups are then replaced with hydrogen and an acyl group is substituted at the C-3′ nitrogen. The resulting compound is acylated at the C-10 hydroxyl position, and deprotected at the C-2′ position by replacing the hydroxyl protecting group with hydrogen to produce paclitaxel or a paclitaxel analog. The present invention also relates to alternative methods of acylating a 10-hydroxy paclitaxel analog. The first method comprises dissolving a 10-hydroxy paclitaxel analog in an acceptable ether solvent therefor to form a first solution at a first temperature.
    Type: Grant
    Filed: January 11, 2001
    Date of Patent: September 10, 2002
    Assignee: NaPro BioTherapeutics, Inc.
    Inventors: Nicholas J. Sisti, Herbert R. Brinkman, James D. McChesney, Medhavi C. Chander, Xian Liang, Jan Zygmunt
  • Direct epoxidation process using a palladium on niobium-containing support
    Patent number: 6441203
    Abstract: The invention is a liquid-phase process for epoxidizing an olefin with hydrogen and oxygen in the presence of a supported catalyst comprising palladium on niobium-containing support. The process exhibits good productivity and selectivity for olefin epoxidation with hydrogen, and oxygen. This is particularly surprising because typical palladium-containing epoxidation catalysts require the presence of a titanium zeolite.
    Type: Grant
    Filed: October 19, 2001
    Date of Patent: August 27, 2002
    Assignee: Arco Chemical Technology, L.P.
    Inventor: Roger A. Grey
  • Podophyllotoxin dimer as DNA topoisomerase II inhibitors, and a process for the preparation therefore
    Patent number: 6441198
    Abstract: The present invention discloses novel podophyllotoxin dimers having structural formula I wherein R is H or CH3 and Z is aryl or subsituted aryl compound selected form the group counting of phenylene, naphthalene, p-terpbhnyl, dimethoxy benzidine and diphenyl ether and a process for the preparation of said novel podophyllotoxin dimers. The new podophyllotoxin dimers, pawculaty 4-arylamino derivatives of the podophyllotoxin dimers of the present invention as useful as potent inhibitors of DNA-topoisomerase II and are also useful as antitumour agents.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: August 27, 2002
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmed Kamal, Laxman Eltepu, Arifuddin Mohammed, Gollapalli Bhasker Ramesh Khanna
  • Direct epoxidation process using a mixed catalyst system
    Patent number: 6441204
    Abstract: The invention is a liquid-phase process for epoxidizing an olefin with hydrogen and oxygen in the presence of a catalyst mixture comprising a titanium zeolite and a supported catalyst comprising palladium on niobium-containing support. The process is highly selective and productive for transforming olefins to epoxides in the liquid-phase reaction of an olefin, hydrogen, and oxygen.
    Type: Grant
    Filed: October 19, 2001
    Date of Patent: August 27, 2002
    Assignee: Arco Chemical Technology, L.P.
    Inventor: Roger A. Grey
  • Process for the preparation of 10-deacetylbaccatin III
    Patent number: 6437154
    Abstract: The present invention discloses a process for the conversion of a mixture of taxol analogues 7-xylosyl-10-deacetylbaccatin taxols of the formula 2 where R is C6H5, CH3C═CHCH3 or C5H11 into 10-deacetylbaccatin III of the formula 1 by dissolving the taxol analogue of formula 2 in a polar solvent, reacting the resultant solution with a base at a temperature of 20-50° C. for a time period in the range of 20-40 hours, and isolating 7-xyloxyl-10-deacetylbaccatin III, dissolving the 7-xylosyl-10-deacetylbaccatin III in a polar solvent, reacting the resultant solution with a periodate at 20-40° C. for a time period in the range of 20-40 hours to cleave the diol system of the xyloside into dialdehyde, treating the generated dialdehyde in an organic acid medium with salts of amine at 0-40° C. for 12-18 hours and isolating 10-deacetylbaccatin III of formula 1.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: August 20, 2002
    Assignee: Council of Scientific and Industrial Research
    Inventors: Sunil Kumar Chattopadhyay, Sachin Srivastava, Vijay Kumar Mehta
  • Tricyclic and tetracyclic taxane intermediates
    Patent number: 6433189
    Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.
