1,3-diazoles (including Hydrogenated) Patents (Class 546/272.7)
  • Publication number: 20040138244
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: October 14, 2003
    Publication date: July 15, 2004
    Inventors: James T. Dalton, Duane D. Miller
  • Publication number: 20040127496
    Abstract: Compounds of formula (I): wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; R1 is hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, heterocyclylC1-6alkyl, heteroaryl, or heteroarylC1-6 alkyl, 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, or R2 and R3 together with the nitrogen atom to which they are attached form a 4- to 10-membered monocyclic or bicyclic ring; Ar is a group of the formula a) or b), wherein A represents a fused 5- to 7-membered ring optionally containing up to two heteroatoms selected from O, S and NR5, wherein R5 is hydrogen or C1-6alkyl, which ring is optionally substituted by up to 2 substituents selected from halogen, C1-6alkyl, hydroxy, C1-6alkoxy or keto; Ra and R4 are independently selected from hydrogen, halogen, C1-6alkyl, ary
    Type: Application
    Filed: November 19, 2003
    Publication date: July 1, 2004
    Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
  • Publication number: 20040122024
    Abstract: An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or —SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isoprop
    Type: Application
    Filed: February 11, 2004
    Publication date: June 24, 2004
    Inventors: Erik De Clercq, Arthur Van Aerschot, Piet Herdewijn, Irene Lagoja, Christophe Pannecoucque
  • Publication number: 20040116440
    Abstract: Bombesin receptor antagonists are provided which are useful for the diagnosis, prevention, or treatment of male sexual dysfunction in humans and animals, female sexual dysfunction in humans and animals, anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, emesis, anorexia, pain, seasonal affective disorders, feeding disorders, or pruritus.
    Type: Application
    Filed: December 4, 2003
    Publication date: June 17, 2004
    Inventors: Michael Higginbottom, Martyn Clive Pritchard, Herman Thijs Stock
  • Publication number: 20040116355
    Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: 1
    Type: Application
    Filed: November 26, 2003
    Publication date: June 17, 2004
    Applicant: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
  • Publication number: 20040110946
    Abstract: The invention relates to compounds of formula (I), a method for the production thereof and the use of the same as pharmaceuticals.
    Type: Application
    Filed: January 7, 2004
    Publication date: June 10, 2004
    Inventors: Ulich Rosentreter, Thomas Kramer, Andrea Vaupel, Walter Hubsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch, Mitsuyuki Shimada
  • Publication number: 20040106621
    Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I 1
    Type: Application
    Filed: November 21, 2003
    Publication date: June 3, 2004
    Inventors: Yong-Jin Wu, Alexandre L'Heureux, Huan He
  • Publication number: 20040106608
    Abstract: Novel imidazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
    Type: Application
    Filed: September 17, 2003
    Publication date: June 3, 2004
    Applicant: Pfizer Inc
    Inventors: Michael J. Munchhof, Laura C. Blumberg
  • Publication number: 20040102609
    Abstract: This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
    Type: Application
    Filed: October 14, 2003
    Publication date: May 27, 2004
    Applicant: Cephalon Inc.
    Inventors: Sankar Chatterjee, John P. Mallamo, Ron Bihovsky, Gregory J. Wells
  • Publication number: 20040102496
    Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.
    Type: Application
    Filed: November 5, 2003
    Publication date: May 27, 2004
    Inventors: Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
  • Publication number: 20040097531
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: July 9, 2003
    Publication date: May 20, 2004
    Inventors: Mark Ledeboer, Jian Wang, Young Choon Moon
  • Patent number: 6737422
    Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.
    Type: Grant
    Filed: November 1, 2001
    Date of Patent: May 18, 2004
    Assignee: ICAgen, Inc.
    Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
  • Publication number: 20040082779
    Abstract: Provided are MC4-R binding compounds of the formula XVII: 1
    Type: Application
    Filed: June 16, 2003
    Publication date: April 29, 2004
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Tricia J. Vos, Michael E. Solomon, Christopher F. Claiborne, Martin P. Maguire, Mingshi Dai, Michael Patane, Thomas H. Marsilje
  • Publication number: 20040077853
    Abstract: The invention provides compounds of formula VI 1
    Type: Application
    Filed: February 18, 2003
    Publication date: April 22, 2004
    Applicant: Pfizer Inc.
    Inventors: John A. Lowe, Robert A. Volkmann
  • Publication number: 20040063763
    Abstract: The present invention provides 2-methoxyimino-2-(pynrdinyloxymetilyl,) phenyl acetamides according to formula (I) as well as their use as fungicidal compounds.
    Type: Application
    Filed: February 27, 2003
    Publication date: April 1, 2004
    Inventors: Neil Vincent Kirby, Jenifer Lynn Adamski Butz, Brent Jeffrey Rieder, James M Renga, Jeannie Rachel Phillips Cetusic, Irene Mae Morrison, John Todd Mathieson, Gary David Gustafson
  • Publication number: 20040063762
    Abstract: Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure 1
    Type: Application
    Filed: July 8, 2003
    Publication date: April 1, 2004
    Inventors: Peter T. W. Cheng, Sean Chen, Charles Z. Ding, Timothy F. Herpin
  • Publication number: 20040054173
    Abstract: Compounds having activity against production of an inflammatory cytokine of formula (I)′: 1
    Type: Application
    Filed: January 30, 2003
    Publication date: March 18, 2004
    Applicant: SANKYO COMPANY, LIMITED
    Inventors: Tomio Kimura, Kazumasa Aoki, Akira Nakao, Shigeru Ushiyama, Takaichi Shimozato, Nobuyuki Ohkawa, Takayoshi Nagasaki, Takanori Yamazaki
  • Publication number: 20040053943
    Abstract: The present invention is directed to novel compounds of Formula (I) for use in the treatment of diseases in a mammal, in which inappropriate, excessive or undesirable angiogenesis has occurred and/or where excessive Tie2 receptor activity has occurred.
    Type: Application
    Filed: May 20, 2003
    Publication date: March 18, 2004
    Inventors: Jerry L. Adams, Deborah L. Bryan
  • Patent number: 6706711
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein R1, R2, T, n and Q are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases, such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: March 16, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Michael R. Hale
  • Publication number: 20040039198
    Abstract: This invention relates to 2-pyridyl substituted diarylimidazoles which are inhibitors of the transforming growth factor, (“TGF”)-&bgr; signaling pathway, in particular, the phosphorylation of smad2 or smad3 by the type I or activin-like kinase (“ALK”)-5 receptor, methods for their preparation and their use in medicine.
    Type: Application
    Filed: May 14, 2003
    Publication date: February 26, 2004
    Inventors: Paul E. Bender, Joelle L. Burgess, James F. Callahan
  • Publication number: 20040038964
    Abstract: Novel compounds (I) and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy wherein Ar is a group of formula a) or b).
    Type: Application
    Filed: March 20, 2003
    Publication date: February 26, 2004
    Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
  • Publication number: 20040038991
    Abstract: Compounds of formula (I) are described in which R1 is optionally substituted heteroaryl; R2 is optionally substituted aryl or optionally substituted heteroaryl; R3 is a group -L1-R7 or -L2-R8 [where L1 is an optionally substituted alkylene linkage; R7 is hydrogen, aryl, cyano, cycloalkyl, heteroaryl, heterocycloalkyl, nitro, —S(O)nR9, —NHSO2R9, —C(=Z)OR10, —C(=Z)R10, —OR10, —N(R11)—C(=Z)R9, —NY1Y2, —SO2—NY1Y2, —C(=Z)-NY1Y2, —N(R11)—C(=Z)-NY1Y2, —N(OR10)—C(=Z)-NY1Y2, —N(OR10)—C(=Z)R10, —C(=NOR10)R10, —C(=Z)NR10OR12, —N(R11)—C(═NR13)—NY1Y2 or —N(R11)—C(=Z)OR11; L2 is a direct bond or a straight- or branched-carbon chain comprising from 2 to about 6 carbon atoms and contains a double or triple carbon-carbon bond; and R8 is hydrogen, aryl, cycloalkenyl, cycloalkyl, heteroaryl or heterocycloalk
    Type: Application
    Filed: May 13, 2003
    Publication date: February 26, 2004
    Applicant: AVENTIS PHARMA LIMITED
    Inventors: Paul L. Bamborough, Alan J. Collis, Frank Halley, Richard A. Lewis, David J. Lythgoe, Jeffrey M. McKenna, Iain M. McLay, Barry Porter, Andrew J. Ratcliffe, Paul A. Wallace
  • Publication number: 20040024014
    Abstract: The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated proton pump inhibitor compound, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.
    Type: Application
    Filed: August 1, 2003
    Publication date: February 5, 2004
    Applicant: NitroMed, Inc.
