Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/314)
  • Publication number: 20030096991
    Abstract: The invention relates to the preparation of compounds (I) 1
    Type: Application
    Filed: November 5, 2002
    Publication date: May 22, 2003
    Inventors: Gerhard Schnabel, Jan Vermehren, Lothar Willms
  • Publication number: 20030092723
    Abstract: The invention relates to a novel process for preparing known asymmetrical 4,6-bis(aryloxy)pyrimidine derivatives.
    Type: Application
    Filed: September 17, 2002
    Publication date: May 15, 2003
    Inventors: Holger Weintritt, Uwe Stelzer, Herbert Gayer, Walter Hubsch
  • Patent number: 6562759
    Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which A represents alkanediyl or alkenediyl, each of which has 2 to 5 carbon atoms and each of which is optionally substituted by cyano, halogen or by in each case optionally halogen- or C1-C4-alkoxy-substituted C1-C4-alkyl, C1-C4-alk-oxy-carbonyl or C2-C4-alkenyl or interrupted by O (oxygen), or represents cyclohexane-1,2-diyl or 1,2-phenylene, Q1 represents O (oxygen) or S (sulphur), Q2 represents O (oxygen) or S (sulphur), R1 represents hydrogen, amino or optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl having 1 to 4 carbon atoms, R2 represents optionally halogen-substituted alkyl having 1 to 4 carbon atoms, R3 represents hydrogen, halogen or optionally halogen-substituted alkyl having 1 to 4 carbon atoms, R4 represents hydrogen, cyano, carbamoyl, thiocarbamoyl or halogen, R5 represents cyano, carbamoyl, thiocarbamoyl or in each case optionally halogen-substituted alkyl or alkoxy ha
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: May 13, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Publication number: 20030087920
    Abstract: The present invention relates to novel butyne diol derivatives of the general formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of the general formula I and especially their use as endothelin receptor antagonists.
    Type: Application
    Filed: June 24, 2002
    Publication date: May 8, 2003
    Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli
  • Publication number: 20030073710
    Abstract: A compound, suitable as an alpha-2B-adrenoceptor antagoist, having a structure of formula (I) 1
    Type: Application
    Filed: July 17, 2002
    Publication date: April 17, 2003
    Inventors: Topi Joutsamo, Andrei Yurievitch Tauber, Harri Salo, Anna-Marja Hoffren, Siegfried Wurster
  • Patent number: 6548449
    Abstract: The invention relates to novel substituted phenyluraciles of the general formula (I) in which m, n, Q and R1-7 are each as defined in the description, and to processes for their preparation and to their use as herbicides.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: April 15, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Markus Dollinger, Mark Wilhelm Drewes, Ingo Wetcholowsky, Randy Allen Myers
  • Patent number: 6545007
    Abstract: A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human a composition comprising a non-nucleoside reverse transcriptase inhibitor (“NNRTI”) that is able to inhibit viral replication for periods exceeding 12, 24, or even 36 days, at concentrations below even 10 &mgr;M. In one embodiment the NNRTI is a dihydro-alkyloxy-benzyl-oxopyrimidine (DABO).
    Type: Grant
    Filed: November 19, 2001
    Date of Patent: April 8, 2003
    Assignees: Idenix (Cayman) Limited, Universita Degli Studi di Cagliari
    Inventors: Jean-Pierre Sommadossi, Martin L. Bryant, Marino Artico, Paolo La Colla
  • Publication number: 20030060626
    Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: 1
    Type: Application
    Filed: March 5, 2002
    Publication date: March 27, 2003
    Inventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
  • Patent number: 6537948
    Abstract: The present invention relates to an uracil compound of the formula [I]: [wherein, Q—R3 represents a R3-substituted group of a 5-membered or 6-membered heterocyclic ring having one or two nitrogen selected from the group consisting of moieties represented in the specification (wherein, this heterocyclic ring may be substituted with at least one kind of substituent, Y represents oxygen, sulfur, imino or C1 to C3 alkylimino, R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl, R2 represents C1 to C3 alkyl, R3 represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, OR7, SR8, N(R9)R10 or the like, X1 represents halogen, cyano, thiocarbamoyl or nitro, X2 represents hydrogen or halogen. {wherein, each of R7, R8 and R10 independently represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, C1 to C6 haloalkoxycarbonyl C1 to C6 alkyl, or the like, and R9 represents hydrogen or C1 to C6 alkyl.}.].
