At 2-position Patents (Class 544/315)
  • Patent number: 6867210
    Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 15, 2005
    Assignee: Euro-Celtique S.A.
    Inventors: Derk J. Hogenkamp, Phong Nguyen, Bin Shao
  • Patent number: 6855716
    Abstract: Dihydropyrimidine derivatives of the following formula or analogs thereof have selective N-type calcium channel antagonistic activity, and they are used as therapeutic agents for various diseases participating in the N-type calcium channels.
    Type: Grant
    Filed: December 26, 2001
    Date of Patent: February 15, 2005
    Assignee: Ajinomoto Co., Inc.
    Inventors: Seiji Ohno, Akiko Okajima, Seiji Niwa, Morikazu Kito, Akira Takahara, Yukitsugu Ono, Yuki Kajigaya, Tomoko Takeda, Hajime Koganei
  • Patent number: 6818648
    Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: November 16, 2004
    Assignee: Bristol-Myers Squibb Pharma
    Inventors: Robert John Chorvat, Parthasarathi Rajagopalan
  • Patent number: 6818631
    Abstract: Fungicidal pyrimidine derivatives and the use as a fungicide of the compounds of formula (1): wherein R1 is H, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl C3-C6cycloalkyl, C1-C6alkoxy, C3-C6cycloalkoxy, C1-C6alylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, phenyl, pyridinyl or azolyl groups, (being optionally substituted by one or more substituents); or N(R4)C(O)R5, R2 is polyfluoroalkyl, R3 is fluorine, chlorine, bromine or iodine; ethenyl or ethynyl (being optionally substituted by one or more of halogen), R4 and R5 are, independently, H, C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl groups, (being optionally substituted by one or more of halogen or cyano); or R4 and R5 can join together to form a 5 or 6-membered ring, Q is a heteroaromatic ring selected from the following ring system; imidazol-1-yl, pyrazol-1-yl, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-1-yl, benzimidazol-1-yl or tetrazol-5-yl groups, (being optionally substituted by one or more of substituents).
    Type: Grant
    Filed: August 15, 2003
    Date of Patent: November 16, 2004
    Assignee: Nippon Soda Co. Ltd.
    Inventors: Yuki Nakagawa, Sergey Bobrov, Charles R. Semer, IV, Thomas A. Kucharek, Masahiro Haramoto
  • Patent number: 6806230
    Abstract: Pyrimidine derivatives having excellent herbicidal activities for crop plants and selectivity between crop plants and weeds, are presented. Pyrimidine derivatives represented by the following formula (I): wherein R1 is a hydrogen atom, an alkyl group, a haloalkyl group or the like; R2 is an alkyl group, a phenyl group which may be substituted, or the like; R3 is a hydrogen atom, an alkyl group, an alkynyl group or the like; R7 is a hydrogen atom, a halogen atom, an alkyl group or the like; R8 is a hydrogen atom, an alkyl group or the like, W is a —C(═Q) Z— group or a —SO2— group; Q is O or S; Z is O, S, a —C(R4)R5—, a —NR6 group or the like; each of R4 and R5 is a hydrogen atom, an alkyl group, an alkoxy group or the like; R6 is a hydrogen atom or an alkyl group; and Ar is a phenyl group which may be substituted, a pyridyl group which may be substituted, or the like, and herbicides containing such pyrimidine derivatives as active ingredients.
    Type: Grant
    Filed: March 11, 2002
    Date of Patent: October 19, 2004
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Atsushi Yasuda, Fumiaki Takabe, Ikumi Urushibata, Mikio Yamaguchi, Yoshihiro Yamaji, Makoto Fujinami, Takeshige Miyazawa
  • Publication number: 20040198728
    Abstract: The invention relates to pyridines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor cells.
    Type: Application
    Filed: September 22, 2003
    Publication date: October 7, 2004
    Applicant: Cell Therapeutics, Inc.
