81 |
PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITORS AND METHODS OF USE THEREOF TO MODULATE LIPID METABOLISM |
US14817690 |
2015-08-04 |
US20160009748A1 |
2016-01-14 |
Daniel A. Lawrence; Cory Emal; Jacqueline Cale; Enming Joe Su; Mark Warnock; Shih-Hon Li; Jeanne Ann Cupp |
The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels. |
82 |
Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism |
US12624126 |
2009-11-23 |
US09120744B2 |
2015-09-01 |
Daniel A. Lawrence; Cory Emal; Jacqueline Cale; Enming J. Su; Mark Warnock; Shih-Hon Li; Jeanne A. Cupp |
The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels. |
83 |
MIRAC PROTEINS |
US14464059 |
2014-08-20 |
US20140356344A1 |
2014-12-04 |
Jay M. Short; Hwai Wen Chang; Gerhard Frey |
This disclosure relates to a method of generating conditionally active biologic proteins from wild type proteins, in particular therapeutic proteins, which are reversibly or irreversibly inactivated at the wild type normal physiological conditions. For example, evolved proteins are virtually inactive at body temperature, but are active at lower temperatures. |
84 |
Polynucleotides encoding therapeutic inhibitors of PAI-1 |
US13769144 |
2013-02-15 |
US08828686B2 |
2014-09-09 |
Thomas D. Reed; Richard E. Peterson; Charles E. Reed; Joan Mazzarelli Sopczynski; Bethany L. Merenick; Jonathan Carson; Catherine L. Keaty; Elena Tasheva |
The invention relates to mammalian PAI-I ligands and modulators. In particular, the invention relates to polypeptides, polypeptide compositions and polynucleotides that encode polypeptides that are ligands and/or modulators of PAI-I. The invention also relates to polyligands that are homopolyligands or heteropolyligands that modulate PAI-I activity. The invention also relates to ligands and polyligands localized to a region of a cell. The invention also relates to localization tethers and promoter sequences that can be used to provide spatial control of the PAI-I ligands and polyligands. The invention also relates to inducible gene switches that can be used to provide temporal control of the PAI-I ligands and polyligands. The invention also relates to methods of treating or preventing atherosclerosis. The invention also relates to methods of treating or preventing fibrosis. |
85 |
Protease screening methods and proteases identified thereby |
US13507480 |
2012-07-02 |
US08663633B2 |
2014-03-04 |
Edwin L. Madison |
Methods for identifying modified proteases with modified substrate specificity or other properties are provided. The methods screen candidate and modified proteases by contacting them with a substrate, such as a serpin, an alpha macroglobulins or a p35 family protein or modified serpins and modified p35 family members or modified alpha macroglobulins, that, upon cleavage of the substrate, traps the protease by forming a stable complex. Also provided are modified proteases. |
86 |
Therapeutic Inhibitors of PAI-1 Function Methods of Their Use |
US13769144 |
2013-02-15 |
US20130267022A1 |
2013-10-10 |
Thomas D. Reed; Richard E. Peterson; Charles E. Reed; Joan Mazzarelli Sopczynski; Bethany L. Merenick; Jonathan Carson; Catherine L. Bair; Elena Tasheva |
The invention relates to mammalian PAI-I ligands and modulators. In particular, the invention relates to polypeptides, polypeptide compositions and polynucleotides that encode polypeptides that are ligands and/or modulators of PAI-I. The invention also relates to polyligands that are homopolyligands or heteropolyligands that modulate PAI-I activity. The invention also relates to ligands and polyligands localized to a region of a cell. The invention also relates to localization tethers and promoter sequences that can be used to provide spatial control of the PAI-I ligands and polyligands. The invention also relates to inducible gene switches that can be used to provide temporal control of the PAI-I ligands and polyligands. The invention also relates to methods of treating or preventing atherosclerosis. The invention also relates to methods of treating or preventing fibrosis. |
87 |
Use of matrix metalloproteinase-10 (MMP-10) for thrombolytic treatments |
US12861357 |
2010-08-23 |
US08541370B2 |
2013-09-24 |
Josune Orbe Lopategui; Jose Antonio Rodriguez Garcia; Jose Antonio Paramo Fernandez; Rosario Serrano Vargas |
The present invention relates to the use of matrix metalloproteinase MMP-10 in the preparation of a pharmaceutical composition useful for thrombolytic therapy, it also being possible for said composition to contain a plasminogen activator. Additionally, the present invention relates to said pharmaceutical composition for the treatment of thrombotic disorders. |
88 |
PROTEASE SCREENING METHODS AND PROTEASES IDENTIFIED THEREBY |
US13506845 |
2012-05-18 |
US20130164820A9 |
2013-06-27 |
Edwin L. Madison |