    Type: Grant
    Filed: January 31, 2001
    Date of Patent: March 25, 2003
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoshitomo Tohyama, Yuzuru Sanemitsu
  • Publication number: 20030055053
    Abstract: The present invention relates to compounds of the formula 1 1
    Type: Application
    Filed: June 5, 2002
    Publication date: March 20, 2003
    Inventors: Robert G. Linde, Matthew Merrill Hayward, Takushi Kaneko
  • Patent number: 6525050
    Abstract: Compounds of the formula: (where R1, R2 and R3 are defined in the specification) are inhibitors of AICARFT. These compounds, as well as their pharmaceutically acceptable salts, solvents, prodrugs, and pharmaceutically active metabolites, are useful in pharmaceutical compositions for treating diseases such as cancer.
    Type: Grant
    Filed: March 1, 2001
    Date of Patent: February 25, 2003
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: William H. Romines, III, Michael D. Varney, Cynthia L. Palmer, Ted M. Bleckman
  • Patent number: 6518425
    Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: February 11, 2003
    Assignees: Emory University, Triangle Pharmaceuticals, Inc.
    Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
  • Publication number: 20030013729
    Abstract: The present invention relates to novel hypolipidemic, antihyperglycemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
    Type: Application
    Filed: April 8, 2002
    Publication date: January 16, 2003
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Javed Iqbal, Gurram Ranga Madhavan, Saibal Kumar Das, Debnath Bhunia, Ranjan Chakrabarti, Ramanujam Rajagopalan
  • Publication number: 20030004347
    Abstract: The invention relates to compounds of the general formula 1
    Type: Application
    Filed: November 5, 2001
    Publication date: January 2, 2003
    Inventors: Martin Eberle, Andre Jeanguenat, Werner Zambach, Arthur Steiger, Saleem Farooq
  • Publication number: 20020173515
    Abstract: Novel derivatives of 5-thia- and 5-selenopyrimidinone are found to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.
    Type: Application
    Filed: October 23, 2001
    Publication date: November 21, 2002
    Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
  • Publication number: 20020169175
    Abstract: The present invention relates to pharmaceutically acceptable salts of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
    Type: Application
    Filed: February 4, 2002
    Publication date: November 14, 2002
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Om Reddy Gaddam, Chandra Sekhar Batchu, Rajender Kumar Potlapally, Ramabhadra Sarma Mamillapalli, Bheema Rao Paraselli, Naga Venkata Srinivasa Rao Mamidi
  • Patent number: 6476224
    Abstract: The invention relates to a process for preparing ar(alk)yluracils of the general formula (I) in which A represents a single bond or represents alkanedlyl, Ar represents optionally substituted aryl, R1 represents optionally substituted alkyl and R2 represents hydrogen, halogen or alkyl, and to novel intermediates for this purpose and to processes for their preparation.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: November 5, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Gallenkamp, Reinhard Lantzsch, Lothar Rohe, Lubbertus Mulder
  • Patent number: 6462195
    Abstract: Compounds having one or more structures represented by general formula (I) as partial structure thereof, which are typified by pyrimidone and pyridone compounds, have two or more reaction sites in alkylation reactions. Accordingly, there is no process for producing O-alkylated products of these compounds at a high selectivity or such processes, if any, are applicable exclusively to those having limited structures. A process for selectivity O-alkylating such a compound as described above by converting it into the copper salt by using a monovalent copper compound such as copper suboxide and then reacting it with an alkylating agent having a leaving group in the presence of a phosphorus compound such as a phosphite. Pyrimidyloxy derivatives or pyridyloxy derivatives obtained by this reaction is useful as intermediates of pesticides or drugs.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: October 8, 2002
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Mitsuru Takase, Yasuyuki Miyazawa, Shiro Tsubokura
  • Patent number: 6455697
    Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides.
