Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,3- And 1,4- Benzothiazines, Etc.) Patents (Class 514/224.2)
  • Publication number: 20040014748
    Abstract: The invention relates to the use of inhibitors of the microsomal triglyceride transfer protein (MTP) for reducing the number of postprandial triglyceride-rich lipoprotein particles (ppTRL) or for reducing their decomposition products i.e. the cholestcrol-rich “small remnant particle” (remnants). Said particles are associated with apolipoprotein B-48 (ApoB-48) and are designated as “ppTRL” in the further course of events.
    Type: Application
    Filed: May 12, 2003
    Publication date: January 22, 2004
    Inventors: Rudi Grutzmann, Ulrich Muller, Hilmar Bischoff, Siegfried Zaiss
  • Publication number: 20040006062
    Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: 1
    Type: Application
    Filed: May 5, 2003
    Publication date: January 8, 2004
    Inventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
  • Publication number: 20040006075
    Abstract: Compounds of formula I, their tautomeric and isomeric forms and salts, 1
    Type: Application
    Filed: July 23, 2003
    Publication date: January 8, 2004
    Inventors: Hartmut Rehwinkel, Peter Hoelscher, Stefan Jaroch, Detley Suelzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Macdougall
  • Publication number: 20040001883
    Abstract: The present invention relates to suppositories consisting essentially of the active ingredient meloxicam or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.
    Type: Application
    Filed: March 21, 2003
    Publication date: January 1, 2004
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Mayumi Matsui, Toshimitsu Ohki, Koichi Wada
  • Publication number: 20040002491
    Abstract: The invention concerns compounds of formula (1): R-A-R′ wherein: A is as defined in the description; R represent a group (V), (VI), (VII), or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description, and medicaments containing the same.
    Type: Application
    Filed: June 16, 2003
    Publication date: January 1, 2004
    Inventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Publication number: 20040002490
    Abstract: The invention concerns compounds of formula (I): R-A-R′ wherein: A is as defined in the description; R represent a group (V), (VI), (VII), or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description, and medicaments containing the same.
    Type: Application
    Filed: June 16, 2003
    Publication date: January 1, 2004
    Inventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Publication number: 20030236245
    Abstract: Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: 1
    Type: Application
    Filed: August 29, 2002
    Publication date: December 25, 2003
    Applicant: Molecumetics, Ltd.
    Inventors: Vincent Huber, Jan Urban, Hiroshi Nakanishi, Masakatsu Eguchi, Jessymol Mathew, Min Sang Lee
  • Publication number: 20030232809
    Abstract: The present invention provides a lipid-rich plaque regressing agent comprising a compound represented by Formula: 1
    Type: Application
    Filed: January 10, 2003
    Publication date: December 18, 2003
    Inventors: Zen-ichi Terashita, Masahira Nakamura, Shogo Marui, Masaki Ogino
  • Publication number: 20030229026
    Abstract: The present invention provides selective kinase inhibitors of formula (I).
    Type: Application
    Filed: December 2, 2002
    Publication date: December 11, 2003
    Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, James Edward Ray, Jianping Huang, Sajan Joseph, Tiechao Li, Michael Paal, Radhakrishnan Rathnachalam, Chuan Shih, Philip Parker Waid, Xun Zhou, Guoxin Zhu
  • Publication number: 20030229081
    Abstract: The present application describes novel uracil derivatives of formula I:
    Type: Application
    Filed: March 14, 2003
    Publication date: December 11, 2003
    Inventor: Thomas P. Maduskuie
  • Publication number: 20030225069
    Abstract: The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.
    Type: Application
    Filed: March 12, 2002
    Publication date: December 4, 2003
    Inventor: Simon N. Haydar
  • Publication number: 20030225070
    Abstract: This invention relates to the treatment of mGluR5 receptor mediated disorders, which comprises administering to a person in need of treatment a compound having the formula 1
    Type: Application
    Filed: April 4, 2003
    Publication date: December 4, 2003
    Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
  • Publication number: 20030225056
    Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula 1
    Type: Application
    Filed: April 25, 2003
    Publication date: December 4, 2003
    Applicant: Pfizer Inc.
    Inventors: Kevin D. Freeman-Cook, Mark C. Noe
  • Publication number: 20030212061
    Abstract: The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.
    Type: Application
    Filed: March 12, 2002
    Publication date: November 13, 2003
    Inventor: Simon N. Haydar
  • Publication number: 20030207868
    Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.