    Inventors: Feng Hong, J. Peter Klein
  • Patent number: 6794378
    Abstract: The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: December 31, 2001
    Date of Patent: September 21, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Koichi Fujita, Ariko Kodaira, Toshihiro Hatanaka, Kenji Takehana, Tsuyoshi Kobayashi, Atsushi Konishi, Takashi Yamamoto
  • Patent number: 6790846
    Abstract: Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.
    Type: Grant
    Filed: May 7, 2002
    Date of Patent: September 14, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Michael Philip Clark, Jane Far-Jine Djung, Steven Karl Laughlin, Joshua Spector Tullis, Michael George Natchus, Biswanath De
  • Patent number: 6787544
    Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: September 7, 2004
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura
  • Patent number: 6780868
    Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.
    Type: Grant
    Filed: February 20, 2003
    Date of Patent: August 24, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
  • Publication number: 20040147761
    Abstract: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): 1
    Type: Application
    Filed: December 15, 2003
    Publication date: July 29, 2004
    Inventors: Jean-Michel Paul, Bernard Dupont
  • Patent number: 6762197
    Abstract: A triazolone compound of the formula [I]: wherein; R1 represents optionally substituted phenyl or the like, T represents m-phenylene optionally substituted by methyl or the like; and a fungicidal composition containing it as an active ingredient.
    Type: Grant
    Filed: June 6, 2002
    Date of Patent: July 13, 2004
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Tomohiro Araki, Yoshiharu Kinoshita, Hiroshi Sakaguchi, Akio Manabe
  • Publication number: 20040132752
    Abstract: This invention discloses and claims diary heterocycles of formula (I) 1
    Type: Application
    Filed: July 24, 2003
    Publication date: July 8, 2004
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Thomas Boehme, Gerhard Hessler, Gerard Rosse, Armin Walser
  • Publication number: 20040087581
    Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1
    Type: Application
    Filed: October 14, 2003
    Publication date: May 6, 2004
    Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
  • Publication number: 20040077641
    Abstract: Novel pyridylpyrimidines of the formula 1
    Type: Application
    Filed: August 19, 2003
    Publication date: April 22, 2004
    Inventors: Thomas Bretschneider, Mazen Es-Sayed, Rudiger Fischer, Fritz Maurer, Christoph Erdelen, Peter Losel
  • Publication number: 20040063659
    Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
    Type: Application
    Filed: September 18, 2003
    Publication date: April 1, 2004
    Applicant: Merrell Pharmaceuticals Inc.
    Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
  • Patent number: 6710045
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which m represents integers from 3 to 10, n represents 0, 1 or 2 and Het represents the following, in each case optionally substituted, groupings: to processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: March 23, 2004
    Assignee: Bayer CropScience AG
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Patent number: 6686369
    Abstract: The present invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings stated in the description, to the preparation of these compounds and to their use as drugs.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: February 3, 2004
    Assignee: Abbott GmbH & Co., KG
    Inventors: Dagmar Klinge, Wilhelm Amberg, Ernst Baumann, Andreas Kling, Hartmut Riechers, Liliane Unger, Manfred Raschack, Stefan Hergenröder, Sabine Schult
  • Patent number: 6664247
    Abstract: This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: December 16, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
  • Patent number: 6653295
    Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): that are useful as serine protease inhibitors, and more particularly as Hepatitis C virus NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: November 25, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter William Glunz, Brent Dale Douty, Wei Han
  • Patent number: 6653258
    Abstract: Fungicidal compounds of the formula (I): and stereoisomers thereof, wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR4; R2, R3 and R4, which may be the same or different, are hydrogen, C1-4 alkyl or C2-4 alkenyl; X is halogen, C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxy, nitro or cyano, and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R1 is unsubstituted phenyl at least one of R2 and R3 is other than hydrogen or methyl.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: November 25, 2003