    Type: Grant
    Filed: July 17, 2001
    Date of Patent: August 13, 2002
    Assignee: Florida State University
    Inventors: Robert A. Holton, Carmen Somoza, Hyeong Baik Kim, Mitsuru Shindo, Ronald J. Biediger, P. Douglas Boatman, Chase Smith, Feng Liang, Krishna Murthi
  • Method for making an oxirane
    Patent number: 6429322
    Abstract: Process for manufacturing an epoxide by reaction between an olefin and a peroxide compound in the presence of a zeolite-based catalyst and in the presence of a solvent, in which the pH of the reaction medium comprising the olefin, the peroxide compound, the catalyst, the epoxide formed and the solvent is from 4.8 to 6.5.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: August 6, 2002
    Assignee: Solvay SA
    Inventors: Jean-Pierre Catinat, Michel Strebelle
  • Method of treating atherosclerosis or restenosis using microtubule stabilizing agent
    Patent number: 6429232
    Abstract: The present invention is a method of preventing or reducing atherosclerosis or restenosis, and a pharmaceutical preparation used therefor. In particular, it is a method of preventing or reducing atherosclerosis or restenosis after arterial injury by treatment with a low dose of a microtubule stabilizing agent such as taxol or a water soluble taxol derivative. The low dose used in the present invention prevents artery blockage while minimizing any negative side effects associated with the drug.
    Type: Grant
    Filed: March 21, 1997
    Date of Patent: August 6, 2002
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: James L. Kinsella, Steven J. Sollot
  • Refining treatment method of liquid reaction mixture obtained from epoxidation reaction of 1,5,9-cyclododecatriene
    Patent number: 6420575
    Abstract: After 1,5,9-cyclododecatriene is epoxidized with hydrogen peroxide in the presence of a catalyst containing a tungsten compound, a quaternary onium salt and a mineral acid, to obtain a liquid reaction mixture containing the resultant 1,2-epoxy-5,9-cyclododecadiene, the catalyst, non-reacted hydrogen peroxide and non-reacted 1,5,9-cyclododecatriene and being phase-separated into an oil phase fraction and an aqueous phase fraction, at least the oil phase fraction of the liquid reaction mixture is treated with an aqueous alkali solution to deactivate and remove the non-reacted hydrogen peroxide and the catalyst contained in at least the oil phase fraction.
    Type: Grant
    Filed: July 2, 2001
    Date of Patent: July 16, 2002
    Assignee: Ube Industries Ltd.
    Inventors: Kouhei Ninomiya, Tsunemi Sugimoto, Junichi Kugimoto, Mitsuo Yamanaka, Kohji Kaiso
  • Method for production of ethylene glycol
    Patent number: 6417411
    Abstract: In a composite process for subjecting ethylene to catalytic gas phase oxidation thereby obtaining ethylene oxide and causing this ethylene oxide to react with water thereby obtaining ethylene glycol, a method for producing the ethylene glycol is provided which permits effective utilization of the energy at the step for dehydrating and concentrating the resultant aqueous ethylene glycol solution. In the production of ethylene glycol by the supply of the aqueous ethylene glycol solution to a concentrating treatment at the multi-effect evaporator, the method contemplated by this invention for the production of ethylene glycol comprises utilizing as the source of heating at least one specific step the steam generated in the multi-effect evaporator.
    Type: Grant
    Filed: April 27, 2001
    Date of Patent: July 9, 2002
    Assignee: Nippon Shokubai Co., Ltd.
    Inventors: Yukihiko Kakimoto, Yoshihisa Oka