The Hetero Ring Is Four-membered Patents (Class 549/510)
Sulfur or halogen attached directly or indirectly to the hetero ring by nonionic bonding (Class 549/511)
  • Taxane prodrugs
    Patent number: 6380405
    Abstract: The present invention generally provides taxane prodrugs comprising at least one taxane joined by hydrolyzable bond(s) to one or more polyethylene glycol oligomer(s) selected from the group consisting of a straight or branched polyethylene glycol oligomer having from 1 to 25 polyethylene glycol units and optionally comprising a salt-forming moiety. The polyethylene glycol oligomer preferably comprises a salt-forming moiety, which is preferably selected from the group consisting of ammonium and carboxylate.
    Type: Grant
    Filed: December 31, 1999
    Date of Patent: April 30, 2002
    Assignee: Nobex Corporation
    Inventors: Nnochiri Ekwuribe, Gary S. Bartley, Christopher H. Price
  • Family of canadensol taxanes, the semi-synthetic preparation and therapeutic use thereof
    Publication number: 20020045771
    Abstract: The present invention relates to a new taxane having the structure as in formula I and its analogs as depicted in Formula II and Formula III. The invention includes novel semisynthetic and isolation methods for the preparation of these novel taxanes. Specifically, the present invention relates to the new taxane Canadensol isolated from plants of the Taxus genus, in particular, Taxus canadensis. The present invention further relates to the use of these new taxanes as anticancer agents.
    Type: Application
    Filed: October 16, 2001
    Publication date: April 18, 2002
    Applicant: Institut National de la Recherche Scientifique
    Inventors: Lolita Zamir, Gaeton Caron, Yi Feng Zheng
  • Novel cephalotaxane derivatives and process for their preparation
    Publication number: 20020045750
    Abstract: The present invention concerns a new general process for asymetric hemisynthesis of harringtonines and their analogs, that are alcaloïds used in chimiotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and fonctionalization are entirely preformed.
    Type: Application
    Filed: March 27, 2001
    Publication date: April 18, 2002
    Inventors: Jean-Pierre Robin, Julie Blanchard, Sylvie Cavoleau, Ludovic Chauviat, Sandra Charbonnel, Robert Dhal, Gilles Dujardin, Florence Fournier, Chrystelle Gilet, Laurent Girodier, Laurence Mevelec, Sandrine Poutot, Sylvie Rouaud
  • Efficient process for the production of 10-DAB III by selective hydrazinolysis of various taxanes
    Publication number: 20020042529
    Abstract: The present invention describes a process for producing 10-deacetyl baccatin III from a solution containing a solvent reactive with hydrazine hydrate and a spectrum of taxanes. The solution is contacted with hydrazine hydrate thereby converting some taxanes therein into 10-deacetyl baccatin III. The process can target taxanes having an ester functionality on at least one of the C-10 and C-13 positions. The hydrazine hydrate cleaves the ester functionality of the taxane solute. The process may be used to produce 10-deacetyl baccatin III from a biomass extract by contacting the biomass extract with a mixture of a solvent and a hydrazine hydrate. The solvent may have a functional group that is cleaved by hydrazine acetate. Acetate solvents are contemplated.
    Type: Application
    Filed: July 5, 2001
    Publication date: April 11, 2002
    Inventors: Madhavi C. Chander, James D. McChesney
  • Method of locking 1 &agr;-OH of vitamin D compounds in axial orientation
    Patent number: 6369099
    Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.
    Type: Grant
    Filed: April 20, 2000
    Date of Patent: April 9, 2002
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal R. Sicinski
  • C13 amido substituted taxane derivatives and pharmaceutical compositions containing them
    Patent number: 6369244
    Abstract: Taxane derivatives having an amino substituted C13 side chain.
    Type: Grant
    Filed: March 10, 2000
    Date of Patent: April 9, 2002
    Assignee: Florida State University
    Inventors: Robert A. Holton, Hossain Nadizadeh, Kasthuri Rengan, Chunlin Tao
  • Radiosensitizing taxanes and their pharmaceutical preparations
    Publication number: 20020040155
    Abstract: Taxanes containing electron-affinic radiosensitizing functional groups, their pharmaceutical preparations, and methods of making and using this new class of highly potent radiosensitizers of tumor cells.