    Type: Grant
    Filed: January 16, 2001
    Date of Patent: September 24, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6451740
    Abstract: The present invention relates to an uracil compound of the formula [I]: wherein W represents oxygen, sulfur, imino or C1 to C3 alkylimino; Y represents oxygen, sulfur, imino or C1 to C3 alkylimino; R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl; R2 represents C1 to C3 alkyl; R4 represents hydrogen or methyl; R5 represents C1 to C6 alkyl, C1 to C6 haloalkyl, or the like; X1 represents halogen, cyano or nitro; X2represents hydrogen or halogen; and each of X3 and X4 independently represents hydrogen, halogen, C1 to C6 alkyl, or the like. The present compound has an excellent herbicidal activity.
    Type: Grant
    Filed: December 5, 2000
    Date of Patent: September 17, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoshitomo Tohyama, Yuzuru Sanemitsu, Tomohiko Gotou
  • Patent number: 6448203
    Abstract: The invention relates to novel substituted aryluracils of the formula (I): to processes for their preparation and to their use as crop protection agents.
    Type: Grant
    Filed: October 7, 1999
    Date of Patent: September 10, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Markus Dollinger, Christoph Erdelen
  • Patent number: 6444616
    Abstract: The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R1, R2, R3, R4 and R5 are each as defined in the description, to a process for their preparation and to their use as herbicides.
    Type: Grant
    Filed: August 1, 2000
    Date of Patent: September 3, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark-Wilhelm Drewes, Roland Andree, Markus Dollinger
  • Patent number: 6440984
    Abstract: There are provided compositions and methods comprising compounds of formula I: wherein R1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: August 27, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
  • Patent number: 6436989
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Grant
    Filed: December 24, 1997
    Date of Patent: August 20, 2002
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Michael R. Hale, Roger D. Tung, Christopher T. Baker, Andrew Spaltenstein
  • Publication number: 20020103213
    Abstract: Pyrimidone compounds of formula (I): 1
    Type: Application
    Filed: February 14, 2001
    Publication date: August 1, 2002
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
  • Publication number: 20020103215
    Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
    Type: Application
    Filed: January 8, 2002
    Publication date: August 1, 2002
    Applicant: DR. REDDY'S RESEARCH FOUNDATION & REDDY-CHEMINOR, INC.
    Inventors: Ranga Madhavan Gurram, Venkateswarlu Akella, Rajagopalan Ramanujam, Ranjan Chakrabarti, Parimal Misra, Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli
  • Publication number: 20020099207
    Abstract: The invention relates to compounds of the formula 1
    Type: Application
    Filed: October 15, 2001
    Publication date: July 25, 2002
    Inventor: Heinz Stadler
  • Patent number: 6417141
    Abstract: The invention relates to novel aminouracils of the general formula (I) in which, Q, R1, R2, R3, R4, R5, R6 and R7 are each as defined in the description, to their use as herbicides and to novel intermediates.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: July 9, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Otto Schallner, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6417192
    Abstract: A group of novel pyrimidone compounds are inhibitors of the enzyme LDL PLA2 and therefore of use in treating atherosclerosis.
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: July 9, 2002
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Roderick Alan Porter, Stephen Allan Smith
  • Publication number: 20020086872
    Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including componds of the Formula VII: 1
    Type: Application
    Filed: December 12, 2001
    Publication date: July 4, 2002
    Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
  • Patent number: 6410484
    Abstract: A 5,6-dihydrouracil compound given by the formula [I]: wherein, R1 represents C1-C2 haloalkyl group and Q represents Q1 of the formula below, etc.: wherein, R3 is hydrogen atom or halogen atom, R15 is C3-C6 alkynyl group, etc., Z is oxygen atom, sulfur atom or NH group, and T is direct bond or methylene group, has an excellent herbicidal efficacy.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: June 25, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Minoru Takano, Hirofumi Mishima
  • Patent number: 6403534
    Abstract: The present invention provides an uracil compound of the formula: wherein A1 represents amino or C1-C3 alkyl, A2 represents C1-C3 haloalkyl, X represents hydrogen or halogen, Y represents halogen, R1 represents —OR21, —ON(R22)R23, —ON═C(R24)R25, —SR26, —N(R27)R28, —N(29)OR30, —N(R31)SO2R32 or —N(R33)N(R34)R35, and R2, R3, R4 and R5 independently represent hydrogen or C1-C3 alkyl and a herbicidal composition comprising the above uracil compound as an active ingredient. The uracil compound has excellent herbicidal activity.
