Patents Examined by Alan L. Rotman
  • N-acyloxylated cycloalkyl compounds, composition containing the same and methods of use therefor
    Patent number: 6713492
    Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: March 30, 2004
    Assignees: Daiichi Radioisotope Laboratories, Ltd., Yamagata Public Corporation for the Development of Industry
    Inventors: Osamu Itoh, Heitaro Obara, Hidekatsu Yokoyama, Masaaki Aoyama
  • Compound having antimalarial activity
    Patent number: 6710074
    Abstract: An object of the present invention is to provide a novel compound having antimalarial acitivity and an antimalarial agent containing the novel compound as an active component. An antimalarial agent containing 12-hidroxy-2-(1-methoxy-carbonylethyl)-5-oxo-10,11,13-trioxatricyclo[7.2.0.01,6]tridecane represented by a following formula (II) as an active agent is prepared.
    Type: Grant
    Filed: August 30, 2002
    Date of Patent: March 23, 2004
    Assignee: Japan Science and Technology Corporation
    Inventors: Masataka Ihara, Kiyosei Takasu, Yusuke Wataya, Hye-Sook Kim
  • Preparation of hydroxyalkylcarbamates from six-membered cyclic carbonates
    Patent number: 6710203
    Abstract: A method of preparing hydroxyalkylcarbamates from six-membered cyclic carbonates. The method involves reacting a six-membered cyclic carbonate with anhydrous ammonia or aqueous ammonium hydroxide. The present invention also provides for hydroxyalkylcarbamates prepared from six-membered cyclic carbonates, and for coating compositions comprising hydroxyalkylcarbamates prepared according to the present invention.
    Type: Grant
    Filed: May 23, 2001
    Date of Patent: March 23, 2004
    Assignee: Huntsman Petrochemical Corporation
    Inventors: John H. Clements, Howard P. Klein, Edward T. Marquis, James R. Machac, Jr.
  • Activators of PPAR delta
    Patent number: 6710063
    Abstract: Compounds of Formula (1) are disclosed. These compounds include selective activators of human PPAR delta.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: March 23, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Esther Yu-Hsuan Chao, Curt Dale Haffner, Millard Hurst Lambert, III, Patrick Reed Maloney, Michael Lawrence Sierra, Daniel David Sternbach, Marcos Luis Sznaidman, Timothy Mark Willson, Huaqiang Eric Xu
  • Process for production of high-purity bis-&bgr;-hydroxyethyl terephthalate
    Patent number: 6710202
    Abstract: To provide a process for producing a high-purity bis-&bgr;-hydroxyethyl terephthalate from crude terephthalic acid.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: March 23, 2004
    Assignee: Aies Co., Ltd.
    Inventors: Shuji Inada, Kikuchi Sato
  • Preparation of 2-haloacyl-3-aminoacrylic acid derivatives
    Patent number: 6706911
    Abstract: The present invention relates to an improved process for preparing 2-haloacyl-3-aminoacrylic acid derivatives and pyrazole-4-carboxylic acids and derivates thereof obtainable from it.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: March 16, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Norbert Lui, Thomas Brackemeyer, Peter Müller, Marielouise Schneider
  • Cytotoxic agents comprising taxanes and their therapeutic use
    Patent number: 6706708
    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: July 31, 2002
    Date of Patent: March 16, 2004
    Assignee: Immunogen, Inc.
    Inventors: Ravi V. J. Chari, Walter A. Blättler
  • Method and catalyst composition for producing aromatic carbonates
    Patent number: 6706908
    Abstract: The present invention provides a method and catalyst composition for carbonylating aromatic hydroxy compounds, comprising the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst composition comprising an effective amount of at least one Group 8, 9, or 10 metal source, an effective amount of a combination of inorganic co-catalysts comprising at least one Group 4 metal source and at least one Group 11 metal source, an effective amount of at least one salt co-catalyst with an anion selected from the group consisting of carboxylate, benzoate, acetate, sulfate, and nitrate, wherein the carbonylation catalyst composition is free of a halide source.
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: March 16, 2004
    Assignee: General Electric Company
    Inventors: Kirill Vladimirovich Shalyaev, Grigorii Lev Soloveichik, Donald Wayne Whisenhunt, Jr., Bruce Fletcher Johnson
  • Thiolesters and uses thereof
    Patent number: 6706729
    Abstract: This invention pertains to the discovery of a novel family of thiolesters and uses thereof. Also provided for are viricidal compounds and pharmaceutical formulations comprising these novel thiolesters. The invention also provides thiolester-inactivated viruses and thiolester-complexed viral proteins.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: March 16, 2004
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: James A. Turpin, Yongsheng Song, Ettore Appella, John K. Inman, David G. Covell, William G. Rice, Anders Wallqvist, Andrew Maynard, Mingjun Huang
  • Method for producing cyclopropanecarboxylates
    Patent number: 6706910
    Abstract: There is provided a method for producing a cyclopropanecarboxylate of formula (1): which comprises contacting a cyclopropanecarboxylate of formula (2): with a monohydroxy compound of formula (3): R7OH  (3) in the presence of a lithium compound of formula (4): R8OLi  (4), wherein R1, R2, R3, R4 and R5 each independently represent a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, or a substituted or unsubstituted aryl group; R6 represents an alkyl group having 1 to 10 carbon atoms or a substituted or unsubstituted phenyl group; R7 and R8 do not simultaneously represent the same and each independently represent a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aryl group.