    Type: Application
    Filed: October 16, 2001
    Publication date: April 4, 2002
    Applicant: Florida State University
    Inventors: Robert A. Holton, Hossain Nadizadeh, Kurt G. Hofer, Li-Xi Yang
  • Naphthalene derivative, binaphthalene derivative and biphenyl derivative and cationically curable compound
    Patent number: 6365760
    Abstract: A naphthalene derivative, binaphthalene derivative and biphenyl derivative, all having an oxetane group, capable of being cationically polymerized and a cationically curable compound containing a naphthalene derivative having an oxetanyl group and an aromatic compound having an epoxy group or an oxetanyl group.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: April 2, 2002
    Assignee: Toagosei Co., Ltd.
    Inventors: Akira Kuriyama, Naokazu Ito, Tetsuya Suzuta, Takashi Tsuda
  • Methods for the preparation of taxanes using oxazolidine intermediates
    Patent number: 6365750
    Abstract: Novel oxazolidines finding utility as intermediates in the preparation of C-13 acyloxy sidechain-bearing taxanes such as paclitaxel and analogs thereof. The present invention also relates to novel methods of coupling the oxazolidines to form the aforementioned taxanes, and to methods of preparing the oxazolidines.
    Type: Grant
    Filed: May 20, 1999
    Date of Patent: April 2, 2002
    Assignee: Bristol Myers Squibb Comp.
    Inventors: John K. Thottathil, Ivan D. Trifunovich
  • Methods for treating pathological conditions of abnormal cell proliferation
    Publication number: 20020038038
    Abstract: New taxoids of general formula (I): 1
    Type: Application
    Filed: September 25, 2001
    Publication date: March 28, 2002
    Applicant: Aventis Pharma S.A.
    Inventors: Herve Bouchard, Jean-Dominique Bourzat, Alain Commercon
  • Taxane anticancer agents
    Patent number: 6362217
    Abstract: The present invention concerns novel 7-deoxy taxane derivatives their use as antitumor agents, and pharmaceutical formulations.
    Type: Grant
    Filed: March 8, 2001
    Date of Patent: March 26, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: John F. Kadow, Wendy S. Schwartz, Paul M. Scola, Qiufen May Xue, Mark D. Wittman, Mu-Jen Wu
  • Stable isotope labeling of paclitaxel
    Patent number: 6358996
    Abstract: A chemical compound comprising an isotopically labeled analog of a standard taxane molecule, wherein said isotopically labeled analog is synthetically formed to have incorporated therein at a selected position a stable isotope of an element existing at said selected positon in said standard taxane molecule, said isotope having amass different form a mass of a mass of a most abundantly occurring isotope of said element in nature, such that said isotopically labeled analog has a molecular weight different form a molecular weight of said standard taxane molecule.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: March 19, 2002
    Assignee: NaPro BioTherapeutics, Inc.
    Inventors: Michael S. Alexander, James D. McChesney, Jan Zygmunt
  • C7 carbamoyloxy substituted taxanes
    Patent number: 6359154
    Abstract: Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: March 19, 2002
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Hydrolytic kinetic resolution of cyclic substrates
    Publication number: 20020032338
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Application
    Filed: July 5, 2001
    Publication date: March 14, 2002
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Process for the preparation of a paclitaxel C-4 methyl carbonate analog
    Patent number: 6353120
    Abstract: A process for the synthesis of a C-4 methyl carbonate paclitaxel analog from 10-deacetylbaccatin III by the selective reduction of the acetate at the C-4 position of 10-deacetylbaccatin using Red-Al.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: March 5, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventor: Joydeep Kant
  • &bgr;-lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes
    Patent number: 6350886
    Abstract: Novel &bgr;-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling &bgr;-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: February 26, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: John K. Thottathil, Ivan D. Trifunovich, David J. Kucera, Wen-Sen Li
  • &bgr;-lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes
    Patent number: 6350887
    Abstract: Novel &bgr;-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling &bgr;-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: February 26, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: John K. Thottathil, Ivan D. Trifunovich, David J. Kucera, Wen-Sen Li
  • Taxoid anti-tumor agents and pharmaceutical compositions thereof