    Assignee: Syngenta Limited
    Inventors: John M Clough, Christopher R A Godfrey, Paul J de Fraine, Michael G Hutchings, Vivienne M Anthony
  • Patent number: 6653300
    Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: November 25, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
  • Patent number: 6649622
    Abstract: aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: November 18, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard Sulsky, Jeffrey A. Robl
  • Patent number: 6632817
    Abstract: The invention relates to novel fluoromethoximino compounds, to a process for their preparation and to their use as pesticides, and also to novel intermediates and to a plurality of processes for their preparation.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: October 14, 2003
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Albrecht Marhold, Uwe Stelzer, Reinhard Lantzsch, Ralf Tiemann, Klaus Stenzel, Astrid Mauler-Machnik, Stefan Dutzmann, Martin Kugler, Hans-Ulrich Buschhaus
  • Publication number: 20030187259
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1
    Type: Application
    Filed: May 12, 2003
    Publication date: October 2, 2003
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrim, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Patent number: 6610691
    Abstract: The invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings defined in the description, to the preparation of these compounds and to their use as drugs.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: August 26, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Heinz Hillen, Liliane Unger, Bernd Elger
  • Patent number: 6608072
    Abstract: Compounds of formula (I) and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof, wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.
    Type: Grant
    Filed: April 22, 2002
    Date of Patent: August 19, 2003
    Assignee: Novartis AG
    Inventor: Lászlo Révész
  • Patent number: 6605611
    Abstract: Nucleoside analogues or base analogues having structure (I), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.
    Type: Grant
    Filed: September 3, 2002
    Date of Patent: August 12, 2003
    Assignee: Nycomed Amersham PLC
    Inventors: Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
  • Publication number: 20030119835
    Abstract: The present invention relates to compounds of the formula 1
    Type: Application
    Filed: July 3, 2002
    Publication date: June 26, 2003
    Inventors: Subas M. Sakya, Andrei Shavnya, Bryson Rast
  • Publication number: 20030114472
    Abstract: This invention concerns the use of compounds of formula 1
    Type: Application
    Filed: November 1, 1999
    Publication date: June 19, 2003
    Inventors: BART DE CORTE, MARC RENE DE JONGE, JAN HEERES, CHIH YUNG HO, PAUL ADRIAAN JAN JANSSEN, ROBERT W. KAVASH, LUCIEN MARIA HENRICUS KOYMANS, MICHAEL JOSEPH KUKLA, DONALD WILLIAM LUDOVICI, KOEN JEANNE ALFONS VAN AKEN
  • Patent number: 6579874
    Abstract: Compounds of formula I wherein the symbols have meaning as defined herein, are p38 MAP kinase inhibitors, and are useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases, such as rheumatoid arthritis, and diseases of bone metabolism, e.g. osteoporosis.
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: June 17, 2003
    Assignee: Novartis AG
    Inventors: Lászlo Révész, Achim Schlapbach
  • Publication number: 20030109484
    Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
    Type: Application
    Filed: June 6, 2002
    Publication date: June 12, 2003
    Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
  • Publication number: 20030105084
    Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: 1
    Type: Application
    Filed: September 18, 2002
    Publication date: June 5, 2003
    Applicant: The Procter & Gamble Company
    Inventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Biswanath De
  • Publication number: 20030096931
    Abstract: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): 1
    Type: Application
    Filed: August 22, 2002
    Publication date: May 22, 2003
    Inventors: Jean-Michel Paul, Bernard Dupont
  • Patent number: 6566357
    Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; two R2 units on the same carbon atom are taken together to form a spirocyclic ring having from 4 to 7 atoms, the balance of the R2 units are independently selected from the group consisting of: a) hydrogen; b) —O(CH2)jR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —CH2)jCON(R10)2; and g) two R2 units can be taken together to form a carbonyl unit; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 uni
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: May 20, 2003
    Assignee: The Procter & Gamble Co.
