Abstract: The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase and TNF-alpha activity and consequently, can be advantageously used as agents against caspase-, interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), interferon-?-(“IFN-?”), or TNF-alpha mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to processes for preparing the compounds of this invention.
Type:
Grant
Filed:
September 14, 2006
Date of Patent:
October 5, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Anita Diu-Hercend, Julian Golec, Thierry Hercend, Ronald Knegtel, Paul Lang, Andrew Miller, Karen Miller, Michael Mortimore, Peter Weber
Abstract: A novel water detection composition for use in place of blue gel and a water detection indicator. The water detection composition comprises, as active components, a porphyrin complex, and at least one inorganic acid salt of a metal selected from a group consisting of alkali metals, alkaline earth metals, Al and Fe. The porphyrin complex is: wherein M is P, X is selected from a group consisting of a halogen and OH, and R2 is phenyl, and the water detection composition is supported by a silica gel.
Abstract: The present invention relates to phosphonate, nucleoside phosphonate or nucleoside phosphate compounds, compositions containing them, processes for obtaining them, and their use in treating a variety of medical disorders, in particular viral infections, cancers and the like.
Type:
Grant
Filed:
April 18, 2007
Date of Patent:
July 6, 2010
Assignees:
Chimerix, Inc., The Regents of the University of California
Inventors:
Karl Y. Hostetler, James R. Beadle, Jacqueline Ruiz, Merrick R. Almond, George R. Painter, Timothy A. Riley, Paula Francom
Abstract: A mutual prodrug of a MRA and a (?-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 ?L) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5?, produced by nebulization or by dry powder inhaler.
Type:
Application
Filed:
December 12, 2007
Publication date:
May 6, 2010
Inventors:
William Baker, Marcin Stasiak, Sundaramoorthi Swaminathan, Musong Kim
Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
Abstract: A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a ?-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another ?-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).
Type:
Application
Filed:
December 7, 2006
Publication date:
March 4, 2010
Inventors:
Eric Desarbre, Bérangère Gaucher, Malcolm G.P. Page, Patrick Roussel
Abstract: The present invention is based on the finding that activation of PPAR? plays a key role in inducing growth arrest and differentiation of certain actively proliferating cells. We show that administration of PPAR? agonists, such as thiazolidinedione ligands (TZDs), is effective both in vitro and in vivo at inhibiting the proliferation of such cells.
Type:
Grant
Filed:
December 19, 2002
Date of Patent:
December 22, 2009
Assignee:
Dana-Farber Cancer Institute
Inventors:
Bruce M. Spiegelman, Elisabetta Mueller, Pasha Sarraf, Soner Altiok, Peter Tontonoz, Samuel Singer
Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.
Type:
Grant
Filed:
December 28, 2006
Date of Patent:
December 1, 2009
Assignee:
Pharmacyclics, Inc.
Inventors:
Orion D. Jankowski, James T. Palmer, Lee Honigberg
Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.
Type:
Application
Filed:
May 22, 2008
Publication date:
November 26, 2009
Applicants:
Universidade De Coimbra, Centro De Neurociencias E Biologia Celular
Inventors:
Joao Nuno Sereno de Almeida Moreira, Vera Lucia Dantas Nunes Caldeira de Moura, Sergio Paulo de Magalhaes Simoes, Maria da Conceicao Monteiro Pedroso de Lima
Abstract: The invention is directed to methods and compositions for treating or preventing reactivation of a latent herpesvirus infection and the associated complications and outcomes. The methods involve administering a composition comprising glutamine, or a derivative, conjugate, or analog thereof.
Abstract: Novel molecular transporter compositions and their use for transporting bioactive substances into cells in living animals are disclosed. To afford in vivo delivery, the composition is covalently linked to the bioactive substance and the resultant composite structure is introduced into the subject. The transporter composition includes multiple guanidine moieties on a dendrimeric scaffold having a tri-functional core. The tri-functional core is a phosphorodiamidate or phosphoramide moiety.
Abstract: Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a UCP and/or Fas antibody or other inhibitor, or combination thereof, and a therapeutically acceptable amount of a fatty acid metabolism inhibitor and/or a therapeutically acceptable amount of a glucose metabolism inhibitor, optionally in combination with one or more chemotherpeutic agents. In preferred embodiments, the invention combines an antibody against UCP and/or Fas antigen with an oxirane carboxylic acid, represented by etomoxir, and/or with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.