    Type: Application
    Filed: December 4, 2002
    Publication date: November 6, 2003
    Inventors: Kuo-Long Yu, Xiangdong Wang, Yaxiong Sun, Christopher Cianci, Jan Willem Thuring, Keith Combrink, Nicholas Meanwell, Yi Zhang, Rita L. Civiello
  • Publication number: 20030203897
    Abstract: This invention concerns the use of a compound of formula (I′) 1
    Type: Application
    Filed: August 29, 2002
    Publication date: October 30, 2003
    Inventors: Christopher Love, Jean Pierre Frans Van Wauwe, Marc De Brabander, Ludwig Cooymans, Nele Vandermaesen, Ludo Edmond Josephine Kennis
  • Publication number: 20030199497
    Abstract: The invention concerns compounds of general formula (I) wherein: 1
    Type: Application
    Filed: April 24, 2003
    Publication date: October 23, 2003
    Inventors: Martial Ruat, Robert Dodd, Helene Veronique Faure, Philippe Marcel Dauban, Albane Kessler, Pierre Jean-Paul Potier
  • Publication number: 20030195199
    Abstract: The subject invention features compounds having the structure: 1
    Type: Application
    Filed: December 20, 2002
    Publication date: October 16, 2003
    Inventors: David Witter, Arlindo Castelhano
  • Publication number: 20030191109
    Abstract: There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, the &bgr;-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The &bgr;-sheet mimetics have utility as inhibitors of one or more of proteases, kinases, CAAX, peptides binding to SH2 domains and MHC-I and/or MHC-II presentation of peptides to T cell receptors in warm-blooded animals.
    Type: Application
    Filed: October 25, 2001
    Publication date: October 9, 2003
    Inventor: Michael Kahn
  • Publication number: 20030191115
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: 1
    Type: Application
    Filed: September 17, 2002
    Publication date: October 9, 2003
    Inventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
  • Publication number: 20030191116
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors.
    Type: Application
    Filed: April 10, 2003
    Publication date: October 9, 2003
    Inventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Caroline Minli Rachel Low, Matthew John Tozer
  • Publication number: 20030186970
    Abstract: Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.
    Type: Application
    Filed: September 9, 2002
    Publication date: October 2, 2003
    Inventors: Robert Higuchi, Kristen L. Arienti, Mani Neelakandha, Barbara Pio, Lin Zhi, Penghui Chen, Thomas R. Caferro
  • Publication number: 20030186901
    Abstract: The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.
    Type: Application
    Filed: August 16, 2002
    Publication date: October 2, 2003
    Inventors: Gregory M. Ross, Igor L. Shamovsky, Sandra Marone, Donald F. Weaver, Richard J. Riopelle
  • Publication number: 20030187256
    Abstract: This invention discloses benzoxazinone and benzothiazinone compounds which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.
    Type: Application
    Filed: November 12, 2002
    Publication date: October 2, 2003
    Inventors: Kent Alan Berryman, Dennis Michael Downing, Danette Andrea Dudley, Jeremy John Edmunds, Lakshmi Sourirajan Narasimhan, Stephen Taras Rapundalo
  • Publication number: 20030186971
    Abstract: The present invention is intended to provide excellent preventives and/or remedies for heart diseases.
    Type: Application
    Filed: February 27, 2003
    Publication date: October 2, 2003
    Inventors: Harihide Kimura, Seiichi Tanida, Tatsuhiko Kaneko
  • Publication number: 20030176422
    Abstract: Pyridoarylphenyl oxazolidinone compounds of the formula: 1
    Type: Application
    Filed: February 6, 2002
    Publication date: September 18, 2003
    Inventors: Steven D. Paget, Michele A. Weidner-Wells, Harvey M. Werblood
  • Publication number: 20030176421
    Abstract: Stasis is treated or prevented in all or any part or parts of the stomach of a patient, especially a human patient, in need of such treatment, where said stasis results from hypomotility in the stomach, particularly gastric hypomotility with delayed emptying of the liquid and/or solid contents of the stomach. Gastric or gastrointestinal disorders are also treated which are characterized by one or more symptoms selected from pain, nausea, vomiting, heartburn, postprandial discomfort, indigestion and gastroesophageal reflux. Such treatment or prevention is achieved by administering to the patient a therapeutically effective amount of an inhibitor of phosphodiesterase-4 (PDE4), including isozyme subtypes thereof, sufficient to treat or prevent such hypomotility or gastric or gastrointestinal disorder in said patient.
    Type: Application
    Filed: December 30, 1999
    Publication date: September 18, 2003
    Inventors: JOHN W. WATSON, PAUL L. R. ANDREWS, ANTHONY J. WOODS
  • Publication number: 20030171366
    Abstract: Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: 1
    Type: Application
    Filed: January 10, 2002
    Publication date: September 11, 2003
    Inventors: Steven Paget, Dennis Hlasta
  • Publication number: 20030166640
    Abstract: Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: 1
    Type: Application
    Filed: May 16, 2002
    Publication date: September 4, 2003
    Applicant: Molecumetics, Ltd.
