Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed 1
Type:
Application
Filed:
October 27, 2003
Publication date:
June 3, 2004
Applicant:
Aventis Pharma Deutschland GmBH
Inventors:
Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed 1
Type:
Application
Filed:
October 27, 2003
Publication date:
May 13, 2004
Applicant:
Aventis Pharma Deutschland GmBH
Inventors:
Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
Abstract: The present invention discloses a method for treating HIV that includes administering &mgr;-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using &bgr;-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. &bgr;-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.
Type:
Application
Filed:
January 23, 2003
Publication date:
April 29, 2004
Inventors:
Raymond F. Schinazi, Jennifer L. Hammond, John W. Mellors, Dennis C. Liotta
Abstract: A treatment for inhibiting microbial or tumor growth is disclosed, which comprises adding to a subject in need of treatment an effective amount of one or more tetracycline derivatives.
Abstract: The present invention pertains to certain N8,N13-disubstituted quino[4,3,2-kl]acridinium salts of formula (Q−) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4; each RA is —H or a ring substituent; each RB is —H or a ring substituent; each RC is —H or a ring substituent; RN8 is a nitrogen substituent; RN13 is a nitrogen substituent; and, Q is an anion. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.
Type:
Application
Filed:
October 7, 2003
Publication date:
April 1, 2004
Inventors:
Malcolm F. G. Stevens, Lloyd R. Kelland, Robert A. Heald
Abstract: Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
Type:
Application
Filed:
July 28, 2003
Publication date:
March 18, 2004
Inventors:
Norbert W. Bischofberger, Terrence C. Dahl, Michael J. M. Hitchcock, Choung U. Kim, Willard Lew, Hongtao Liu, Roger G. Mills, Matthew A. Williams
Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.
Type:
Application
Filed:
March 24, 2003
Publication date:
February 12, 2004
Applicant:
Merck Frosst Canada & Co.
Inventors:
Daniel Dube, Rejean Fortin, Richard Friesen
Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.
Type:
Application
Filed:
April 3, 2003
Publication date:
February 5, 2004
Applicant:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.
Abstract: The invention provides &bgr;3-adrenoreceptor agonists, pharmaceutical compositions comprising &bgr;3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.
Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.
Type:
Application
Filed:
April 2, 2003
Publication date:
January 8, 2004
Applicant:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: The invention relates to novel 3, 5, and/or 6 swainsoninc analogues, processes for their preparation and their use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.
Type:
Application
Filed:
October 7, 2002
Publication date:
December 25, 2003
Applicant:
GlycoDesign Inc.
Inventors:
Rajan Shah, Jeremy Carver, Jose Marino-Albernas, Igor Tvaroska, Francois Daniel Tropper, James Dennis
Abstract: Compounds useful for inducing apoptosis in proliferative cells, particularly cancer cells, including but not limited to prostate cancer, leukemia, non-smalll cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, bladder cancer, lymphoma, and breast cancer. These compounds are particularly useful in the treatment of androgen-independent cancers, including hormone-refractory prostate cancer. Further provided are methods of treating cancer in a subject in need of such treatment using the compounds of the present invention. Further provided are methods for using the compounds of the present invention to treat, inhibit, or delay the onset of cancer in a subject. Further provided are methods of inducing apoptosis in rapidly proliferating cells, particularly, though not necessarily cancer cells, using the compounds of the present invention.
Type:
Application
Filed:
April 8, 2003
Publication date:
December 25, 2003
Inventors:
Ching-Shih Chen, Xueqin Song, Ho-Pi Lin
Abstract: This invention relates to novel fluorinated phenyl thiphenyl (also named diarylsulfide) derivatives and their use in Positron Emission Tomagraphy (PET) imaging of Serotonin Transporters (SERTS). The present invention also provides diagnostic compositions comprising the novel compounds of the present invention, and a pharmaceutically acceptable carrier or diluent. The invention further provides a method of imaging SERTS, comprising introducing into a patient a detectable quantity of a labeled compound of the present invetion, or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.
Type:
Application
Filed:
March 14, 2003
Publication date:
December 25, 2003
Inventors:
Hank F. Kung, Chyng-Yann Shiue, Shunichi Oya, Seok Rye Choi, Grace G. Shiue, Ping Fang
Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.
Type:
Application
Filed:
November 18, 2002
Publication date:
December 18, 2003
Inventors:
Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.