Type:
Grant
Filed:
January 7, 2005
Date of Patent:
March 31, 2009
Assignee:
The Regents of the University of Colorado
Inventors:
Martha Karen Newell, Evan Newell, Elizabeth Villobos-Menvey
Abstract: Provided herein are compositions, combinations, and methods comprising NMDA antagonists including, but not limited to, NMDA glutamate receptor antagonists such as [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1-(7)-en-2-yl)alkyl]phosphonic acid and derivatives thereof, which are effective in reducing the amount of anesthetic required to maintain anesthesia (i.e. to achieve an anesthetic-sparing effect).
Type:
Application
Filed:
August 26, 2008
Publication date:
March 5, 2009
Applicant:
Wyeth
Inventors:
Cecil Mark Eppler, David Robert Hustead, Thomas Gerard Cullen, Raphael Johannes Zwijnenberg, William W. Muir, III
Abstract: The invention comprises a process wherein the DNA synthesis and, thus, the proliferation of mononuclear cells (MNZ) and of T cells as well is inhibited by the simultaneous and combined inhibition of the enzyme activity (I) of alanyl aminopeptidase and of dipeptidyl peptidase IV; (II) of dipeptidyl peptidase IV and of the angiotensin-converting enzyme; (III) of dipeptidyl peptidase IV and of prolyl oligopeptidase; and (IV) of dipeptidyl peptidase IV and of X-Pro-aminopeptidase to an extent which cannot be achieved by an application of a single one of said enzyme inhibitors, even at a higher dosage. Although the said inhibitors exercise an influence on the very same process finally, i.e. the DNA synthesis and, thus, the proliferation of immune cells, this effect is not complete and is not long lasting when a single inhibitor is applied.
Type:
Grant
Filed:
May 22, 2001
Date of Patent:
February 3, 2009
Assignee:
IMTM GmbH
Inventors:
Siegfried Ansorge, Marco Arndt, Frank Buehling, Uwe Lendeckel, Klaus Neubert, Dirk Reinhold, Stefan Brocke
Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.
Type:
Grant
Filed:
January 23, 2006
Date of Patent:
January 13, 2009
Assignee:
John Hopkins University School of Medicine
Inventors:
Philip A. Beachy, James K. Chen, Anssi Jussi Nikolai Taipale
Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
Type:
Grant
Filed:
January 18, 2005
Date of Patent:
December 2, 2008
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence de Garavilla, Bruce E. Maryanoff
Abstract: The invention provides methods of identifying and making compounds that inhibit the interaction between MUC1 and either p53 or TBP. Also embraced by the invention are in vivo and in vitro methods of inhibiting such an interaction and of inhibiting the expression of MUC1 by a cell.
Abstract: The present invention generally relates to systems and methods for treating inflammatory and proliferative diseases, and wounds, using a combination of (1) fatty acid metabolism inhibitors and (2) glycolytic inhibitors and/or UCP and/or Fas inhibitors or antibodies. More particularly, the invention combines an oxirane carboxylic acid compound, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and/or an antibody against UCP and/or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers (i.e., cancers resistant to conventional cancer drug therapies).
Type:
Grant
Filed:
April 28, 2005
Date of Patent:
November 4, 2008
Assignee:
The Regents of the University of Colorado
Inventors:
Martha Karen Newell, Elizabeth Villobos-Menuey, Evan Newell
Abstract: The invention is related to phosphorus substituted IMPDH inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
April 26, 2004
Date of Patent:
September 23, 2008
Assignee:
Gilead Sciences, Inc.
Inventors:
Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Thorsten Kirschberg, Hyung-Jung Pyun, William J. Watkins, Jennifer R. Zhang
Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.
Abstract: Phosphorus substituted mycophenolate oxime derivatives with anti-cancer, anti-viral, anti-inflammatory anti-tissue/organ transplant rejection properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit tumor growth, viral growth, inflammation, and tissue/organ transplant rejection and/or are useful therapeutically for the treatment or prevention of cancer, viral infection, inflammation and tissue/organ transplant rejection, as well as in assays for the detection of cancer, viral infection, inflammation and tissue/organ transplant rejection.