Methods for identifying modified proteases with modified substrate specificity or other properties are provided. The methods screen candidate and modified proteases by contacting them with a substrate, such as a serpin, an alpha macroglobulins or a p35 family protein or modified serpins and modified p35 family members or modified alpha macroglobulins, that, upon cleavage of the substrate, traps the protease by forming a stable complex. Also provided are modified proteases. |
89 |
Polynucleotides encoding therapeutic inhibitors of PAI-1 |
US12812127 |
2009-01-09 |
US08431363B2 |
2013-04-30 |
Thomas D. Reed; Richard E. Peterson; Charles C. Reed; Joan Mazzarelli Sopczynski; Bethany L. Merenick; Jonathan Carson; Catherine L. Bair; Elena Tasheva |
The invention relates to mammalian PAI-I ligands and modulators. In particular, the invention relates to polypeptides, polypeptide compositions and polynucleotides that encode polypeptides that are ligands and/or modulators of PAI-I. The invention also relates to polyligands that are homopolyligands or heteropolyligands that modulate PAI-I activity. The invention also relates to ligands and polyligands localized to a region of a cell. The invention also relates to localization tethers and promoter sequences that can be used to provide spatial control of the PAI-I ligands and polyligands. The invention also relates to inducible gene switches that can be used to provide temporal control of the PAI-I ligands and polyligands. The invention also relates to methods of treating or preventing atherosclerosis. The invention also relates to methods of treating or preventing fibrosis. |
90 |
PROTEASE SCREENING METHODS AND PROTEASES IDENTIFIED THEREBY |
US13506845 |
2012-05-18 |
US20120301945A1 |
2012-11-29 |
Edwin L. Madison |
Methods for identifying modified proteases with modified substrate specificity or other properties are provided. The methods screen candidate and modified proteases by contacting them with a substrate, such as a serpin, an alpha macroglobulins or a p35 family protein or modified serpins and modified p35 family members or modified alpha macroglobulins, that, upon cleavage of the substrate, traps the protease by forming a stable complex. Also provided are modified proteases. |
91 |
Protease screening methods and proteases identified thereby |
US11825627 |
2007-07-05 |
US08211428B2 |
2012-07-03 |
Edwin L. Madison |
Methods for identifying modified proteases with modified substrate specificity or other properties are provided. The methods screen candidate and modified proteases by contacting them with a substrate, such as a serpin, an alpha macroglobulins or a p35 family protein or modified serpins and modified p35 family members or modified alpha macroglobulins, that, upon cleavage of the substrate, traps the protease by forming a stable complex. Also provided are modified proteases. |
92 |
Molecular Determinants Associated With Prostate Cancer And Methods Of Use Thereof |
US13011416 |
2011-01-21 |
US20110206689A1 |
2011-08-25 |
William C. Hahn; Atish Choudury; Isil Guney |
The present invention provides methods of treating cancer by inhibiting pserine threonine kinase activity and detecting cancer using biomarkers. |
93 |
C1-Inhibitor Prevents Non-Specific Plasminogen Activation by a Prourokinase Mutant without Impeding Fibrin-Specific Fibrinolysis |
US12947573 |
2010-11-16 |
US20110081334A1 |
2011-04-07 |
Victor Gurewich; Ralph Pannell |
A mutant prourokinase plasminogen activator (M5) was developed to make prouPA less subject to spontaneous activation during fibrinolysis. C1-inhibitor complexes with tcM5. The effect of C1-inhibitor on fibrinolysis and fibrinogenolysis by M5 was determined. Supplemental C1-inhibitor restores the stability of M5 but not that of prouPA. Clot lysis by M5 with supplemental C1-inhibitor showed no attenuation of the rate of fibrinolysis, whereas fibrinogenolysis was prevented by C1-inhibitor. Due to higher dose tolerance of M5 with C1-inhibitor, the rate of fibrin-specific lysis reached that achievable by nonspecific fibrinolysis without inhibitor. Plasma C1-inhibitor stabilized M5 in plasma by inhibiting tcM5 and thereby non-specific plasminogen activation. At the same time, fibrin-specific plasminogen activation remained unimpaired. This unusual dissociation of effects has significant implications for improving the safety and efficacy of fibrinolysis. Methods of reducing bleeding and non-specific plasminogen activation during fibrinolysis by administering M5 along with exogenous C1-inhibitor are disclosed. |
94 |
Anti-invasive and anti-angiogenic compositions |
US11600302 |
2006-11-15 |
US07807621B2 |
2010-10-05 |
Andrew P. Mazar; Terence R. Jones |
A peptide compound having the sequence Lys-Pro-Ser-Ser-Pro-Pro-Glu-Glu [SEQ ID NO:2] or a substitution variant, addition variant or other chemical derivative thereof inhibits cell invasion, endothelial tube formation or angiogenesis in vitro. A number of substitution variants and addition variants of this peptide, preferably capped at the N- and C-termini, as well as peptidomimetic derivatives, are useful for treating diseases and conditions mediated by undesired and uncontrolled cell invasion and/or angiogenesis. Pharmaceutical compositions comprising the above peptides and derivatives are administered to subjects in need of such treatment in a dosage sufficient to inhibit invasion and/or angiogenesis. The disclosed compositions and methods are particularly useful for suppressing the growth and metastasis of tumors. |