    Publication number: 20020022651
    Abstract: Pharmaceutical compositions, methods of administration, and methods of treatment of cancer with new generation taxoids, of formulas (I) and (II), and derivatives thereof, are described: 1
    Type: Application
    Filed: April 2, 2001
    Publication date: February 21, 2002
    Inventor: Iwao Ojima
  • Stabilization of taxane-containing dispersed systems
    Patent number: 6348215
    Abstract: The invention provides a method of stabilizing a taxane in a dispersed system, which method comprises exposing the taxane to a molecule which improves physical stability of the taxane in the dispersed system. By improving physical stability of the taxane in the dispersed system, higher taxane content can be achieved. The invention thus further provides a stable taxane-containing liposome preparation comprising a liposome containing one or more taxanes present in the liposome in an amount of less than 20 mol % total taxane to liposome, wherein the liposome is suspended in a glycerol:water composition having at least 30% glycerol.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: February 19, 2002
    Assignee: The Research Foundation of State University of New York
    Inventors: Robert M. Straubinger, Sathyamangalam V. Balasubramanian
  • Water soluble tri-substituted 1,2-dioxetane compounds having increased storage stability, synthetic processes and intermediates
    Publication number: 20020019553
    Abstract: Stable, enzymatically triggered chemiluminescent 1,2-dioxetanes with improved water solubility and storage stability are provided as well as synthetic processes and intermediates used in their preparation. Dioxetanes further substituted with two or more water-solubilizing groups disposed on the dioxetane structure and an additional fluorine atom or lower alkyl group provide superior performance by eliminating the problem of reagent carryover when used in assays performed on capsule chemistry analytical systems. These dioxetanes display substantially improved stability on storage. Compositions comprising these dioxetanes, a non-polymeric cationic surfactant enhancer and optionally a fluorescer, for providing enhanced chemiluminescence are also provided.
    Type: Application
    Filed: April 20, 2001
    Publication date: February 14, 2002
    Inventors: Hashem Akhavan-Tafti, Renuka DeSilva, Kumar Thakur, Zahra Arghavani
  • Taxane anticancer agents
    Publication number: 20020016356
    Abstract: The present invention concerns novel 7-deoxy taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.
    Type: Application
    Filed: March 8, 2001
    Publication date: February 7, 2002
    Inventors: John F. Kadow, Wendy S. Schwartz, Paul M. Scola, Qiufen May Xue, Mark D. Wittman, Mu-Jen Wu
  • Water soluble analogs and prodrugs of paclitaxel
    Patent number: 6344571
    Abstract: The invention relates to water soluble antitumor analogs of paclitaxel of formula (I) wherein R1=C(O)CH2CH(OH)COOX, R2=H, C(O)CH2CH(OH)COOX, X=H, Li, Na or any other pharmaceutically acceptable counterion, as well as to a pharmaceutical composition comprising an antineoplastically effective amount of such analogs as an active ingredient.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: February 5, 2002
    Assignee: Pharmachemie B.V.
    Inventors: Peter H. G. Wiegerinck, Duncan Sperling, Lesly Braamer, Eric W. P. Damen, Johan W. Scheeren, Dick de Vos
  • Taxane prodrugs
    Publication number: 20020013484
    Abstract: Taxane prodrugs comprise a taxane joined by a hydrolyzable bond to one or more oligomers that comprise a polyethylene glycol moiety. The oligomer preferably further comprises a salt-forming moiety.
    Type: Application
    Filed: March 9, 2001
    Publication date: January 31, 2002
    Inventors: Nnochiri N. Ekwuribe, Christopher H. Price, Gary S. Bartley
  • C7 ester substituted taxanes
    Publication number: 20020013346
    Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Application
    Filed: February 2, 2001
    Publication date: January 31, 2002
    Inventor: Robert A. Holton
  • Cytotoxic agents comprising taxanes and their therapeutic use
    Publication number: 20020013485
    Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
    Type: Application
    Filed: August 21, 2001
    Publication date: January 31, 2002
    Inventors: Ravi V.J. Chari, Walter A. Blattler
  • Nitrosated and nitrosylated taxanes, compositions and methods of use
    Publication number: 20020010146
    Abstract: The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The present invention also provides novel compositions comprising at least one taxane and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The compounds and compositions of the present invention can also be bound to a matrix.