Abstract: The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Type:
Application
Filed:
September 20, 2007
Publication date:
July 10, 2008
Inventors:
Constantine G. Boojamra, Aesop Cho, William J. Watkins
Abstract: 4-Biarylyl-1-phenylazetidin-2-ones useful for the treatment of hypercholesterolemia are disclosed. The compounds are of the general formula in which represents an aryl or heteroaryl residue; Ar represents an aryl residue; U is a two to six atom chain; and the R's represent substituents.
Type:
Application
Filed:
December 11, 2007
Publication date:
July 10, 2008
Applicant:
MICROBIA, INC.
Inventors:
Eduardo J. Martinez, John J. Talley, Stephen Antonelli, Timothy C. Barden, Regina Lundrigan-Soucy, Wayne C. Schairer, Jing-Jing Yang, Daniel P. Zimmer, Brian Cali, Mark G. Currie, Peter S. Yorgey
Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.
Type:
Application
Filed:
May 2, 2006
Publication date:
May 15, 2008
Applicant:
ALLERGAN, INC.
Inventors:
David W. Old, Danny T. Dinh, Robert M. Burk
Abstract: There are disclosed a novel ?-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.
Abstract: The present invention relates to phosphinic acid derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of a disease related to the inhibition of ?-secretase, inter alia for the treatment of Alzheimer's disease.
Type:
Grant
Filed:
November 8, 2004
Date of Patent:
March 18, 2008
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Hans Hilpert, Roland Humm, Dietmar Knopp, Peter Weiss
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:
April 15, 2002
Date of Patent:
January 15, 2008
Assignee:
Karo Bio AB
Inventors:
Johan Malm, Peter Brandt, Karin Edvinsson, Thomas Ericsson, Sandra Gordon
Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Type:
Application
Filed:
May 23, 2007
Publication date:
November 29, 2007
Inventors:
Robert G. Gentles, Min Ding, Piyasena Hewawasam
Abstract: Disclosed are methods and compositions useful for treatment of neuropathic pain. In particular, the present invention provides methods of activating gamma-subtype peroxisome proliferator-activated receptors (PPAR?) to inhibit, relieve, or treat neuropathic pain.
Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an ? bonds, the solid triangle represents a ? bond, the wavy segments represent ? or ? bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.
Type:
Grant
Filed:
October 26, 2004
Date of Patent:
May 29, 2007
Assignee:
Allergan, Inc.
Inventors:
Robert M. Burk, Mark Holoboski, Mari F. Posner
Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.
Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treatment or prophylaxis of undesired thrombosis.
Type:
Grant
Filed:
December 6, 2004
Date of Patent:
April 3, 2007
Inventors:
Jin-An Jiao, Lawrence K. Luepschen, Esperanza Nieves, Hing C. Wong, Dean P. Taylor
Abstract: The invention relates to the use of treosulfan as a conditioning agent before allogenic transplantation of bone marrow or haematopoietic stem cells, whereby treosulfan is administered, either as single effective agent, or in combination with other chemotherapetic agents or immunosuppressant agents.
Type:
Grant
Filed:
November 3, 2000
Date of Patent:
April 3, 2007
Assignee:
Medac Gesellschaft fur Klinische Spezialpraparate mbH
Abstract: The invention provides a drug combination for the treatment of diseases associated with bone metastasis. The combination provides adenosine or a derivative thereof, a bisphosphonate, and a targeting agent(s) to decrease the signs or symptoms associated with such diseases.
Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceuticals compositions. Methods of treatment and combinations with other agents are also disclosed.
Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.
Type:
Grant
Filed:
October 13, 2000
Date of Patent:
August 29, 2006
Assignee:
Johns Hopkins University School of Medicine
Inventors:
Philip A. Beachy, James K. Chen, Anssi J. Taipale
Abstract: Methods and composisions for enhancing cellular function through protection of a tissue components such receptors, proteins, lipids, nucleic acids, carbohydrates, hormones, vitamins, and cofactors, by administering pyrophosphate analogs or related compounds.
Type:
Grant
Filed:
April 27, 2001
Date of Patent:
August 1, 2006
Assignee:
HealthPartners Research Foundation
Inventors:
William H. Frey, II, John Randall Fawcett
Abstract: Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substituted or unsubstituted alkanoyl, (iv) substituted or unsubstituted alkenoyl wherein the double bond is cis, and (v) (ortho or para) carbonyl-substituted aryl; and wherein the subtituent is each an independent group or linked together thereby forming a ring; and wherein X is one or more substituted or unsubstituted group containing one or more O, N, or S atom and wherein the substituent is each an independent group or linked together thereby forming a ring; and wherein the therapeutic agent is an alcohol-containing water-insoluble steroids or another alcohol containing compounds and methods to prepare such compounds.
Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.
Abstract: The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c).
Type:
Grant
Filed:
March 20, 2001
Date of Patent:
March 28, 2006
Assignee:
Applied Research Systems ARS Holding N.V.
Inventors:
Serge Halazy, Anna Quattropani, Agnes Bombrun, Mattias Schwarz, Russel Thomas, Anthony Baxter
Abstract: The present invention relates to novel water-soluble, stable derivatives of combretastatin A-4, and novel synthesis methods therefore. The combretastatin A-4 prodrugs described herein appear to be useful in the treatment of neoplastic disease.
Type:
Grant
Filed:
January 8, 1999
Date of Patent:
March 28, 2006
Assignee:
Arizona Broad of Regents acting for and on behalf of Arizona State University
Abstract: Hypocholesterolemic substituted 2-azetidinone compounds of the formula: are disclosed, as well as a methods of lowering cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a substituted 2-azetidinone cholesterol-lowering agent and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.
Type:
Grant
Filed:
June 11, 2002
Date of Patent:
January 3, 2006
Assignee:
Schering Corporation
Inventors:
Anima Ghosal, Shmuel Zbaida, Swapan K. Chowdhury, Robert M. Iannucci, Wenqing Feng, Kevin B. Alton, James E. Patrick, Harry R. Davis
Abstract: Compounds that demonstrate chelation affinity and selectivity for first transition series elements are administered to patients suffering from such conditions as ischemia, prolonged seizures and trauma to provide neuroprotection, cardioprotection, or both. These compounds when administered form complexes with chelatable iron and copper cations and thereby mitigate the ability of these cations to catalyze Haber-Weiss reactions that form toxic hydroxy free radicals that cause tissue injury. These compounds also form complexes with chelatable zinc cations thereby inhibiting the cytotoxicity associated with excess chelatable zinc.
Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.
Abstract: Compositions and uses associated with the MT103 family of compounds are disclosed. Particular structural features and properties of the compounds are described in detail. Uses include administering an MT103 family member to a patient for therapeutic purposes. Compositions include chemicals belonging to the MT103 family and pharmaceuticals that contain such chemicals. Methods of treating cells are also described.
Type:
Application
Filed:
April 30, 2004
Publication date:
December 30, 2004
Inventors:
Jorge Galvez, Javier Llompart, Kollol Pal
Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.
Type:
Application
Filed:
June 27, 2003
Publication date:
December 30, 2004
Inventors:
Roger D. Tung, Scott L. Harbeson, David D. Deininger, Mark A. Murcko, Govinda R. Bhisetti, Luc J. Farmer
Abstract: The present invention is related to compounds, their intermediates, processes for their preparation and use, and pharmaceutical compositions comprising the compounds. The novel compounds are useful in therapy, and in particular for the treatment of viral infection, particularly HIV infection.
Type:
Application
Filed:
February 6, 2004
Publication date:
December 9, 2004
Applicant:
Kemia, Inc.
Inventors:
Justin T. Ernst, Erik Boman, Susana C. Ceide, Antonio G. Montalban, Hiroshi Nakanishi, Edward Roberts, Eddine Saiah, Christopher Lum
Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treatment or prophylaxis of undesired thrombosis.
Type:
Grant
Filed:
September 24, 1999
Date of Patent:
December 7, 2004
Assignee:
Sunol Molecular Corporation
Inventors:
Jin-An Jiao, Lawrence K. Luepschen, Esperanza Nieves, Hing C. Wong, Dean P. Taylor
Abstract: The invention provides certain macrocyclic triaza compounds which down-regulate CD4 expression for use in the treatment of autoimmune diseases and inflammatory diseases or conditions. In a specific embodiment, the invention provides certain naphthalene substituted triaza macrocycles which exhibit high activity for down regulation of CD4 expression. In particular, triaza macrocycles having dansyl groups are provided for use in pharmaceutical compositions.
Type:
Application
Filed:
October 6, 2003
Publication date:
November 4, 2004
Inventors:
Thomas Bell, Dominique Schols, Kaka Dey, Kurt Vermeire