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: March 16, 2004
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kazunori Iwakura, Hiroshi Souda, Tohei Takagaki, Yoshimi Yamada
  • Methods of making pyrrolidones
    Patent number: 6706893
    Abstract: The present invention provides methods for making N-methylpyrrolidine and analogous compounds via hydrogenation. Novel catalysts for this process, and novel conditions/yields are also described. Other process improvements may include extraction and hydrolysis steps. Some preferred reactions take place in the aqueous phase. Starting materials for making N-methylpyrrolidine may include succinic acid, N-methylsuccinimide, and their analogs.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: March 16, 2004
    Assignee: Battelle Memorial Institute
    Inventors: Todd Werpy, John G. Frye, Jr., Yong Wang, Alan H. Zacher
  • Heteroaryl derivatives and their use as medicaments
    Patent number: 6706722
    Abstract: The invention relates to novel acridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: March 16, 2004
    Assignee: Zentaris AG
    Inventors: Peter Emig, Eckhard Günther, Bernd Nickel, Gerhard Bacher, Silke Baasner, Thomas Beckers, Beate Aue
  • 3-cyano-2,4,5-trifluoro-benzoyl fluoride and intermediate products for the production thereof
    Patent number: 6706918
    Abstract: The present invention relates to 3-cyano-2,4,5-trifluorobenzoyl fluoride and to intermediates for its preparation and to the process for the preparation of 3-cyano-2,4,5-trifluoro-benzoyl fluoride, which starts from 5-fluoro-1,3-xylene (VIII); which is bichlorinated in the ring in the presence of a catalyst under ionic conditions to give 2,4-dichloro-5-fluoro-1,3-dimethylbenzene (VII). The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene (VI).
    Type: Grant
    Filed: October 22, 2002
    Date of Patent: March 16, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Albrecht Marhold, Peter Wolfrum
  • Indolinone derivatives as protein kinase/phosphatase inhibitors
    Patent number: 6706709
    Abstract: The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: March 16, 2004
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, G. Davis Harris, Xiaoyuan Li
  • Optically active amino acid derivatives and processes for the preparation of the same
    Patent number: 6706916
    Abstract: In producing optically-active amino acid benzyl esters by reacting optically-active amino acids with benzyl alcohols, hydrazines are present in the reaction system, or the compounds are reacted in the absence of oxygen, or the compounds are reacted in the absence of oxygen while hydrazines are present in the reaction system. The processes are simple and give optically-active amino acid benzyl esters of high optical purity.
    Type: Grant
    Filed: August 17, 2001
    Date of Patent: March 16, 2004
    Assignee: Toray Fine Chemicals Co., Ltd.
    Inventors: Haruyo Sato, Takae Ohno, Shiho Iwata
  • Substituted bicyclic heteroaryl compounds and their use as integrin antagonists
    Patent number: 6706738
    Abstract: The invention is directed to physiologically active compounds of general formula (I): R1Z1—Het—L1—Ar1—L2—Y  (I) wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; Z1 represents a direct bond, an alkylene chain, NR4, O or S(O)n; L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z3)—NR4—, —NR4—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z3)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—,
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: March 16, 2004
    Assignee: Aventis Pharma Limited
    Inventors: David Edward Clark, Paul Robert Eastwood, Neil Victor Harris, Clive McCarthy, Andrew David Morley, Stephen Dennis Pickett
  • Preparing method of 2-phenylalkanoic acid derivatives
    Patent number: 6706917
    Abstract: The present invention relates to a preparing method of 2-phenylalkanoic acid derivatives and more particluarly, to the preparing method of 2-phenylalkanoic acid derivatives expressed by formula (1) from 5,6-dihydro-2(4H)-benzofuranone as a starting material in the presence of a catalyst, organic acid alkali metal salt, in a mild condition, wherein R1 prepresents benzoyl, naphthoyl, nicotinoyl, furoyl or thenoyl group; and R2 prepresents a hydrogen atom or C1-C6 alkyl group.
    Type: Grant
    Filed: July 3, 2002
    Date of Patent: March 16, 2004
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Dae Whang Kim, Hae Sung Chang, Young Kwan Ko, Jae Wook Ryu, Jae Chun Woo, Dong Wan Koo
  • Benzoxazole compounds, process for the preparation thereof and herbicides
    Patent number: 6706664
    Abstract: The present invention relates to a benzoxazole compound represented by the following formula (1): wherein R1 to R4 each represents hydrogen atom, C1-6 alkyl group, C1-4 alkoxy group, C1-4 haloalkyl group, C1-4 haloalkoxy group, halogen atom, nitro group, cyano group, etc.; R5 represents C1-4 haloalkyl group, C1-4 haloalkoxy group, halogen atom, nitro group, cyano group, etc.; R6 represents hydrogen atom, halogen atom, cyano group, nitro group, etc.; R7 represents hydrogen atom, C1-6 alkyl group, C1-4 haloalkyl group, etc.; and X represents O, S, SO or SO2, a process for producing the same and a herbicide containing the same as an effective ingredient.
    Type: Grant
    Filed: October 30, 2001
    Date of Patent: March 16, 2004
    Assignee: UBE Industries, Ltd.
    Inventors: Shohei Fukuda, Akira Nakamura, Motohisa Shimizu, Tatsuo Okada, Takehiko Asahara, Satoshi Oohida
  • Compounds, their preparation and use
    Patent number: 6703401
    Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by clear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: November 27, 2001
    Date of Patent: March 9, 2004
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Process for the preparation of 5-carboxyphthalide
    Patent number: 6703516
    Abstract: There is described a process for the preparation of 5-carboxy phthalide, which comprises adding terephthalic acid to fuming sulfuric acid containing at least 20% of SO3, then adding formaldehyde to the mixture, heating the mixture at a temperature of 120-145° C. and isolating 5-carboxyphthalide from the reaction mixture.
    Type: Grant
    Filed: August 23, 2002
    Date of Patent: March 9, 2004
    Assignee: Infosint SA
    Inventors: Leone Dall'Asta, Umberto Casazza, Giovanni Cotticelli