    Type: Application
    Filed: June 22, 2001
    Publication date: January 24, 2002
    Inventors: David S. Garvey, L. Gordon Letts, Chia-En Lin, Stewart K. Richardson, Tiansheng Wang
  • Methods for preparing new taxoids and pharmaceutical compositions containing them
    Publication number: 20020010348
    Abstract: Methods of preparing methylthiomethyloxy taxoids of formula (XXXIV) 1
    Type: Application
    Filed: March 5, 2001
    Publication date: January 24, 2002
    Inventors: Herve Bouchard, Jean-Dominique Bourzat, Alain Commercon, Iwao Ojima
  • Cytotoxic agents comprising taxanes and their therapeutic use
    Patent number: 6340701
    Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: January 22, 2002
    Assignee: Immunogen INC
    Inventors: Ravi V. J. Chari, Walter A. Blättler
  • Arylsulfonylamino hydroxamic acid derivatives
    Publication number: 20020006920
    Abstract: A compound of the formula 1
    Type: Application
    Filed: July 18, 2001
    Publication date: January 17, 2002
    Inventors: Ralph Pelton Robinson, Kim Francis McClure
  • C2 substituted phenyl taxane derivatives and pharmaceutical compositions containing them
    Patent number: 6339164
    Abstract: Taxane derivatives having alternative C2 substituents.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: January 15, 2002
    Assignee: Florida State University
    Inventors: Robert A. Holton, Chunlin Tao
  • Process for the extraction of a compound by a fluorocarbon compound
    Publication number: 20020004079
    Abstract: A process for extracting a compound or composition of matter from a raw material containing that compound or composition as a constituent part is described. The process comprises the steps of (1) contacting a sample of the raw material with an extraction solvent comprising a C1-4 (hydro)fluorocarbon alone or with a co-solvent, and (2) separating the solvent liquor thus obtained containing the extract from the raw material. The process may be used to extract natural products, such as flavored or aromatic oils, and biologically active compounds, such as pesticides and pharmaceuticals.
    Type: Application
    Filed: April 26, 2001
    Publication date: January 10, 2002
    Inventors: Richard Llewellyn Powell, Timothy James Noakes
  • C7 TAXANE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20020002292
    Abstract: Taxane derivatives having alternative C7 substituents.
    Type: Application
    Filed: October 25, 1999
    Publication date: January 3, 2002
    Inventors: ROBERT A. HOLTON, KI-BYUNG CHAI
  • Taxanes having an alkyl substituted side-chain and pharmaceutical compositions containing them
    Patent number: 6335362
    Abstract: Taxane derivatives having an alkyl substituted C13 side chain.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: January 1, 2002
    Assignee: Florida State University
    Inventors: Robert A. Holton, Ki-byung Chai, Hamid Idmoumaz, Hossain Nabizadeh, Yukio Suzuki
  • Chromatographic separation method of paclitaxel and cephalomannin
    Patent number: 6333419
    Abstract: A method for separating paclitaxel from cephalomannin and other related compounds by obtaining a starting material that contains paclitaxel and cephalomannin; dissolving the starting material in any one of a number of particularly defined solvents such as butyl formate and butyl acetate to form a mixture; subjecting the mixture to column chromatography to obtain an eluted fraction of paclitaxel, an eluted fraction of cephalomannin and a residue; and separately drying the paclitaxel and cephalomannin fractions to obtain separate crystalline forms of paclitaxel and cephalomannin, respectively.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: December 25, 2001
    Assignee: Indena SpA
    Inventors: Bruno Gabetta, Gianfranco Zini
  • Taxoids, their preparation and pharmaceutical compositions containing them
    Patent number: 6331635
    Abstract: New taxoids of general formula (I): their preparation and pharmaceutical compositions containing them. The new products of general formula (I) in which Z represents a radical of general formula (II): display noteworthy antitumour and antileukaemic properties.
    Type: Grant
    Filed: April 28, 1998
    Date of Patent: December 18, 2001
    Assignee: Aventis Pharma S.A.
    Inventors: Hervé Bouchard, Jean-Dominique Bourzat, Alain Commerçon
  • Methods of treating cell lines expressing multidrug resistance P-glycoprotein
    Publication number: 20010051736
    Abstract: New taxoids of general formula (I): 1
    Type: Application
    Filed: January 3, 2001
    Publication date: December 13, 2001
    Applicant: Rhone-Poulenc Rorer,S.A.