    Type: Grant
    Filed: June 28, 2001
    Date of Patent: June 11, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takashi Komori, Yuzuru Sanemitsu
  • Patent number: 6391826
    Abstract: The present invention relates to an optically active uracil compounds of the formula (I): wherein, R1 is C1-C8 alkyl or C3-C8 alkenyl, and * represents an asymmetric carbon atom whose configuration is R. The compounds have excellent herbicidal activity.
    Type: Grant
    Filed: December 23, 1999
    Date of Patent: May 21, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Yuzuru Sanemitsu
  • Patent number: 6376504
    Abstract: Novel phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity as well as anti-viral activity. These novel compounds can be incorporated within contraceptive compositions to provide for spermicidal or sperm-immobilizing activity.
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: April 23, 2002
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Osmond D'Cruz
  • Patent number: 6372691
    Abstract: The present invention relates to a method for controlling weeds in corn field which comprises applying a herbicidal composition comprising 2-[2-chloro-4-fluoro-5-{3-methyl-2,6-dioxo-4-(trifluoromethyl)-1,2,3,6-tetrahydropyrimidin-1-yl}phenoxy]propionic acid ester as an active ingredient to corn fields after seeding corn. According to the present method, kinds of weeds in corn fields can be controlled widely and no problematic phytotoxicity to corn is caused.
    Type: Grant
    Filed: December 14, 2000
    Date of Patent: April 16, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Nobuaki Mito
  • Patent number: 6369066
    Abstract: This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): wherein; R1 is hydrogen, and R2 is cytosine or 5-fluorocytosine; and pharmaceutically acceptable salts and esters thereof. This invention also relates to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents, particularly in combination therapy.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: April 9, 2002
    Assignee: BioChem Pharma, Inc.
    Inventors: Tarek S. Mansour, Haolun Jin
  • Patent number: 6362337
    Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: March 26, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Otto Schallner, Katharina Voigt, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6350753
    Abstract: Nucleoside analogues containing a 1,3-dioxolane structure are suitable antiviral agents, particulary for the treatment of the HIV infections in mammals, especially humans. Examples of the nucleoside analogues include: cis-2-acetoxymethyl-4-(thymin-1′-yl)-1,3,-dioxolane, cis-2-hydroxymethyl-4-(thymin-1′-yl)-1,3-dioxolane, cis-2-benzoyloxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane, and cis-2-hydroxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane. These compounds can be in the form of their racemates or their separate enantiomers.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: February 26, 2002
    Assignee: Biochem Pharma Inc.
    Inventors: Bernard Belleau, Dilip M. Dixit, Paul Nguyen-Ba
  • Publication number: 20020016324
    Abstract: The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).
    Type: Application
    Filed: May 4, 2001
    Publication date: February 7, 2002
    Applicant: DR. REDDY'S RESEARCH FOUNDATION
    Inventors: Srinivas Nanduri, Sriram Rajagopal, Venkateswarlu Akella
  • Patent number: 6344460
    Abstract: The present invention provides compounds comprising propynyl uracils having the formula wherein R1 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R2 is iodine or bromine; and R3 is propynyl, 3-iodopropynyl, 3-bromopropynyl, substituted or unsubstituted 2-furanyl, substituted or unsubstituted 3-furanyl, substituted or unsubstituted 2-pyrrolidinyl, substituted or unsubstituted 3-pyrrolidinyl, D-ribose, or deoxyribose. Another embodiment of the invention encompasses propynyl uracils having the formula wherein R4 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R5 is hydrogen or propynyl; and R6 is iodine or bromine. Also, methods of preparing these propynyl uracils are provided.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: February 5, 2002
    Assignee: Lonza Inc.