Type:
Grant
Filed:
December 4, 2000
Date of Patent:
December 16, 2003
Assignee:
Emory University
Inventors:
James P. Snyder, Matthew C. Davis, Brian Adams, Mamoru Shoji, Dennis C. Liotta, Eva M. Ferstl, Ustun B. Sunay
Abstract: Novel formulations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and swine respiratory disease, are also disclosed.
Type:
Application
Filed:
January 24, 2003
Publication date:
November 27, 2003
Applicant:
Schering-Plough Animal Health Corporation
Inventors:
Raul E. Kohan, Kanwal J. Varma, Robert D. Simmons, Abu Huq, Keith A. Freehauf
Abstract: Novel formulations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and swine respiratory disease, are also disclosed.
Type:
Application
Filed:
May 20, 2003
Publication date:
November 20, 2003
Applicant:
SCHERING-PLOUGH ANIMAL HEALTH
Inventors:
Raul E. Kohan, Kanwal J. Varma, Robert D. Simmons, Abu Huq
Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Type:
Application
Filed:
September 17, 2002
Publication date:
November 20, 2003
Inventors:
Michael R. Palovich, Katherine L. Widdowson, Hong Nie
Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.
Type:
Application
Filed:
October 7, 2002
Publication date:
November 13, 2003
Applicant:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: A method of modulating the activity of a aberrant cell topoisomerase enzyme involving contacting the enzyme with a compound that inhibits enzyme-mediated cleavage of a polynucleotide substrate with which the enzyme is in complex. Pharmaceutical compositions containing such compounds may be used to treat neoplasias or to inhibit the growth of certain cancer cells. Screening methods can be employed to identify other compounds for these uses.
Type:
Application
Filed:
May 20, 2003
Publication date:
October 30, 2003
Applicant:
SmithKline Beecham Corporation and SmithKline Beecham p.l.c.
Inventors:
Symon G. Erskine, Michael Gwynn, Neil David Pearson, Edwina Imogen Wilding
Abstract: The invention provides pharmaceutically useful thieno[2,3-d]pyrimidinediones, processes for their production, pharmaceutical compositions containing them and methods of treatment involving their use.
Type:
Application
Filed:
October 7, 2002
Publication date:
October 9, 2003
Applicant:
AstraZeneca AB
Inventors:
David Cheshire, Andrew Cooke, Martin Cooper, David Donald, Mark Furber, Matthew Perry, Philip Thorne
Abstract: Imidazopyridine compounds that contain amide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
Type:
Application
Filed:
February 4, 2003
Publication date:
October 2, 2003
Applicant:
3M Innovative Properties Company
Inventors:
Joseph F. Dellaria, Chad A. Haraldson, Kyle J. Lindstrom, Bryon A. Merrill
Abstract: The present invention relates to a method for detecting an agent for use in the treatment of herpes virus infection and use of known agents, such as 2,2′-dithiobisbenzamide (DIBA) and azodicarbonamide (ADA), and unknown agents, which selectively eject zinc bound to a zinc finger protein, for the manufacture of a medicament for the treatment of herpesvirus infections.
Type:
Application
Filed:
February 11, 2003
Publication date:
October 2, 2003
Inventors:
John Barklie Clements, Alasdair Roderick Maclean
Abstract: The invention concerns the use of certain compounds related to fatty acids to control nematodes that infest plants or the situs of plants. Nematodes that parasitize animals can also be controlled using the methods and composition of this invention. Certain of the useful compounds are fatty acid esters that are predicted inhibitors of nematode delta-12 fatty acid desaturases and can be, for example, from C16 to C20 in length.
Type:
Application
Filed:
July 1, 2002
Publication date:
September 18, 2003
Inventors:
Deryck J. Williams, Andrew P. Kloek, Michelle Coutu Hresko
Abstract: The present invention relates to methods of preparation and use of coumarin and chromene compounds for treating or preventing viral infections.
Type:
Application
Filed:
November 15, 2002
Publication date:
September 18, 2003
Inventors:
Ze-Qi Xu, Hongwei Yuan, Jennifer Crabb, Raghu Samy, Ailing Li, Hua Cao, Jeff Deignan, Lihui Sun
Abstract: The present invention relates to novel oxazolidinone derivatives, their pharmaceutically acceptable salts and a process for the preparation thereof. More particularly, the present invention relates to oxazolidinone derivatives having pyridine or pyrimidine moeity substituted by heterocycle and heteroaromaticcycle at 4-position of phenyl ring. The compounds of the present invention have wide antibacterial spectrum, superior antibacterial activity and low toxicity, such that the compound of this invention can be used as an antibacterial agent.
