Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
Type:
Grant
Filed:
August 23, 2004
Date of Patent:
October 30, 2007
Assignee:
Encysive Pharmaceuticals, Inc.
Inventors:
Chengde Wu, Daxin Gao, Ronald Biediger, Jie Chen, Robert V. Market
Abstract: Compounds of formula I in free or salt form, wherein Ar, X, Y, R1, R2, R3, R5, m, n, p and q have the meanings as indicated in the specification, are useful for treating conditions mediated by CCR3. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
Type:
Grant
Filed:
March 14, 2003
Date of Patent:
October 30, 2007
Assignee:
Novartis AG
Inventors:
Darren Mark Le Grand, Clive McCarthy, Clive Victor Walker, John James Woods
Abstract: Fluorescent dyes and probes are key components in multiphoton based fluorescence microscopy imaging of biological samples. In order to address the demand for better performing dyes for two-photon based imaging, a new series of reactive fluorophores tailored for multiphoton imaging has been disclosed. These fluorophores are based upon the fluorene ring system, known to exhibit high fluorescence quantum yields, typically >0.7, and possess high photostability. They have been functionalized with moieties to act, e.g., as efficient amine-reactive fluorescent probes for the covalent attachment onto, e.g., proteins and antibodies. The synthesis and the single-photon spectral characteristics, as well as measured two-photon absorption cross sections of the reactive fluorophores in solution are presented. Spectral characterizations of bovine serum albumin (BSA) conjugated with the new reactive probe is presented.
Type:
Grant
Filed:
April 11, 2007
Date of Patent:
October 16, 2007
Assignee:
Research Foundation of The University of Central Florida, Inc.
Inventors:
Kevin D. Belfield, Katherine J. Schafer
Abstract: This invention provides estrogen receptor modulators having the structure: wherein R1 to R6 and R8 are as defined in the specification; or a pharmaceutically acceptable salt thereof.
Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.
Type:
Grant
Filed:
August 13, 2002
Date of Patent:
October 9, 2007
Assignee:
Karo Bio AB
Inventors:
Johan Malm, Peter Brandt, Karin Edvinsson, Konrad Koehler, Andrei Sanin, Sandra Gordon
Abstract: The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
Type:
Grant
Filed:
April 15, 2005
Date of Patent:
October 9, 2007
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Kirsten Arndt, Henri Doods, Gerhard Schaenzle
Abstract: A compound of formula I wherein R1 represents chloro, fluoro or hydroxy as well as optical isomers and racemates thereof as well as pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, processes for preparing such compounds, their utility in treating clinical conditions associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 18, 2002
Date of Patent:
October 2, 2007
Assignee:
AstraZeneca AB
Inventors:
Eva-Lotte Alstermark Lindstedt, Anna Maria Persdotter Boije, Patrick Holm
Abstract: There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of ?-lactamase inhibitors.
Type:
Grant
Filed:
May 12, 2004
Date of Patent:
October 2, 2007
Assignee:
Wyeth Holdings Corporation
Inventors:
Michael William Winkley, Anita Wai-Yin Chan, Ivo L. Jirkovsky, Kenneth Alfred Martin Kremer, Joseph Zeldis, Antonia Aristotelevna Nikitenko, Henry Lee Strong, Tarek Mansour, Gulnaz Khafizova, Aranapakam M. Venkatesan
Abstract: The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof:
Type:
Grant
Filed:
July 15, 2002
Date of Patent:
September 25, 2007
Assignees:
SB Pharmco Puerto Rico Inc., Neurocrine Biosciences Inc.
Inventors:
Romano Di Fabio, Collin F Regan, Yves St-Denis, Fabrizio Micheli, Michael K Schwaebe
Abstract: Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R11 and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
Abstract: New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C ?-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.
