Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/314)
  • Patent number: 7205260
    Abstract: The present invention relates to an herbicide composition comprising, as active ingredients, a uracil compound represented by the following formula (I): wherein Z represents halogen or cyano; A represents oxygen, sulfur or NH; R1 represents hydroxyl, C1–C7 alkoxy or others, and R2 represents hydrogen or methyl, and one or more compounds selected from the group consisting of N-(7-fluoro-3,4-dihydro-3-oxo-4-prop-2-ynyl-2H-1,4-benzoxazin-6-yl)cyclohex-1-ene-1,2-dicarboxamide and N-[2,4-dichloro-5-[4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1H-1,2,4-triazol-1-yl]phenyl]methanesulfonamide; and a method for controlling weeds which comprises applying an effective amounts of said herbicide composition to weeds. According to the invention, particularly weeds in orchards, soybean fields and non-crop lands can be effectively controlled.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: April 17, 2007
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Nobuaki Mito, Shinsuke Shibuya
  • Patent number: 7179815
    Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: February 20, 2007
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
  • Patent number: 7169790
    Abstract: Arylpyrimidinone compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
    Type: Grant
    Filed: June 7, 2005
    Date of Patent: January 30, 2007
    Assignee: Neurogen Corporation
    Inventors: Kevin J. Hodgetts, Dario Doller
  • Patent number: 7115544
    Abstract: A plant growth regulator for cotton harvest, which contains as an active ingredient, a compound of formula (I): wherein X is CH or nitrogen; Z is halogen; A is oxygen, sulfur, or NH; R1 is hydroxyl, C1–C7 alkoxy, C3–C7 alkenyloxy, C3–C7 alkynyloxy, C5–C7 cycloalkoxy, {(C1–C7 alkoxy)carbonyl}C1–C3 alkoxy, (C1–C7 alkylamino)oxy, {di(C1–C7 alkyl)amino}oxy, (C3–C7 alkylideneamino)oxy, C1–C7 alkylamino, di(C1–C7 alkyl)amino, C3–C7 alkenylamino, C3–C7 alkynylamino, C5–C7 cycloalkylamino, {(C1–C7 alkoxy)carbonyl}C1–C3 alkylamino, or (C1–C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1–C3 alkyl, or C1–C3 alkoxy.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: October 3, 2006
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Nobuaki Mito
  • Patent number: 7109334
    Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: September 19, 2006
    Assignee: Shire BioChem, Inc.
    Inventor: Qing Yu
  • Patent number: 7026477
    Abstract: The invention relates to a preparation process for a compound (I) or a salt thereof, in which Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) ammonolyzing a comp. (II) in which Hal=halogen atom to give (III), pref. (a1) carrying out the reaction in an organic solvent mixture (org. solv. mixture) comprising (1) opt. halogenated aromatic hydrocarbons and (2) polar aprotic solvents, in a weight ratio of solv. (1): solv. (2) of 20:1 to 1:1, (b) phosgenating the comp. (III) with phenylsulfonyl isocyanate of the formula (IV), pref. (b1) in the case X*=halogen, carrying out the reaction with phosgene in an org. solv. in the presence of isocyanates R?-NCO as catalyst, where R?=(subst.) hydrocarbon, with or without addition of an amine base, (c) reacting the resulting compound (IV) in org. solv. with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) to give the comp. (I) or a salt thereof, pref. (c1) carrying out the reaction in a solv. mixture of opt. halogenated arom.
    Type: Grant
    Filed: September 28, 2000
    Date of Patent: April 11, 2006
    Assignee: Aventis CropScience GmbH
    Inventors: Jan Vermehren, Ernst Schmidt, Mark James Ford, Richard W. G. Foster, Ian A. Bourne
  • Patent number: 6987114
    Abstract: The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or trisubstituted phenyl with a group selected from hydroxy, C1–C4 alkyl, C1–C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1–C4 alkyl, C1–C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1–C4 alkoxycarbonyl; C1–C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1–C4 alkyl, R2 and R3 represent independently hydrogen or C1–C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.