    Inventors: Herve Bouchard, Jean-Dominique Bourzat, Alain Commercon
  • C7 carbamoyloxy substituted taxanes
    Publication number: 20010051640
    Abstract: Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10, and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Application
    Filed: February 2, 2001
    Publication date: December 13, 2001
    Inventor: Robert A. Holton
  • C10 ester substituted taxanes
    Publication number: 20010051639
    Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Application
    Filed: February 2, 2001
    Publication date: December 13, 2001
    Inventor: Robert A. Holton
  • Benzopyranyl guanidine derivatives, process for preparation thereof, and pharmaceutical compositions containing them
    Patent number: 6323238
    Abstract: The present invention relates to novel benzopyranyl guanidine derivatives of the formula 1, process for preparation therof and pharmaceutical use of the benzopyranyl guanidine derivatives. The benzopyranyl guanidine derivatives of the present invention can be used for protecting heart, neuronal cell or brain damage, preserving organs, and also the benzopyranyl guanidine derivatives are pharmacologically useful for inhibiting NO generation, and for suppressing lipid peroxidation, angiogenesis or restenosis. Wherein R1, R2, R3, R4, R5, R6, n and * are each defined in specification.
    Type: Grant
    Filed: October 20, 2000
    Date of Patent: November 27, 2001
    Assignee: Dongbu Hannong Chemical Co., Ltd.
    Inventors: Sung-Eun Yoo, Kyu Yang Yi, Sun Kyung Lee, Nak-Jeong Kim, Jee Hee Suh, Young Sook Park, Sun Kyung Hwang, Hwa Sup Shin, Byung Ho Lee, Ho Won Seo, Hong Lim, Sun-Ok Kim, In Sun Cho, Miae Namgoong, Dongsoo Jang
  • Kit for conducting an assay to detect a substance using enzymatically-induced decomposition of dioxetanes
    Patent number: 6322727
    Abstract: A kit for detecting a first substance in a sample including a stabilized 1,2-dioxetane bearing an enzyme-labile substituent, which is destabilized and caused to decompose by contacting the 1,2-dioxetane with an enzyme under conditions which cause the enzyme to cleave the enzyme-labile group from the dioxetane, thereby yielding a negatively charged oxygen anion bonded to the 1,2-dioxetane, which causes the 1,2-dioxetane to decompose without input from an external excitation energy source, the decomposition being accompanied by chemiluminescence; and a second component selected from the group consisting of a specific affinity substance (e.g., an antigen, an antibody or a nucleic acid probe) and an enzyme which destabilizes said 1,2-dioxetane.
    Type: Grant
    Filed: March 29, 2000
    Date of Patent: November 27, 2001
    Assignee: Tropix, Inc.
    Inventor: Irena Y. Bronstein
  • Process for the preparation of a paclitaxel C-4 methyl carbonate analog
    Publication number: 20010044549
    Abstract: A process for the synthesis of a C-4 methyl carbonate paclitaxel analog from 10-deacetylbaccatin III by the selective reduction of the acetate at the C-4 position of 10-deacetylbaccatin using Red-Al.
    Type: Application
    Filed: March 20, 2001
    Publication date: November 22, 2001
    Inventor: Joydeep Kant
  • Pentacyclic compound
    Publication number: 20010041796
    Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1).
    Type: Application
    Filed: January 16, 2001
    Publication date: November 15, 2001
    Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyma
  • Conversion of 9-dihydro-13-acetylbaccatin III to baccatin III and 10-deacetyl baccatin III
    Publication number: 20010041803
    Abstract: Novel methods and synthetic intermediates to prepare baccatin III and 10-deacetylbaccatin from readily available 9-dihydro-13-acetylbaccatin III are described. Selective protection and deprotection of the C-7 hydroxyl functionality provides an entry into facile synthesis of novel taxol intermediates, as well as, providing new methods for the preparation of paclitaxel and docetaxel in large scale. Selective oxidation of the C-9 hydroxyl without the need for protection of the C-7 hydroxyl is described.
