Oxygen Bonded Directly To The Diazine Ring Patents (Class 544/123)
  • Patent number: 6743914
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: June 1, 2004
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Patent number: 6743798
    Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.
    Type: Grant
    Filed: April 11, 2001
    Date of Patent: June 1, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky, Elke Stahl
  • Publication number: 20040087789
    Abstract: The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral nervous systems, including age related cognitive disorders such as senility and Alzheimer's disease, nerve injuries, peripheral neuropathies, and seizure disorders such as epilepsy.
    Type: Application
    Filed: June 27, 2003
    Publication date: May 6, 2004
    Inventors: Lilia M. Beauchamp, Thomas A. Krenitsky, James L. Kelley
  • Publication number: 20040082780
    Abstract: Compounds having the general structure 1
    Type: Application
    Filed: August 8, 2003
    Publication date: April 29, 2004
    Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
  • Patent number: 6720322
    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: Grant
    Filed: June 24, 2002
    Date of Patent: April 13, 2004
    Assignee: Actelion Pharamceuticals Ltd.
    Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli
  • Patent number: 6720321
    Abstract: Disclosed are compounds of the formula (I) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein n, X, A, L, J, p, Q, Y and z are described herein.
    Type: Grant
    Filed: May 24, 2002
    Date of Patent: April 13, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Eugene R. Hickey
  • Publication number: 20040063936
    Abstract: A pyrimidine derivative compound of formula (I) or a salt thereof and a method for the preparation thereof.
    Type: Application
    Filed: June 25, 2003
    Publication date: April 1, 2004
    Inventors: Tsuneyuki Sugiura, Toshihide Horiuchi, Toru Miyazaki, Tsutomu Kojima, Shinsuke Hashimoto
  • Publication number: 20040063937
    Abstract: The invention relates to novel N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives of the general formula (1) wherein the sum of (m+p) together is 0, 1, 2 or 3; n and q are independently of each other 0 or 1, and the sum of (m+p+q) together is 1, 2, 3 or 4; R1 is hydrogen, halogen, alkoxy, haloalkyl, haloalkoxy or alkyl; R2 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl or C1-C6-alkoxy; R2A is hydrogen, C1-C6-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; each of R3, R4, R5 and R6 is, independently of the others, hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, hydroxy-C1-C6-alkyl or C1-C6-alkoxy-C1-C6-alkyl, or the ring members CR3R4 or CR5R6 or CR2R2A are independently of each other a carbonyl group (C═O) or a group C═S; X is C═O, C═S, S═O or O═S=O; Y is O, S, C═O, CH2A, —N(R8)—, —O—N(R8)—, —N(R8)—O— or NH—; R7 is hydrogen, C1-C4-alkyl, C3-C4-alkenyl, C3-C4-alkynyl, —CH2OR8, CH2SR8, —C(O)R8, —C(O)OR8,
    Type: Application
    Filed: June 25, 2003
    Publication date: April 1, 2004
    Inventors: Martin Eberle, Hugo Ziegler, Fredrik Cederbaum, Peter Ackermann, Anita Schnyder
  • Publication number: 20040038969
    Abstract: Compounds having the general structure 1
    Type: Application
    Filed: May 20, 2003
    Publication date: February 26, 2004
    Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
  • Publication number: 20040029876
    Abstract: This invention relates to novel acylamino cyclopropane derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as modulators of dopamine D3 receptors and for the treatment of anxiety, psychosis, substance abuse, Parkinson's disease, sexual dysfunction, and other central nervous system disorders.
    Type: Application
    Filed: July 29, 2003
    Publication date: February 12, 2004
    Applicant: Pfizer Inc
    Inventors: Anton F. J. Fliri, Anthony R. Reinhold
  • Publication number: 20040029857
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: April 25, 2003
    Publication date: February 12, 2004
    Inventors: Michael Robin Hale, Francois Maltais, Qing Tang, Judith Straub, Alexander Aronov
  • Publication number: 20040009975
    Abstract: Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them are useful for the treatment of inflammation and immunological diseases.
    Type: Application
    Filed: April 9, 2003
    Publication date: January 15, 2004
    Applicant: ORCHID CHEMICALS & PHARMACEUTICALS LIMITED
    Inventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
  • Publication number: 20040009974
    Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 14, 2003
    Publication date: January 15, 2004
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
  • Patent number: 6677337
    Abstract: The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, or enantiomeric and diasteriomeric forms or pharmaceutically acceptable salts thereof, have the formula: wherein R is an ether or amino unit, R1 is substituted phenyl, each R2 and R3 unit is independently selected from the group consisting of: a) hydrogen; and b) substituted or unsubstituted C1-C10 hydrocarbyl selected from the group consisting of: i) C1-C10 linear, branched or cyclic alkyl; ii) C1-C10 aryl; iii) C1-C10 heterocyclic; iv) C1-C10 heteroaryl.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: January 13, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Matthew John Laufersweiler, Cynthia Monesa Crago Clark, Michael Philip Clark, Jane Far-Jine Djung, Biswanath De, Michael George Natchus
  • Publication number: 20040006068
    Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
    Type: Application
    Filed: January 24, 2003
    Publication date: January 8, 2004
    Applicant: Tularik Inc.
    Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
  • Publication number: 20030232813
    Abstract: The present invention relates to novel amino substituted pyrimidinone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel amino substituted pyrimidinone derivatives of the general formula (I) and a method thereof.
    Type: Application
    Filed: April 9, 2003
    Publication date: December 18, 2003
    Applicant: ORCHID CHEMICALS & PHARMACEUTICALS LIMITED
    Inventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
  • Publication number: 20030229084
    Abstract: The present application describes novel barbituric acid derivatives of formula I: 1
    Type: Application
    Filed: December 17, 2002
    Publication date: December 11, 2003
    Inventors: Jingwu Duan, Bin Jiang, Lihua Chen, Zhonghui Lu, Joseph Barbosa, William J. Pitts
  • Publication number: 20030225075
    Abstract: The present invention relates to novel pyrimidone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel pyrimidone derivatives of the general formula (I) and a method thereof.
    Type: Application
    Filed: April 9, 2003
    Publication date: December 4, 2003
    Applicant: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar, Debendranath Dey, Biswajit Nag
  • Publication number: 20030207865
    Abstract: This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.
    Type: Application
    Filed: October 23, 2001
    Publication date: November 6, 2003
    Inventors: Brian R. Dixon, Cedo M. Bagi, Catherine R. Brennan, David R. Brittelli, William H. Bullock, Jinshan Chen, William L. Collibee, Robert Dally, Jeffrey S. Johnson, Harold C. E. Kluender, William F. Lathrop, Peiying Liu, Carol Ann Mase, Aniko M. Redman, William J. Scott, Klaus Urbahns, Donald J. Wolanin
  • Patent number: 6635636
    Abstract: The invention concerns novel substituted 6-benzyl-4-oxopyrimidines and pharmaceutically acceptable salts thereof. These compounds inhibit reverse transcriptase encoded by human immunodeficiency virus (HIV), and are useful to prevent and treat HIV infection and acquired immune deficiency syndrome (AIDS). Pharmaceutical compositions containing the compounds and a method of use of the present compounds and other agents for the treatment of AIDS and viral infection by HIV are also envisaged.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: October 21, 2003
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Marino Artico, Paolo La Colla
  • Publication number: 20030171359
    Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) 1
    Type: Application
    Filed: October 16, 2002
    Publication date: September 11, 2003
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Georg Dahmann, Frank Himmelsbach, Bernd Krist, Martin Lenter, Alexander Pautsch, Gisela Schnapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoops, Steffen Steurer
  • Publication number: 20030166647
    Abstract: The present application describes novel barbituric acid derivatives of formula I: 1
    Type: Application
    Filed: December 17, 2002
    Publication date: September 4, 2003
    Inventors: Jingwu Duan, Zhonghui Lu
  • Patent number: 6613764
    Abstract: The present invention provides a compound of formula (I) wherein a, b, c, d, and e, are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen. R7 and R8 are H or alkyl, R1 and R2 are H or alkyl, and R3 is a non-aromatic substituent. Substituent A is OH, NH2, or SH. Substituents B and B1 include amide and sulfonamide groups, which can be cyclic, acyclic, or amino acid derivatives. Alternatively, B and R′ together with the nitrogen to which they are bonded, and/or B′ and R2 together with the nitrogen to which they are bonded, define a heterocycle. The present invention further provides a pharmaceutical composition that includes a carrier and a therapeutically effective amount of at least one compound of the present invention.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: September 2, 2003
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Ramnarayan S. Randad, John W. Erickson, Michael A. Eissenstat, Lucyna Lubkowska
  • Publication number: 20030162967
    Abstract: The present invention relates to compounds of the formula I, 1
    Type: Application
    Filed: August 26, 2002
    Publication date: August 28, 2003
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Otmar Klingler, Gerhard Zoller, Elisabeth Defossa, Fahad A. Al-Obeidi, Armin Walser, James Ostrem
  • Publication number: 20030149037
    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: December 20, 2002
    Publication date: August 7, 2003
    Inventors: Francesco Salituro, Guy Bemis, John Cochran
  • Publication number: 20030139403
    Abstract: This invention features pyrimidine compounds of formula (I): 1 2
    Type: Application
    Filed: November 30, 2001
    Publication date: July 24, 2003
    Inventors: M. Ono, Lijun Sun, Teresa Przewloka, Shijie Zhang, Elena Kostic, Weiwen Ying, Yumiko Wada, K. Koya
  • Publication number: 20030134838
    Abstract: The present invention relates to trisubstituted pyrimidines of formula 1
    Type: Application
    Filed: October 16, 2002
    Publication date: July 17, 2003
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Klaus Bornemann, Hans Briem, Cornelia Dorner-Clossek, Katja Fechteler, Klaus Fuchs, Frank Himmelsbach, Klaus Klinder, Markus Kostka
  • Publication number: 20030119828
    Abstract: The present application relates to novel guanidine derivatives of the formula (I) 1
    Type: Application
    Filed: October 1, 2002
    Publication date: June 26, 2003
    Inventors: Klaus Wagner, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
  • Publication number: 20030114446
    Abstract: This invention features pyrimidine compounds of formula (I): 1
    Type: Application
    Filed: July 10, 2002
    Publication date: June 19, 2003
    Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostic, Yumiko Wada
  • Publication number: 20030114445
    Abstract: Compounds useful for treating Gram-positive bacterial and mycoplasmal infections are disclosed. The compounds have the general formulae shown below.