    Type: Grant
    Filed: April 8, 2000
    Date of Patent: January 17, 2006
    Assignee: Samjin Pharmaceutical Co., Ltd
    Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Jae-Eung Lee, Jeong-Ho Joo
  • Patent number: 6960568
    Abstract: The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and antibacterial applications. Preferred embodiments of the instant invention include novel 2 halogen-substituted, 3 halogen-substituted, and 2?,3?dihalogen-substituted analogues of 3-deazaadenosine, and novel 3 halogen-substituted analogues of 3-deazaguanosine. Compounds of the instant invention, including 4-Amino-6-fluoro-1-(?-D-ribofuranosyl)imidazo[4,5-c]pyridine and 6-Amino-7-bromo-1,5-dihydro-1-?-D-ribofuranosylimidazo[4,5-c]pyridin-4-one, have exhibited potent antiviral and anticancer activity in vitro. The compounds are also useful in the concomitant treatment of bacterial infections associated with viral infections such as AIDS.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: November 1, 2005
    Assignee: Yale University
    Inventors: Alan C. Sartorelli, Yung-Chi Cheng, Mao-Chin Liu
  • Patent number: 6958345
    Abstract: Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.
    Type: Grant
    Filed: August 6, 2004
    Date of Patent: October 25, 2005
    Assignees: The Regents of the University of Michigan, Wayne State University
    Inventors: Jiri Zemlicka, Yao-Ling Qiu, John C. Drach, Roger G. Ptak
  • Patent number: 6943173
    Abstract: Arylpyrimidinone compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
    Type: Grant
    Filed: July 18, 2001
    Date of Patent: September 13, 2005
    Assignee: Neurogen Corporation
    Inventors: Kevin J. Hodgetts, Dario Doller
  • Patent number: 6939965
    Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl)3Ti(isopropoxide). Using the processes described herein, the compounds can be provided as isolated enantiomers.
    Type: Grant
    Filed: February 11, 2003
    Date of Patent: September 6, 2005
    Assignees: Gilead Sciences, Inc., Emory University
    Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, José D. Soria, Marcos Sznaidman
  • Patent number: 6936602
    Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: August 30, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
  • Patent number: 6930112
    Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and epileptogenesis. Methods for preparing the compounds of the invention are also described.
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: August 16, 2005
    Assignee: Queen's University at Kingston
    Inventors: Donald F. Weaver, John R. Carran
  • Patent number: 6924271
    Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: August 2, 2005
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden
  • Patent number: 6872728
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: February 6, 2003
    Date of Patent: March 29, 2005
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
  • Patent number: 6838562
    Abstract: This invention relates to a process for the synthesis and method of use of an effective amount of a creatine heterocyclic acid salt for the regulation athletic function in humans.
    Type: Grant
    Filed: April 1, 2003
    Date of Patent: January 4, 2005
    Inventors: Sal Abraham, Shengli Jiang
  • Publication number: 20040248913
    Abstract: The present invention relates to a method of modulating retinoid X receptor activity in a mammal, novel compounds and pharmaceutical compositions for
    Type: Application
    Filed: May 26, 2004
    Publication date: December 9, 2004
    Inventors: Timothy Alan Grese, Kevin M Gardinier, Marcus F Boehm
  • Publication number: 20040242875
    Abstract: The invention relates to a process for the preparation of certain pyrimidinone compounds.
    Type: Application
    Filed: July 2, 2004
    Publication date: December 2, 2004
    Inventors: Keith Raymond Mulholland, Andrew R Ross, Graham Ralph Slater, Gillian Elizabeth Smith
  • Publication number: 20040198757
    Abstract: Compounds of the formula (I): wherein R1, R2, R3, p, q, and X are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
    Type: Application
    Filed: May 27, 2004
    Publication date: October 7, 2004
    Inventors: Nicholas John Newcombe, Andrew Peter Thomas
  • Publication number: 20040186114
    Abstract: Disclosed are compounds of formula (I) 1
    Type: Application
    Filed: February 27, 2004
    Publication date: September 23, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Matthew Russell Netherton, Kevin Chungeng Qian, Mark Stephen Ralph, Lifen Wu, Zhaoming Xiong
  • Publication number: 20040186119
    Abstract: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various GSK-3-mediated disorders, such as diabetes and Alzheimer's disease.