95 |
Plasminogen Activator Inhibitor-1 Inhibitors and Methods of Use Thereof to Modulate Lipid Metabolism |
US12624126 |
2009-11-23 |
US20100137194A1 |
2010-06-03 |
Daniel A. Lawrence; Cory Emal; Jacqueline Cale; Enming J. Su; Mark Warnock; Shih-Hon Li; Jeanne A. Cupp |
The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels. |
96 |
Anti-invasive and anti-angiogenic compositions |
US11600302 |
2006-11-15 |
US20090143303A1 |
2009-06-04 |
Andrew P. Mazar; Terence R. Jones |
A peptide compound having the sequence Lys-Pro-Ser-Ser-Pro-Pro-Glu-Glu [SEQ ID NO:2] or a substitution variant, addition variant or other chemical derivative thereof inhibits cell invasion, endothelial tube formation or angiogenesis in vitro. A number of substitution variants and addition variants of this peptide, preferably capped at the N- and C-termini, as well as peptidomimetic derivatives, are useful for treating diseases and conditions mediated by undesired and uncontrolled cell invasion and/or angiogenesis. Pharmaceutical compositions comprising the above peptides and derivatives are administered to subjects in need of such treatment in a dosage sufficient to inhibit invasion and/or angiogenesis. The disclosed compositions and methods are particularly useful for suppressing the growth and metastasis of tumors. |
97 |
Methods, Devices, And Compositions For Lysis Of Occlusive Blood Clots While Sparing Wound Sealing Clots |
US12187807 |
2008-08-07 |
US20090136557A1 |
2009-05-28 |
Victor Gurewich; Jian-Ning Liu; Paolo Sarmientos |
It has now been discovered that certain mutant forms of pro-urokinase (“pro-UK”), such as so-called pro-UK mutant “M5” (Lys.sup.300.fwdarw.His)-, perform in the manner of pro-UK in lysing “bad” blood clots (those clots that occlude blood vessels), while sparing hemostatic fibrin in the so-called “good” blood clots (those clots that seal wounds, e.g., after surgery or other tissue injury). Thus, these pro-UK mutants are excellent and safe thrombolytic agents. These advantages allow them to be used in a variety of new methods, devices, and compositions useful for thrombolysis and treating various cardiovascular disorders in clinical situations where administration of other known thrombolytic agents has been too risky or even contraindicated. |
98 |
TARGETING VECTOR TO THE UROKINASE PLASMINOGEN ACTIVATOR RECEPTOR |
US11468348 |
2006-08-30 |
US20080318320A1 |
2008-12-25 |
Michael J. Welsh; Paola T. Drapkin |
The present invention relates to the targeted delivery of a delivery vehicle construct which specifically binds to and stimulates endocytosis into cells expressing the urokinase plasminogen activator receptor (uPAR), and particularly human airway epithelia. The delivery vehicle construct comprises a portion of uPA and a cargo linked thereto and is useful for the targeted delivery of the cargo to a cell. In one aspect of the invention, the uPA portion of the delivery vehicle construct comprises the wild-type uPA, a fragment of uPA which has the PAI-1 binding region deleted, or a uPA peptide comprising amino acids 13-19 and is useful for the targeted delivery of the cargo to cells, and in particular to airway epithelia. The present invention also provides a method for delivering the delivery vehicle construct to a cell. The method comprises the steps of (a) contacting a target cell with a delivery vehicle construct comprising a uPA portion and a cargo portion; and (b) obtaining a desired result in the target cell. |
99 |
Integrated Infusion Container |
US11994186 |
2006-06-28 |
US20080269712A1 |
2008-10-30 |
Gi-Bum OH |
The present invention relates to unitary bottle for injection, more particularly, to a unitary medicine bottle having an integral structure where a medicine container is easily connected with a plastic container including a solution at a completely sterilized state so that powdered, freeze-dried or liquid medicine is mixed with the solution with one touch for a short time. The unitary medicine bottle for injection according to the present invention comprises: a plastic container equipped with a coupling member connected with a medicine container at one end and a releasing member for releasing a liquid medicine to be at the other end; a protection cap integrally formed with the coupling member to accept the medicine container; and a flue needle which moves forward in a direction of the medicine container and perforates a stopper of the medicine container and is inserted in the coupling member connecting the plastic container with the medicine container. |
100 |
Pharmaceutical compositions of glycoconjugates |
US10492261 |
2002-10-09 |
US07416858B2 |
2008-08-26 |
Shawn DeFrees; David A. Zopf; Robert J. Bayer; Caryn Bowe; David James Hakes; Xi Chen |
The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group of peptide. |