    Inventor: Peter C. Nirchio
  • Patent number: 6339155
    Abstract: The uracil compounds represented by the formula [V]: wherein R1 represents C1-C5 perfluoroalkyl group and Q represents an aromatic group, can be produced by making the amide compounds represented by the formula [II]: wherein R1 and Q have the same meanings defined above, or its hydrate react with a cyanate salt in the presence of a protonic acid.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: January 15, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Minoru Takano, Hirofumi Mishima
  • Patent number: 6333296
    Abstract: Diaryl ether compounds useful in the control of weeds are described. An exemplary compound is represented by the general formula (I): In this formula Q is represented by Q9: X and Y represent a hydrogen atom, halogen atom, cyano group, nitro group or (C1-6)haloalkyl group. A1 and A2 are independently oxygen or sulfur atoms. R9 and R10 represent a hydrogen atom, a (C1-6)alkyl group, an acyl group, or a (C1-6)alkylsulfonyl group; or R9 and R10 may form a ring consisting of polymethylene, (CH2)m groups, where m is an integer of 2, 3, 4 or 5, together with the nitrogen atom of NR9R10, which may or may not have a (C1-6)alkyl substituent. Methods of making the compounds are also described.
    Type: Grant
    Filed: September 10, 1999
    Date of Patent: December 25, 2001
    Assignee: ISK Americas Incorporated
    Inventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Hiroshi Shimoharada, Masamitsu Tsukamoto
  • Patent number: 6329522
    Abstract: The invention relates to a diastereoselective process for the preparation of compounds of formula (1), wherein W is S, S═O, SO2 or O; X is S, S═O, SO2 or O; R1 is hydrogen or acyl, and R2 is a purine or pyrimidine base or an analogue or derivative thereof.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: December 11, 2001
    Assignee: Glaxo Group Limited
    Inventors: Malcolm Leithead Hill, Andrew Jonathan Whitehead, Roy Hornby, Peter Hallett, Michael David Goodyear, P. Owen Dwyer
  • Patent number: 6313072
    Abstract: The novel compounds of formula I: (A, B, R1, R2, R3, X and m are defined in the specification) show selective herbicidal activity. The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.
    Type: Grant
    Filed: February 18, 1999
    Date of Patent: November 6, 2001
    Assignee: American Cyanamid Company
    Inventors: Stephen Scheiblich, Thomas Maier, Axel Kleemann, Helmut Siegfried Baltruschat
  • Patent number: 6297261
    Abstract: A compound having the formula (I) or a pharmaceutically acceptable salt thereof where the variables are defined in the specification are useful in the treatment of sickle-cell anemia.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: October 2, 2001
    Assignee: Neurosearch A/S
    Inventors: Palle Christophersen, Ove Pedersen
  • Publication number: 20010025108
    Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: 1
    Type: Application
    Filed: May 4, 2001
    Publication date: September 27, 2001
    Applicant: Berlex Laboratories, Inc.
    Inventor: Gary B. Phillips
  • Publication number: 20010023291
    Abstract: This invention is directed to polyhydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: 1
    Type: Application
    Filed: May 4, 2001
    Publication date: September 20, 2001
    Applicant: Berlex Laboratories, Inc.
    Inventor: Gary B. Phillips
  • Publication number: 20010018441
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: March 12, 2001
    Publication date: August 30, 2001
    Applicant: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Patent number: RE37623
    Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula where X is S or Se; Y is H, I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R1 is H or an acyclo tail having the general formula where R2 is H, CH2 OH or CH2 NH2; R3 is OH, NH2, or OCOCH2CH2CO2H; and R4 is O, S, or CH2. The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: April 2, 2002
    Inventors: Mahmoud H. el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
  • Patent number: RE37979
    Abstract: The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I′] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.
    Type: Grant
    Filed: October 23, 1997
    Date of Patent: February 4, 2003
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik Desiré DeClercq, Masanori Baba, Richard Thomas Walker, Masaru Ubasawa