    Type: Application
    Filed: March 12, 2004
    Publication date: September 23, 2004
    Inventor: Young-Choon Moon
  • Patent number: 6787539
    Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceutic
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: September 7, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Heinz Stadler
  • Patent number: 6780821
    Abstract: The invention relates to new substituted phenyluracils of the general formula (I) in which n, Q, R1, R2, R3, R4, R5 and X have the meanings given in the description, to process and new intermediates for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: June 20, 2002
    Date of Patent: August 24, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky, Hans-Georg Schwarz
  • Patent number: 6734139
    Abstract: The present invention provides herbicidal active compound combinations which comprise, N-aryl-uracils and herbicidally active compounds and/or compounds which improve crop plant compatibility. The combinations find use in controlling monocotyledonous and dicotyledonous weeds in crops of useful plants.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: May 11, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Feucht, Peter Dahmen, Mark Wilhelm Drewes, Birgit Krauskopf, Mathias Kremer, Rolf Pontzen, Ingo Wetcholowsky, Roland Andree
  • Publication number: 20040063705
    Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.
    Type: Application
    Filed: August 21, 2002
    Publication date: April 1, 2004
    Inventors: Jean-Christophe Harmange, Shon Booker, John L. Buchanan, Stuart Chaffee, Perry M. Novak, Simon Van Der Plas, Xiaotian Zhu
  • Patent number: 6713486
    Abstract: 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C6-10 aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-4 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O—(C1-6 alkyl)-substituted oximino, C—1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethlyl, C1-6 alkoxymethyl, C1-6 acyloxynethyl, carbamoyloxymethyl, anminomethyl, N—(C1-3 alkyl)aminomethyl, N,N-di(C1-3 alkyl)aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl)amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl)carbamoyl, aminocarbamoyl, dimethylamin
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: March 30, 2004
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jong-Chan Son, Seun-Shil Shin, Shin-Keol Kim, Chong-Kyo Lee, Hae-Soo Kim
  • Publication number: 20040053951
    Abstract: Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated.
    Type: Application
    Filed: February 11, 2003
    Publication date: March 18, 2004
    Applicant: Pfizer Inc.
    Inventors: Lance C. Christie, Mark B. Anderson, Jun Feng, Yufeng Hong, Ved P. Pathak, Ranjan J. Rajapakse, Eileen V. Tompkins, Haresh Vazir, Haitao Li
  • Publication number: 20040044203
    Abstract: The present invention provides compounds of formula I 1
    Type: Application
    Filed: October 2, 2002
    Publication date: March 4, 2004
    Inventors: Mark D. Wittman, Neelakantan Balasubramanian, Upender Velaparthi, Kurt Zimmermann, Mark G. Saulnier, Peiying Liu, Xiaopeng Sang, David B. Frennesson, Karen M. Stoffan, James G. Tarrant, Anne Marinier, Stephan Roy
  • Patent number: 6696475
    Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: February 24, 2004
    Assignee: NeuroSearch A/S
    Inventors: Bjarne H. Dahl, Palle Christophersen
  • Publication number: 20040030134
    Abstract: A novel process is provided for the preparation of chiral intermediates useful in the asymmetric syntheses of &agr;v&bgr;3 integrin receptor antagonists. Also provided are the enantiomerically enriched intermediates that are obtained from the process.
    Type: Application
    Filed: September 11, 2003
    Publication date: February 12, 2004
    Inventors: James Christopher McWilliams, Elizabeth Buck, Kan K. Eng, Guy R. Humphrey, Peter E. Maligres, Jess W. Sager, Marjorie See Waters
  • Publication number: 20040019067
    Abstract: The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.
    Type: Application
    Filed: October 22, 2002
    Publication date: January 29, 2004
    Applicant: Amgen Inc.