    Type: Application
    Filed: June 17, 2002
    Publication date: June 19, 2003
    Inventors: Chengxin Zhi, Zheng-Yu Long, George E. Wright, Neal C. Brown, Serge Lamothe, Irina Motorina
  • Patent number: 6579982
    Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: June 17, 2003
    Assignee: Pfizer Inc.
    Inventor: Julian Blagg
  • Patent number: 6573377
    Abstract: This invention provides compounds having antitumor effect, namely a compound represented by the following formula (I) or (Ia) having various substituents in which G and G1 are condensed tricyclic heterocyclic rings or salts thereof, and a compound represented by the following formula (Ib) having various substituents or salts thereof.
    Type: Grant
    Filed: January 24, 2001
    Date of Patent: June 3, 2003
    Assignee: Daiichi Pharmaceuticals Co., Ltd.
    Inventors: Akio Ejima, Satoru Ohsuki, Hitoshi Ohki, Hiroyuki Naito, Chie Makino
  • Publication number: 20030100549
    Abstract: The present invention relates to inhibitors of JNK, 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: December 3, 2001
    Publication date: May 29, 2003
    Inventors: Francesco Salituro, Guy Bemis, Jeremy Green, Jasna Fejzo, Xiaoling Xie
  • 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: 20030096990
    Abstract: A process for producing 3-phenyl-2,4(1H,3H)-pyrimidinediones having the general formula I and their salts 1
    Type: Application
    Filed: September 26, 2001
    Publication date: May 22, 2003
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Mark Read, Masamitsu Tsukamoto, Sandeep Gupta
  • Patent number: 6562967
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: November 5, 2001
    Date of Patent: May 13, 2003
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Patent number: 6562966
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: May 13, 2003
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Patent number: 6559155
    Abstract: Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which: R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH; R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system; R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system; W is SO2 or a bond; X is O or S; and Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: May 6, 2003
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Colin Andrew Leach, Stephen Allan Smith
  • Patent number: 6548512
    Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: April 15, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
  • 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
  • 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: 6525051
    Abstract: N-Heterocyclic derivatives selected from the group consisting of the following formulae: where Z1, Z2, Z3, R1, R2, R3, R4, R5 and R6 are described herein, are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: February 25, 2003
    Assignee: Schering Aktiengesellschaft
    Inventors: David D. Davey, Eric Pham, Gary B. Phillips, Wei Xu
  • 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
  • Publication number: 20030004161
    Abstract: This invention describes novel pyrazole compounds of formula I′: 1
    Type: Application
    Filed: December 19, 2001
    Publication date: January 2, 2003
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
  • Patent number: 6498253
    Abstract: Compounds of the formula (I) and salts thereof in which W1, W2, R, n, R1, R2, R4, X, Y and Z are as defined in claim 1 and R3 is an acyl radical, are suitable as herbicides and plant growth regulators. The herbicides can be prepared by the process variants from claim 5, the novel intermediate products (II), (IV), (VI) and (VIII)* of claims 9 and 10 being employed.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: December 24, 2002
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • 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
  • Publication number: 20020120139
    Abstract: A group of novel pyrimidone compounds are inhibitors of the enzyme LDL PLA2 and therefore of use in treating atherosclerosis.
    Type: Application
    Filed: April 2, 2002
    Publication date: August 29, 2002
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Roderick Alan Porter, Stephen Allan Smith
  • Patent number: 6440965
    Abstract: The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral systems.
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: August 27, 2002
    Assignee: Krenitsky Pharmaceuticals, Inc.
    Inventors: James L. Kelley, Thomas A. Krenitsky, Lilia M. Beauchamp
  • Publication number: 20020111353
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: December 5, 2001
    Publication date: August 15, 2002
    Inventors: Mark Ledeboer, Francesco Salituro, Young-Choon Moon
  • 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