    Type: Application
    Filed: March 19, 2001
    Publication date: November 15, 2001
    Inventors: Gertrude C. Kasitu, Japheth W. Noah
  • 2-oxetanone sizing agents and their use in paper
    Patent number: 6316095
    Abstract: Fine paper that is sized with a 2-oxetanone alkaline sizing agent and that does not encounter machine feed problems in high speed converting or reprographic machines, including continuous forms bond paper and adding machine paper, processes for converting the paper into envelopes, continuous forms bond paper and adding machine paper, and paper products of the processes.
    Type: Grant
    Filed: October 18, 1999
    Date of Patent: November 13, 2001
    Assignee: Hercules Incorporated
    Inventors: Donald K. Black, Kyle J. Bottorff, Clement Linus Brungardt, David Howard Dumas, Susan Merrick Ehrhardt, John Charles Gast, Jian-Jian Zhang
  • &bgr;-lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes
    Patent number: 6310201
    Abstract: Novel &bgr;-lactams finding utility as intermediates in the preparation of sidechain-bearing taxes such as tall and tall derivatives. The present invention also relates to novel methods of coupling &bgr;-lactams to form such sidechain-bearing taxes, and to novel sidechain-bearing taxes.
    Type: Grant
    Filed: June 11, 1999
    Date of Patent: October 30, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: John K. Thottathil, Ivan D. Trifunovich, David J. Kucera, Wen-Sen Li
  • WATER SOLUBLE PACLITAXEL DERIVATIVES
    Publication number: 20010034363
    Abstract: Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.
    Type: Application
    Filed: March 30, 1998
    Publication date: October 25, 2001
    Inventors: CHUN LI, SIDNEY WALLACE, DONG-FANG YU, DAVID J. YANG
  • Taxoid derivatives and process for producing the same
    Patent number: 6306893
    Abstract: An object of the invention is to develop galactose or mannose derivatives of docetaxel, etc. having improved solubility and physiological activity, to alleviate burden imposed on patients and to provide effective therapeutic drug for tumors. The present invention provides taxoid derivatives comprising any of paclitaxel, docetaxel and 10-deacetyl-baccatin III to which galactose or mannose is linked through a spacer, and methods for producing taxoid derivatives comprising reacting paclitaxel, docetaxel or 10-deacetyl-baccatin III with tetrabenzyl acetyloxygalactoside or tetrabenzyl acetyloxymannoside, subjecting the product to debenzylation reaction, and optionally to detriethylsilylation reaction.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: October 23, 2001
    Assignees: Ensuiko Sugar Refining Company, Ltd, Bio Research Corporation of Yokohama, Kaken Pharmaceutical Company, Ltd.
    Inventors: Tadakatsu Mandai, Hiroshi Okumoto, Koji Hara, Katsuhiko Mikuni, Kozo Hara, Yoshinori Tsuchiya, Kosho Nakamura, Teruhiko Umetsu
  • Synthesis of paclitaxel from baccatin III by protection of the 7-hydroxyl of baccatin III using a strong base and an electrophile
    Patent number: 6307071
    Abstract: Process for synthesizing paclitaxel by treating baccatin III with a strong base in a solvent, adding an electrophile to the solution to form a 7-O-protected baccatin III derivative, reacting the 7-O-protected baccatin III derivative with a protected paclitaxel sidechain in a solvent such that the protected paclitaxel sidechain is coupled to the 13-hydroxyl of the 7-O-protected baccatin III, and subsequently deprotecting the protected paclitaxel sidechain and the 7-O protecting group to form paclitaxel, and intermediates used therein.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: October 23, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventor: Francis S. Gibson
  • PHOSPHONOOXYMETHYL ETHERS OF TAXANE DERIVATIVES
    Publication number: 20010023255
    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: Application
    Filed: June 6, 1997
    Publication date: September 20, 2001
    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
  • Process for selective derivatization of taxanes
    Patent number: 6291691
    Abstract: Processes for the preparation of taxol and other taxanes through selective derivatization of the C(7) and C(10) hydroxyl groups of 10-DAB, particularly a novel process using a new strategy in which the C(10) hydroxyl group is protected or derivatized prior to the C(7) hydroxyl group; and the provision of C(7) and C(10) derivatized 10-DAB compounds.
    Type: Grant
    Filed: June 7, 2000
    Date of Patent: September 18, 2001
    Assignee: Florida State University
    Inventors: Robert A. Holton, Zhuming Zhang, Paul A. Clarke