    Inventors: David M. Armistead, Jean E. Bemis, Daniel Elbaum, Gregory J. Habgood, Perry M. Novak, Joseph J. Nunes, Leticia M. Toledo-Sherman
  • Publication number: 20040002599
    Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I), 1
    Type: Application
    Filed: October 21, 2002
    Publication date: January 1, 2004
    Inventors: Klaus-Helmut Muller, Hans-Georg Schwarz, Stefan Herrmann, Dorothee Hoischen, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Akihiko Yanagi, Shinichi Narabu, Toshio Goto, Seishi Ito, Chieko Ueno
  • Patent number: 6664214
    Abstract: The invention provides an uracil compound represented by the general formula: wherein W represents oxygen or sulfur; R1 represents C1- to C3-alkyl or C1- to C3-haloalkyl; R2 represents C1- to C3-alkyl or C1- to C3-haloalkyl; R3 represents hydrogen, C1- to C3-alkyl, phenyl, C1- to C3-haloalkyl or cyano; R4 represents hydrogen or C1- to C3-alkyl; R5 represents C1- to C6-alkyl, C1- to C6-haloalkyl, C3- to C6-alkenyl, C3- to C6-haloalkenyl, C3- to C6-alkynyl or C3- to C6-haloalkynyl; X1 represents halogen; X2 represents hydrogen or halogen; X3 and X4 are independent with each other and each represents hydrogen, halogen, C1- to C6-alkyl, C1- to C6-haloalkyl, C2- to C6-alkenyl, C2- to C6-haloalkenyl, C3- to C6-alkynyl, C3- to C6-haloalkynyl, C1- to C6-alkoxy-C1- to C6-alkyl, C1- to C6-alkoxy, C1- to C6-haloalkoxy or cyano; and n represents an integer of 1 to 4.
    Type: Grant
    Filed: January 7, 2002
    Date of Patent: December 16, 2003
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Akira Shuto
  • Patent number: 6649760
    Abstract: Phenyluracils of the general formula (I) in which Q, R1, R2, R3, R4, R5 and R6 each have one of the meanings given in the description, and processes for their preparation and their use as herbicides.
    Type: Grant
    Filed: February 20, 2002
    Date of Patent: November 18, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Hans-Georg Schwarz, Karl-Heinz Linker, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 6624120
    Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which m, n, Q, R1, R2, R3, R4, R5, X and Y are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides.
    Type: Grant
    Filed: December 13, 2001
    Date of Patent: September 23, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Hans-Georg Schwarz, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Publication number: 20030176642
    Abstract: The present invention relates to certain substituted oxadiazole peptoids and nonpeptoids useful as inhibitors of serine proteases, especially human neutophil elastase (HNE). Compounds of the present invention are useful for the treatment or amelioration of symptoms of adult respiratory distress syndrome, septic shock, and multiple organ failure. Processes mediated by HNE are also implicated in conditions such as arthritis, periodontal disease, glomerulonephritis, and cystic fibrosis.
    Type: Application
    Filed: January 30, 2003
    Publication date: September 18, 2003
    Inventors: Albert Gyorkos, Lyle Spruce, Kazuyuki Ohmoto, Kazuhito Kawabata
  • Publication number: 20030176677
    Abstract: Compounds having structure (1) 1
    Type: Application
    Filed: November 14, 2002
    Publication date: September 18, 2003
    Inventors: Kuei-Ying Lin, Mark D. Matteucci
  • Patent number: 6620932
    Abstract: Novel 2-alkoxy-5-methoxypyrimidines and tautomeric forms thereof and also processes for preparing them are described. The 2-alkoxy-5-methoxypyrimidines according to the invention can be synthesized in few reaction steps and in high yields from simple precursors.
    Type: Grant
    Filed: August 15, 2002
    Date of Patent: September 16, 2003
    Assignee: Degussa AG
    Inventors: Thomas Güthner, Karl-Heinz Neuhauser
  • Publication number: 20030171368
    Abstract: The disclosure is directed to compounds of the formula (I) 1
    Type: Application
    Filed: February 6, 2002
    Publication date: September 11, 2003
    Inventors: Werner Seitz, Andreas Kling, Herve Geneste, Thomas Subkowski, Claudia Graef, Wilfried Hornberger
  • Patent number: 6613773
    Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: September 2, 2003
    Assignee: Syngenta Limited
    Inventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
  • Patent number: 6608197
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: January 25, 2001
    Date of Patent: August 19, 2003
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
  • Publication number: 20030153758
    Abstract: Oxadiazole derivatives represented by formula (I): 1
    Type: Application
    Filed: January 17, 2003
    Publication date: August 14, 2003
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tsutomu Kojima, Katsutoshi Hachiya, Kazuyuki Ohmoto
  • Publication number: 20030144300
    Abstract: Compounds of formula (1.0.0) are described, as well as the usefulness of a pharmaceutical composition for treating inflammatory, respiratory and allergic diseases and conditions, especially asthma; chronic obstructive pulmonary disease (COPD) including chronic bronchitis, emphysema, and bronchiectasis; chronic rhinitis; and chronic sinusitis.
