Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
Type:
Application
Filed:
September 17, 2001
Publication date:
November 28, 2002
Inventors:
Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Gunnar J. Hanson, Susan L. Hockerman, Susan C. Howard, Steve A. Kolodziej, Hui Li, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil
Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
Type:
Application
Filed:
December 3, 2001
Publication date:
November 21, 2002
Inventors:
John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
Abstract: Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Application
Filed:
August 14, 2001
Publication date:
November 21, 2002
Inventors:
Vincent Santora, Benny Askew, Arup Ghose, Andrew Hague, Tae Seong Kim, Ellen Laber, Aiwen Li, Brian Lian, Gang Liu, Mark Norman, Leon Smith, Andrew Tasker, Christopher Tegley, Kevin Yang
Abstract: Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (Ia), 1
Type:
Application
Filed:
December 18, 2001
Publication date:
November 21, 2002
Inventors:
Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Hans-Willi Jansen
Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.
Type:
Application
Filed:
December 11, 2001
Publication date:
November 14, 2002
Applicant:
Tularik Inc.
Inventors:
Julio C. Medina, Michael G. Johnson, An-Rong Li, Jiwen Liu, Alan Xi Huang, Liusheng Zhu, Andrew P. Marcus
Abstract: Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.
Type:
Application
Filed:
September 17, 2001
Publication date:
October 10, 2002
Inventors:
Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
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 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 31, 2001
Publication date:
September 26, 2002
Inventors:
Jing Wu, Eugene D. Thorsett, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Varghese John, Lawrence Y. Fang, James E. Audia
Abstract: The present invention relates to novel heterocyclyl-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
Type:
Application
Filed:
June 25, 2001
Publication date:
September 19, 2002
Inventors:
Gary T. Wang, Sheldon Wang, Robert Gentles
Abstract: Compounds of formula (I)
are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
Type:
Grant
Filed:
May 8, 1998
Date of Patent:
September 17, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
Abstract: The disclosed invention is a composition agonists and/or antagonists of V2, V1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.
Type:
Application
Filed:
December 17, 2001
Publication date:
September 12, 2002
Inventors:
James P. Snyder, Dennis C. Liotta, Hariharan Venkatesan, Minmin Wang, Matthew C. Davis
Abstract: The present invention relates beta-amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Abstract: The present invention relates to cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Abstract: The present invention relates to a method of treating depression, obsessive compulsive disorder and psychosis in a mammal, including a human, by administering to the mammal an atypical antipsychotic in combination with an antidepressant agent with improvement in efficiency. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, an atypical antipsychotic, and an SRI.
Abstract: Described are salts of hyperforin and adhyperforin of formula I
[A−]m[B]p+ (I)
wherein m is an integer from 1 to 3, p is equal to m and gives the total number of positive charges of the residue [B],
[A−] is an anion of formula II with n=0 or 1
and [B]p+ is an ion of an alkali metal or an ammonium ion of a salt-forming nitrogen base of formula III
wherein R1 through R4 have a variety of meanings including hydrogen, alkyl, cycloalkyl and similar groups which in turn may be substituted with one or more substituents. The salts serve inter alia for enriching or purifying hyperforin and adhyperforin from St. John's Wort extracts. Pharmaceutical preparations containing the salts are used for treating Alzheimer's Disease.
Type:
Grant
Filed:
August 11, 2000
Date of Patent:
September 3, 2002
Assignee:
Willmar Schwabe GmbH & Co.
Inventors:
Shyam Sunder Chatterjee, Clemens Erdelmeier, Klaus Klessing, Dieter Marme, Christoph Schächtele
Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.
Type:
Application
Filed:
December 13, 2000
Publication date:
August 29, 2002
Inventors:
Jeffrey W. Jacobs, Dinesh Patel, Jason Lewis, Zhi-Jie Ni
Abstract: This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmicokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic and neurological drugs, agents and compounds, for rapid and efficient introduction of such agents across the blood-brain barrier.
