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.
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
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
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
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
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
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.
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
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.
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
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.
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
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
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
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
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
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.
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
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).
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.
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
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
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
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
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
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
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