    Inventors: Xinqin Fang, David S. Garvey, L. Gordon Letts
  • Publication number: 20040019044
    Abstract: The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I 1
    Type: Application
    Filed: July 21, 2003
    Publication date: January 29, 2004
    Inventors: Dieter Dorsch, Henning Boettcher, Michael Arlt, Christoph Seyfried, Gerd Bartoszyk, Juergen Harting, Rudolf Gottschlich
  • Publication number: 20040019085
    Abstract: Compounds having the formula (I), 1
    Type: Application
    Filed: June 17, 2003
    Publication date: January 29, 2004
    Inventors: William A. Slusarchyk, Scott A. Bolton, Timothy Herpin, Gregory S. Bisacchi, Zulan Pi, E. Scott Priestley
  • Patent number: 6683097
    Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.
    Type: Grant
    Filed: February 11, 2003
    Date of Patent: January 27, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Patent number: 6683192
    Abstract: A compound represented in general formula (X) and (XI):
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: January 27, 2004
    Assignee: Curis, Inc.
    Inventors: Anthony David Baxter, Edward Andrew Boyd, Oivin M. Guicherit, Jeffrey Porter, Stephen Price, Lee Rubin, John Harry Alexander Stibbard
  • Patent number: 6673818
    Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.
    Type: Grant
    Filed: April 16, 2002
    Date of Patent: January 6, 2004
    Assignee: Pharmacia Corporation
    Inventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
  • Publication number: 20030236257
    Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Application
    Filed: January 31, 2003
    Publication date: December 25, 2003
    Inventors: Michael S. South, Chun C. Ma, Kevin J. Koeller, Hayat K. Rahman, William L. Neumann
  • Publication number: 20030229076
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: September 16, 2002
    Publication date: December 11, 2003
    Inventors: Stanislaw Rachwal, Alan Hutchison, Kenneth Shaw, George D. Maynard, Xiao-Shu He, Robert DeSimone, Kevin Hodgetts
  • Publication number: 20030229092
    Abstract: Bradykinin B1-receptor antagonists of formula 1
    Type: Application
    Filed: January 14, 2002
    Publication date: December 11, 2003
    Applicant: PHARMACOPEIA, INC.
    Inventors: Michael H.J. Ohlmeyer, John G. Baldwin, Roland E. Dolle, Vidyadhar Paradkar, Jorge Gabriel Quintero, Gonghua Pan
  • Publication number: 20030225138
    Abstract: The present invention relates to small molecules according to formula (I) that are potent inhibitors of &agr;L&bgr;2 mediated cell adhesion and which could be useful for the treatment of inflammatory diseases: 1
    Type: Application
    Filed: January 27, 2003
    Publication date: December 4, 2003
    Inventors: Ila Sircar, Yun Feng Xie, Nicholas Smith, Paul S Furth
  • Publication number: 20030220372
    Abstract: This invention provides a compound of the formula (I): 1
    Type: Application
    Filed: April 9, 2003
    Publication date: November 27, 2003
    Inventors: Misato Hirano, Satoru Iguchi, Kazunari Nakao, Tatsuya Yamagishi
  • Publication number: 20030216441
    Abstract: Compounds having the formula 1
    Type: Application
    Filed: May 10, 2002
    Publication date: November 20, 2003
    Inventors: Stephen L. Gwaltney, Lissa T.J. Nelson, Stephen J. O'Connor, Hing L. Sham, Gerard M. Sullivan, Weibo Wang
  • Publication number: 20030207896
    Abstract: The invention is directed to an imidazole derivative represented by formula (1): 1
    Type: Application
    Filed: November 5, 2002
    Publication date: November 6, 2003
    Inventors: Fujiko Konno, Yoshihiro Nagao, Kazuo Isomae, Mari Ohtsuka, Yoshiyuki Takahashi, Fumio Ishii, Hiroyuki Hirota, Sunao Takeda, Noriyuki Kawamoto, Haruyoshi Honda, Susumu Sato
  • Patent number: 6642379
    Abstract: Benzamide derivatives represented by the general formula (I): and insecticides for agricultural and horticultural use and usage thereof, wherein Z1 is O or S; R is H, (substituted) alkyl, or alkoxycarbonyl; X is halogeno, cyano, nitro, C3-C6(halo)cycloalkyl, (substituted) phenyl, a (substituted) heterocyclic group, or —A1—R1 [wherein A1 is —O—, —S—, —SO—, —SO2—, —C(═O)—, or —C(═NOR2)— (wherein R2 is H, C1-C6(halo)alkyl, (substituted) phenylated C1-C4 alkyl, or the like); and R1 is halogeno, C3-C6 cycloalkyl, C3-C6 halocycloalkenyl, (substituted) phenyl, or the like]; n is 0 to 4; Y is halogeno, cyano, nitro, C3-C6 halocycloalkyl, (substituted) phenyl, or the like; m is 1 to 5; Q is a heterocycle such as oxazoline; and B1 to B4 are each CH or N.