Type:
Application
Filed:
November 27, 2002
Publication date:
September 4, 2003
Inventors:
Jae-Gul Lee, Won-Bin Leem, Jong-Hwan Cho, Sung-Hak Choi, Jong-Jin Lee, Sang-Kuk Park, Tae-Hoo Lee, Dong-Goo Kim, Hyun-Jung Sung
Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Type:
Application
Filed:
October 7, 2002
Publication date:
August 14, 2003
Inventors:
James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
Abstract: Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.
Type:
Application
Filed:
October 28, 2002
Publication date:
August 7, 2003
Inventors:
David J. Chaplin, Charles Manly Garner, Robert Ronald Kane, Kevin G. Pinney, Joseph Anthony Prezioso, Klaus Edvardsen
Abstract: This invention relates to a method of using novel 5-(arylsulfonyl)-, 5-(arylsulfinyl)- and 5-(arylsulfanyl)thiazolidine-2,4-diones of Formula (1), wherein Ar, Ar′, R6, m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras- oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.
Type:
Application
Filed:
August 23, 2002
Publication date:
July 31, 2003
Applicant:
American Cyanamid Company
Inventors:
Semiramis Ayral-Kaloustian, Joseph William Epstein, Gary H. Birnberg, Edward James Salaski, Gloria Macewan, Katherine Cheung
Abstract: The present invention provides compounds of formula Ia and Ib
or a pharmaceutically acceptable salt, prodrug, or ester thereof, useful in the inhibition of neuraminidase enzymes from disease-causing microorganisms, especially influenza neuraminidase, pharmaceutical formulations containing same, processes and intermediates for preparing said compounds, as well as methods of using said compounds, including preventing and treating diseases caused by microorganisms having said neuraminidase enzyme.
Type:
Grant
Filed:
September 22, 2000
Date of Patent:
July 15, 2003
Assignee:
Abbott Laboratories
Inventors:
Clarence J. Maring, Vincent L. Giranda, Yu Gui Gu, Stephen Hanessian, Dale J. Kempf, Darold L. Madigan, Kent Stewart, Vincent S. Stoll, Minghua Sun, Gary T. Wang, Jianchio Wang, Chen Zhao
Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.
Type:
Application
Filed:
May 9, 2002
Publication date:
June 26, 2003
Inventors:
John William Lackey, Daniel S. Kinder, Nicolai A. Tvermoes
Abstract: It is shown here that hedgehog proteins possess novel activities beyond phenotype specification. Using cultures derived from the embryonic day 14.5 (E14.5) rat ventral mesencephalon, we show that hedgehog is also trophic for dopaminergic neurons. Interestingly, hedgehog not only promotes dopaminergic neuron survival, but also promotes the survival of midbrain GABA-immunoreactive (GABA-ir) neurons.
Type:
Application
Filed:
December 1, 1999
Publication date:
June 26, 2003
Inventors:
NINGNING MIAO, MONICA WANG, NAGESH K. MAHANTHAPPA, PING JIN, KEVIN PANG
Abstract: The present invention relates to compounds useful as inhibitors of CAK, compositions thereof. The present invention also relates to methods using the compositions for treating CAK-mediated diseases, such as fungal infections.
Type:
Application
Filed:
June 6, 2002
Publication date:
June 26, 2003
Inventors:
Brian Ledford, Cameron Stuver Moody, Michael Mullican, Mark Namchuk
Abstract: Novel sulphones of formula I are disclosed: 1
Type:
Application
Filed:
August 20, 2002
Publication date:
June 19, 2003
Inventors:
Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Duncan Edward Shaw, Martin Richard Teall, Susannah Williams, Brian John Williams
Abstract: This invention pertains to a method for treating a human with human immunodeficiency virus infection which comprises administering to the human a therapeutically effective amount of a thymidine analog, which analog acts as an inhibitor of viral reverse transcriptase necessary for viral replication of human immunodeficiency virus, and a thymidylate synthase inhibitor, or pharmaceutically acceptable salts thereof.
Type:
Application
Filed:
May 17, 2002
Publication date:
May 29, 2003
Applicant:
UNIVERSITY OF MEDICINE & DENTISTRY OF NEW JERSEY
Inventors:
Roger Strair, Daniel Medina, Peter Tung