Type:
Grant
Filed:
February 15, 2000
Date of Patent:
August 20, 2002
Assignee:
Oregon Health and Science University
Inventors:
Milton B. Yatvin, Michael H. B. Stowell, Michael J. Meredith
Abstract: The present invention relates to amino-alkyl derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Abstract: The present invention provides non-steroidal compounds of Formula I, and prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.
Type:
Application
Filed:
October 26, 2001
Publication date:
August 8, 2002
Inventors:
Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Type:
Application
Filed:
January 3, 2002
Publication date:
August 8, 2002
Inventors:
David Lauffer, Brian Ledford, Michael Mullican
Abstract: Provided, among other things, is a method of treating, ameliorating or preventing certain fibrotic diseases or other indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I:
Type:
Application
Filed:
December 31, 2001
Publication date:
August 8, 2002
Inventors:
Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
Abstract: The present invention relates N-heterocyclic derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Type:
Application
Filed:
January 3, 2002
Publication date:
August 8, 2002
Inventors:
David Lauffer, Brian Ledford, Michael Mullican
Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a 5-HT3 receptor antagonist in combination with an SRI antidepressant agent with improvement in sexual function and/or reduction in gastro-intestinal side effects. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5-HT3 receptor antagonist and an SRI antidepressant.
Abstract: Use of agonists and antagonists of the nicotinergic acetylcholine receptors of insects for the non-systemic control of parasitic insects, such as fleas, lice and flies, on humans and on animals.
Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Abstract: The present invention relates to a method of treating depression, especially refractory depression, in a mammal, including a human, by administering to the mammal a sigma receptor ligand in combination with an antidepressant agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a sigma receptor ligand and a serotonin reuptake inhibitor.
Abstract: The invention relates to the use of 5-HT6 receptor antagonists containing arylsulfamide or arylaminosulfonyl groups in the manufacture of a medicament for the treatment of Attention Deficit Hyperactivity Disorder (ADHD).
Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I).
Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
Type:
Grant
Filed:
August 26, 1997
Date of Patent:
July 9, 2002
Assignee:
The Proctor & Gamble Company
Inventors:
Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
Abstract: N-Benzoyl arylsulfonamides having the formula 1
Type:
Application
Filed:
September 20, 2001
Publication date:
July 4, 2002
Inventors:
David J. Augeri, Steven A. Baumeister, Milan Bruncko, Daniel A. Dickman, Hong Ding, Jurgen Dinges, Stephen W. Fesik, Philip J. Hajduk, Aaron R. Kunzer, William McClellan, David G. Nettesheim, Thorsten Oost, Andrew M. Petros, Saul H. Rosenberg, Wang Shen, Sheela A. Thomas, Xilu Wang, Michael D. Wendt
Abstract: In accordance with the present invention, there is provided a class of compounds which are capable of modulating processes mediated by peroxisome proliferator activated receptor-gamma (PPAR-&ggr;). The identification of such compounds makes it possible to intervene in PPAR-&ggr; mediated pathways.
Type:
Grant
Filed:
February 16, 2001
Date of Patent:
July 2, 2002
Assignee:
The Salk Institute for Biological Studies
Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
Type:
Application
Filed:
November 30, 2001
Publication date:
June 27, 2002
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Andrew Spaltenstein, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski
Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
Type:
Application
Filed:
September 25, 2001
Publication date:
June 27, 2002
Inventors:
Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
February 28, 2000
Date of Patent:
June 25, 2002
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
Abstract: Benzene fused derivatives represented by the following formula:
having strong TXA2 receptor antagonistic action and PGI2 receptor agonistic action, and effective for treating or preventing diseases concerning TXA2.
Abstract: The invention relates to novel compounds of the formula
in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.
Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
Type:
Application
Filed:
December 14, 2001
Publication date:
June 6, 2002
Applicant:
Synaptic Pharamceutical Corporation
Inventors:
Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
Abstract: One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
Type:
Application
Filed:
September 12, 2001
Publication date:
May 30, 2002
Inventors:
Xinhe Wu, Brian M. Aquila, Liming Shao, Heike Radeke, Gregory D. Cuny, James R. Hauske, Roger L. Xie
Abstract: A class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: —O— Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.