    Type: Grant
    Filed: April 4, 2002
    Date of Patent: November 4, 2003
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Takashi Furuya, Eiji Kohno, Masanori Tohnishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
  • Publication number: 20030203941
    Abstract: This invention provides compounds of formula I, having the structure 1
    Type: Application
    Filed: April 8, 2003
    Publication date: October 30, 2003
    Applicant: Wyeth
    Inventors: Joseph P. Sabatucci, Craig E. Caufield, Alexander A. Greenfield, Koi M. Morris, Eamonn P. Morrison
  • Publication number: 20030195188
    Abstract: The present invention provides compounds of formula (I) 1
    Type: Application
    Filed: February 11, 2003
    Publication date: October 16, 2003
    Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Claus Riemer, Peter Weiss
  • Publication number: 20030191311
    Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.
    Type: Application
    Filed: February 11, 2003
    Publication date: October 9, 2003
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Publication number: 20030186991
    Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.
    Type: Application
    Filed: April 15, 2003
    Publication date: October 2, 2003
    Applicant: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Taracad K. Venkatachalam
  • Publication number: 20030186947
    Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
    Type: Application
    Filed: February 11, 2003
    Publication date: October 2, 2003
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
  • Publication number: 20030187268
    Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.
    Type: Application
    Filed: February 13, 2003
    Publication date: October 2, 2003
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Publication number: 20030181479
    Abstract: The present invention relates to novel substituted imidazoles, to the use of these compounds as medicaments, to pharmaceutical compositions comprising the compounds, and to a method of treatment employing these compounds and compositions. The present compounds show a high and selective binding affinity to the histamine H3 receptor indicating a histamine H3 receptor antagonistic or agonistic activity. As a result, the compounds are useful for the treatment of disorders related to the histamine H3 receptor. More particularly, the present compounds possess a histamine H3 receptor agonistic activity and are accordingly useful in the treatment of disorders in which a histamine H3 receptor activation is beneficial.
    Type: Application
    Filed: November 8, 2002
    Publication date: September 25, 2003
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Klaus Rudolf, Rudolf Hurnaus, Dirk Stenkamp, Stephan Mueller, Bernd Krist
  • Publication number: 20030171218
    Abstract: A description is given of substituted 3-heteroaryl(amino- or oxy)pyrrolidin-2-ones of the formula (I), processes for preparing them, and their use as herbicides or as plant growth regulators.
    Type: Application
    Filed: July 9, 2002
    Publication date: September 11, 2003
    Inventors: Guido Bojack, Lothar Willms, Alfred Angermann, Hermann Bieringer, Hubert Menne, Thomas Auler
  • Publication number: 20030166633
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1, R2 and R3 represent various functional groups, and one of X1 and X2 is N and the other is NR10; and their use as pharmaceuticals.
    Type: Application
    Filed: October 29, 2002
    Publication date: September 4, 2003
    Inventors: Laramie Mary Gaster, Michael Stewart Hadley, John David Harling, Frank Peter Harrington, Jag Paul Heer, Thomas Daniel Heightman, Andrew Hele Payne
  • Patent number: 6610723
    Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: August 26, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Publication number: 20030158232
    Abstract: Compounds are provided which have the structure 1
    Type: Application
    Filed: November 14, 2002
    Publication date: August 21, 2003
    Inventors: Peter T. Cheng, Hao Zhang, Narayanan Hariharan
  • Publication number: 20030158418
    Abstract: Compounds represented by the general formula (I): 1
    Type: Application
    Filed: September 25, 2002
    Publication date: August 21, 2003
    Inventors: Nagaaki Sato, Osamu Okamoto, Makoto Jitsuoka, Keita Nagai, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Takehiro Fukami
  • Publication number: 20030153588
    Abstract: Compounds of 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, C1-6-alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, heterocyclylC1-6alkyl, heteroaryl, or heteroarylC1-6alkyl any of which except for hydrogen may be optionally substituted; R2 and R3 independently represent optionally substituted C1-6-alkyl, or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted C3-7cycloalkyl or C3-7cycloalkenyl ring; or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted 5 to 7-membered heterocyclyl ring containing up to 3 heteroatoms selected from N, O, S.
    Type: Application
    Filed: January 7, 2003
    Publication date: August 14, 2003
    Inventors: Jon Graham Steadman, Andrew Kenneth Takle
  • Publication number: 20030153567
    Abstract: Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Application
    Filed: January 29, 2003
    Publication date: August 14, 2003
    Applicant: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Joseph Weinstock, Jia-Ning Xiang