    Inventors: Matthew John Laufersweiler, Michael Philip Clark, Jane Far-Jine Djung, Adam Golebiowski, Todd Andrew Brugel, Biswanath De
  • Publication number: 20030092678
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: May 15, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6562832
    Abstract: Novel 1,4,5-subsituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: May 13, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Jeffrey C. Boehm, Timothy Francis Gallagher
  • Patent number: 6554966
    Abstract: The invention relates to a process for preparing essentially formic acid-free N-alkyl-N′-methylalkyleneureas of the formula with R1=H or CH3, R2=CnH2n+1 with n=1-4 and x=0 or 1, from the corresponding alkyleneureas by reaction with monomeric or polymerized formaldehyde in the presence of formic acid. This entails feeding the mixture, obtained in the reaction, of N-alkyl-N′-methylalkyleneurea and formic acid to the upper region of a distillation column, distilling without further additions and removing essentially formic acid-free N-alkyl-N′-methylalkyleneurea in the lower region of the column.
    Type: Grant
    Filed: June 26, 2000
    Date of Patent: April 29, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Kramer, Johann-Peter Melder, Heinz RĂĽtter, GĂĽnter Riewe, Wolfgang Siegel, Hans-JĂĽrgen Weyer
  • Publication number: 20030069242
    Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): 1
    Type: Application
    Filed: April 15, 2002
    Publication date: April 10, 2003
    Applicant: KUMIAI CHEMICAL INDUSTRY CO., LTD.
    Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
  • Publication number: 20030064980
    Abstract: Compound represented by the structural formula 1
    Type: Application
    Filed: June 6, 2002
    Publication date: April 3, 2003
    Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
  • Patent number: 6534492
    Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.
    Type: Grant
    Filed: May 4, 2001
    Date of Patent: March 18, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
  • Patent number: 6528510
    Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
    Type: Grant
    Filed: November 2, 2000
    Date of Patent: March 4, 2003
    Assignee: Warner-Lambert Company
    Inventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Michael James Lovdahl, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
  • Patent number: 6525025
    Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods for treatment of caspase-3 mediated diseases.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: February 25, 2003
    Assignee: Merck Frosst Canada & Co.
    Inventors: Yongxin Han, Andre Giroux, Erich L. Grimm, Renee Aspiotis, Cameron Black
  • Publication number: 20030036543
    Abstract: This invention describes novel pyrazole compounds of formula IIIa: 1
    Type: Application
    Filed: December 19, 2001
    Publication date: February 20, 2003
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
  • 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
  • Patent number: 6509341
    Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the meaning as commented in the description. It also relates to the production and use of same as endothelin receptor antagonists.
    Type: Grant
    Filed: April 20, 2000
    Date of Patent: January 21, 2003
    Assignee: Abbott Laboratories
    Inventors: Wilhelm Amberg, Rolf Jansen, Stefan Hergenröder, Manfred Raschack, Liliane Unger
  • Patent number: 6506763
    Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: January 14, 2003
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Publication number: 20020193375
    Abstract: The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The, invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).
    Type: Application
    Filed: June 27, 2002
    Publication date: December 19, 2002
    Applicant: ZENECA LIMITED
    Inventors: Peter Warner, Roger James, Thorsten Nowak
  • Patent number: 6492366
    Abstract: A compound selected from those of formula (I): wherein: R1 and R2 each independently represent hydrogen or, alkyl, T1 and T2 each independently represent alkylene, G represents a heterocyclic group selected of formula (&agr;):  wherein: W1 to W5 and X1 to X4 are so defined in the description. Medicinal products containing the same are useful as serotonin-reuptake inhibitors.
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: December 10, 2002
    Assignee: Les Laboratoires Servier
    Inventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Didier Cussac, Anne Dekeyne
  • Patent number: 6489325
    Abstract: The present invention relates to novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 inhibitors.
    Type: Grant
    Filed: March 30, 2000
    Date of Patent: December 3, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Ralph F. Hall