Type:
Grant
Filed:
December 9, 2003
Date of Patent:
September 18, 2007
Assignees:
Northwestern University, University of Modena
Abstract: Pharmaceutically suitable crystalline and amorphous alkali and earth-alkali salts of 2-n-butyl-4-chloro-5-hidrox-ymethyl-1-[[2?-(1 H-tetrazole-5-yl)[1.1?-biphenyl]-4-yl]-1 Himidazole have been prepared and new manufacturing, purification and isolation procedure for said salts in high purity have been described. Stable pharmaceutical compositions containing new crystalline potassium salts of 2-n-butyl-5-chloro-5hidroxymethyl-1-[[2?-(1H-tetrazole-5-yl)[1.1?-biphenyl]-44-yl]-1H-imidazole have been prepared.
Type:
Grant
Filed:
January 29, 2004
Date of Patent:
September 18, 2007
Assignee:
Lek Pharmaceuticals D.D.
Inventors:
Ljubomir Antoncic, Anton Copar, Peter Svete, Breda Husu-Kovacevic, Zoran Ham, Boris Marolt
Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
Type:
Grant
Filed:
February 27, 2004
Date of Patent:
August 28, 2007
Assignee:
Abbott Laboratories
Inventors:
David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
Abstract: Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
Type:
Grant
Filed:
May 20, 2005
Date of Patent:
August 28, 2007
Assignee:
Telik, Inc.
Inventors:
Louise Robinson, Steven R. Schow, Songyuan Shi
Abstract: The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.
Type:
Grant
Filed:
October 17, 2005
Date of Patent:
August 14, 2007
Assignee:
Celgene Corporation
Inventors:
Hon-Wah Man, George W. Muller, Weihong Zhang
Abstract: The present invention relates to novel compounds useful in the treatment of androgen receptor associated conditions, such as age-related diseases, pharmaceutical compositions containing at least one of the compounds of the present invention and methods of treating a patient in need of therapy for an androgen receptor associated condition by administering a therapeutically effective amount of at least compound of the present invention.
Type:
Grant
Filed:
November 9, 2004
Date of Patent:
August 14, 2007
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yingzhi Bi, Lawrence G. Hamann, Mark C. Manfredi, Ligaya M. Simpkins
Abstract: Fluorescent dyes and probes are key components in multiphoton based fluorescence microscopy imaging of biological samples. In order to address the demand for better performing dyes for two-photon based imaging, a new series of reactive fluorophores tailored for multiphoton imaging has been disclosed. These fluorophores are based upon the fluorene ring system, known to exhibit high fluorescence quantum yields, typically >0.7, and possess high photostability. They have been functionalized with moieties to act, e.g., as efficient amine-reactive fluorescent probes for the covalent attachment onto, e.g., proteins and antibodies. The synthesis and the single-photon spectral characteristics, as well as measured two-photon absorption cross sections of the reactive fluorophores in solution are presented. Spectral characterizations of bovine serum albumin (BSA) conjugated with the new reactive probe is presented.
Type:
Grant
Filed:
May 13, 2005
Date of Patent:
August 7, 2007
Assignee:
Research Foundation of The University of Central Florida, Inc.
Inventors:
Kevin D. Belfield, Katherine J. Schafer
Abstract: Disclosed is a novel use of a prostaglandin compound as a chloride channel opener. According to the instant invention, chloride channels in a mammalian subject can be opened by a prostaglandin compound to facilitate chloride ion transportation.
Abstract: The invention is concerned with novel hexafluoroisopropanol substituted cyclohexane derivatives of formula (I) wherein R1 to R4, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
Abstract: Benzodioxepines of the formula (I) and physiologically tolerated salts and solvates thereof, in which R1, R2, R3, R4, A, B, a and b have the meanings indicated in claim 1, are ligands of the 5HT1A receptors and/or the 5HT4 receptors with simultaneously strong serotonin reuptake inhibition.
Type:
Grant
Filed:
November 27, 2003
Date of Patent:
August 7, 2007
Assignee:
Merck Patent GmbH
Inventors:
Timo Heinrich, Henning Böttcher, Kai Schiemann, Günter Hölzemann, Christoph van Amsterdam, Gerd Bartoszyk, Hartmut Greiner, Christoph Seyfried, Michel Brunet, Jean Zeiller, Jean Berthelon