    Type: Application
    Filed: July 24, 2002
    Publication date: July 31, 2003
    Inventors: Thomas Victor Magee, Anthony Marfat, Robert James Chambers
  • Patent number: 6600044
    Abstract: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: July 29, 2003
    Assignee: Brantford Chemicals Inc.
    Inventors: K. S. Keshava Murthy, Gurijala V. Reddy, Zhi-xian Wang, Chandrawansha B. W. Senanayake
  • Publication number: 20030138864
    Abstract: The present invention relates to a method for identification of enzymes that are preferentially expressed in certain tumor tissue as compared with rapidly growing normal cells or tissue, use of said enzymes for the compound design to generate an active anti-cancer substance selectively in tumor tissue, compounds designed based on said enzymes, their pharmaceutically acceptable salts as well as pharmaceutical composition thereof.
    Type: Application
    Filed: November 21, 2002
    Publication date: July 24, 2003
    Inventors: Hideo Ishitsuka, Hisafumi Okabe, Nobuo Shimma, Takuo Tsukuda, Isao Umeda
  • Publication number: 20030139407
    Abstract: An efficient synthesis of sulfonyl pyrazoles of formula I: 1
    Type: Application
    Filed: November 1, 2002
    Publication date: July 24, 2003
    Inventors: Andrei Shavnya, Subas M. Sayka, Martha L. Minich, Bryson Rast
  • Publication number: 20030134850
    Abstract: The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: 1
    Type: Application
    Filed: November 1, 2002
    Publication date: July 17, 2003
    Applicant: Pfizer Inc.
    Inventors: Subas M. Sakya, Bryson Rast
  • Publication number: 20030134837
    Abstract: Compounds of the formula (I) wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; V is CH or N; R1 is hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, hererocyclylC1-6alkyl, heteroaryl, or heteroarylC1-6alkyl any of which except hydrogen may be optionally substituted; R2 and R3 independently represent hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heteroaryl, heteroarylC1-6alkyl, heterocyclyl, or heterocyclylC1-6alkyl any one of which except hydrogen may be optionally substituted, or R2 and R3 together with the nitrogen atom to which they are attached form a 4- to 10-membered optionally substituted monocyclic or bicyclic ring; Ar is an aryl or heteroaryl ring either of which may be optionally substituted; one of X1 and X2 is N and the other is NR4, wherein R4 is hydrogen, C1-6alkyl, or arylC1-6alkyl; or pharmaceutically acceptable salts thereof; their use as inhibitors of Raf kinases and pharmaceutical compositions containing them.
    Type: Application
    Filed: December 18, 2002
    Publication date: July 17, 2003
    Inventors: Alessandra Gaiba, Andrew Kenneth Takle, David Matthew Wilson
  • Publication number: 20030114414
    Abstract: Methods of preparing N3-substituted-4-pyrimidones are disclosed. The methods include combining a 4-pyrimidone and a non-aqueous base, followed by an alkylating agent, for a time sufficient for the pyrimidone and the alkylating agent to react. Methods of preparing an N3-substituted-6-(substituted amino)uracil are also disclosed. The methods include (a) combining an N3-substituted-2-alkoxy-6-amino-4-pyrimidone with an amine compound selected from the group consisting of an amine salt and the corresponding free amine, to form a reaction mixture; and (b) heating the reaction mixture to at least 80° C. for a time sufficient for the N3-substituted-2-alkoxy-6-amino-4-pyrimidone and the amine compound to react to form the final product.
    Type: Application
    Filed: June 17, 2002
    Publication date: June 19, 2003
    Inventors: Chengxin Zhi, Zheng-Yu Long, Andrzej Manikowski, George E. Wright
  • Publication number: 20030096817
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Application
    Filed: May 10, 2002
    Publication date: May 22, 2003
    Inventors: Jeremy Green, Scott L. Harbeson, John E. Cochran