    Inventors: Jan Urban, Hiroshi Nakanishi, Min S. Lee
  • Publication number: 20030166928
    Abstract: The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
    Type: Application
    Filed: December 23, 2002
    Publication date: September 4, 2003
    Inventor: Nathalie Schlienger
  • Publication number: 20030158181
    Abstract: A method for treating cerebral ischaemia which comprises administering a compound of general formula (I) 1
    Type: Application
    Filed: January 6, 2003
    Publication date: August 21, 2003
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Karin Winter, Thomas Weiser, Stefan M. Blech, Angelo Ceci
  • Publication number: 20030158182
    Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure 1
    Type: Application
    Filed: January 15, 2003
    Publication date: August 21, 2003
    Applicant: Wyeth
    Inventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Publication number: 20030153558
    Abstract: The present invention relates to 4-pyridyl- und 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1 1
    Type: Application
    Filed: November 5, 2002
    Publication date: August 14, 2003
    Inventors: Hans-Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
  • Publication number: 20030149017
    Abstract: The present invention relates to 2-aminopyridine derivatives of the formula 1
    Type: Application
    Filed: December 6, 2002
    Publication date: August 7, 2003
    Applicant: Pfizer Inc.
    Inventor: John Adams Lowe
  • Publication number: 20030149028
    Abstract: The invention relates to a compound which is a 4-spirocyclic pyrazole of formula (I): 1
    Type: Application
    Filed: September 11, 2002
    Publication date: August 7, 2003
    Inventors: Juriy Grigorievich Shermolovich, Uwe Doller, Sergiy Vasiliovich Yemets, Maria-Theresia Thonessen, Waltraud Hempel
  • Patent number: 6602868
    Abstract: The invention provides methods and use of heterocyclic amines, and phenylazacycloalkane compounds, and their pharmacologically acceptable salts for the treatment of Restless Legs Syndrome (RLS).
    Type: Grant
    Filed: October 29, 2001
    Date of Patent: August 5, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: Sylvia McBrinn, Richard Wayne Anderson
  • Publication number: 20030144275
    Abstract: The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.
    Type: Application
    Filed: December 12, 2002
    Publication date: July 31, 2003
    Applicant: AstraZeneca AB
    Inventors: Keith Fagnou, Mark Lautens
  • Publication number: 20030144276
    Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1
    Type: Application
    Filed: January 6, 2003
    Publication date: July 31, 2003
    Applicant: Eisai Co. Ltd.
    Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
  • Publication number: 20030139399
    Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
    Type: Application
    Filed: February 4, 2003
    Publication date: July 24, 2003
    Inventors: Michael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
  • Publication number: 20030139389
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:
    Type: Application
    Filed: December 11, 2002
    Publication date: July 24, 2003
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
  • Publication number: 20030139398
    Abstract: The invention is directed to novel quinazoline and quinazoline-like derivatives of Formula (I): 1
    Type: Application
    Filed: April 5, 2002
    Publication date: July 24, 2003
    Inventors: William J. Hoekstra, Edward C. Lawson, Michael J. Costanzo
  • Publication number: 20030139400
    Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
    Type: Application
    Filed: February 6, 2003
    Publication date: July 24, 2003
    Inventors: Michael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
  • Publication number: 20030130257
    Abstract: The present application describes to novel bicyclic hydroxamates derivatives of formula I: 1
    Type: Application
    Filed: August 15, 2002
    Publication date: July 10, 2003
    Inventors: James E. Sheppeck, Jingwu Duan
  • Publication number: 20030119785
    Abstract: The present invention relates to compounds of the formula I,
    Type: Application
    Filed: November 19, 2002
    Publication date: June 26, 2003
    Applicant: Hoechst Aktiengesellschaft and Genentech Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Publication number: 20030105085
    Abstract: Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.
    Type: Application
    Filed: February 27, 2002
    Publication date: June 5, 2003
    Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
  • Publication number: 20030096804
    Abstract: This invention relates generally to a novel class of bicyclic heterocyclic compounds of the Formula (I): 1
    Type: Application
    Filed: May 22, 2002
    Publication date: May 22, 2003
    Inventors: Irina C. Jacobson, Mimi L. Quan, Yun-Long Li, Ruth R. Wexler, Patrick Y.S. Lam
  • Publication number: 20030087898
    Abstract: The subject invention provides a compound of the formula 1, 1
    Type: Application
    Filed: October 22, 2002
    Publication date: May 8, 2003
    Applicant: Pfizer Inc.
    Inventors: Stanton F. McHardy, Spiros Liras, Steven D. Heck
  • Publication number: 20030087897
    Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.
    Type: Application
    Filed: May 10, 2002
    Publication date: May 8, 2003
    Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
  • Publication number: 20030087883
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: September 19, 2002
    Publication date: May 8, 2003
    Inventor: Jian-Min Fu
  • Publication number: 20030078258
    Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.
    Type: Application
    Filed: December 7, 2001
    Publication date: April 24, 2003
    Inventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich