Serine Protease Inhibitor Affecting Or Utilizing Patents (Class 514/20.3)
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Publication number: 20120328517Abstract: This invention provides: novel protein homologous of a Kunitz domain, which are capable of binding kallikrein; polynucleotides that encode such novel proteins; and vectors and transformed host cells containing these polynucleotides.Type: ApplicationFiled: August 9, 2012Publication date: December 27, 2012Applicant: Dyax Corp.Inventors: William Markland, Robert C. Ladner
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Publication number: 20120309693Abstract: The present disclosure serves to reduce the healing time of tissue wounds, including those formed during surgery, whether necessary or elective (including cosmetic surgery), by providing a therapeutic dose of a pancreatic enzyme inhibitor.Type: ApplicationFiled: September 28, 2010Publication date: December 6, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Frank A. DeLano, Geert W. Schmid-Schonbein
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Patent number: 8318669Abstract: The present invention provides methods for modification and regulation of glucagon-like peptide 1 (GLP-1) metabolism by administering therapeutically effective amounts of an inhibitor of dipeptidylpeptidase IV (DPIV) or a pharmaceutically acceptable salt thereof, where the inhibitor has a Ki for inhibition of DPIV of 10 nM or less; and the inhibitor is administered in an amount sufficient to inhibit DPIV proteolysis of GLP-1 but not sufficient to suppress the immune system of the animal.Type: GrantFiled: November 9, 2010Date of Patent: November 27, 2012Assignees: Trustees of Tufts College, New England Medical Center Hospitals, Inc., 1149336 Ontario, Inc.Inventors: William W. Bachovchin, Andrew G. Plaut, Daniel J. Drucker
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Publication number: 20120282271Abstract: The invention provides methods and compositions for modulating hepsin activity and the MSP/Ron pathway, in particular by regulating pro-MSP activation by hepsin.Type: ApplicationFiled: October 21, 2010Publication date: November 8, 2012Applicant: Genentech, Inc.Inventors: Rajkumar Ganesan, Daniel Kirchhofer
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Publication number: 20120263759Abstract: A copolymer comprising a block of an elastin pentapeptide and method of making and using the copolymer are provided. The copolymer may be used as a coating on a stent. Methods of using a stent coated with the copolymer are also provided.Type: ApplicationFiled: September 2, 2011Publication date: October 18, 2012Applicant: Abbott Cardiovascular Systems Inc.Inventors: Syed F.A. Hossainy, Yiwen Tang, Lothar W. Kleiner
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Patent number: 8257699Abstract: The invention relates to the discovery of novel soluble neutral active Hyaluronidase Glycoproteins (sHASEGPs), methods of manufacture, and their use to facilitate administration of other molecules or to alleviate glycosaminoglycan associated pathologies. Minimally active polypeptide domains of the soluble, neutral active sHASEGP domains are described that include asparagine-linked sugar moieties required for a functional neutral active hyaluronidase domain. Included are modified amino-terminal leader peptides that enhance secretion of sHASEGP. The invention further comprises sialated and pegylated form of a recombinant sHASEGP to enhance stability and serum pharmacokinetics over naturally occurring slaughterhouse enzymes. Further described are suitable formulations of a substantially purified recombinant sHASEGP glycoprotein derived from a eukaryotic cell that generate the proper glycosylation required for its optimal activity.Type: GrantFiled: December 15, 2011Date of Patent: September 4, 2012Assignee: Halozyme, Inc.Inventors: Louis H. Bookbinder, Anirban Kundu, Gregory I. Frost
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Publication number: 20120171190Abstract: Methods for diagnosing chronic diarrhea and other gastrointestinal conditions. In the methods, a sample of gastrointestinal secretions is obtained from a control group; or a group who has been diagnosed with either healthy gastrointestinal tracts or with a gastrointestinal condition, like chronic diarrhea. The control group samples are analyzed in any suitable manner to determine the levels of gastrointestinal secretions, including one or more autophagy-related proteins, cytokeratins, digestive enzymes, or other proteins. The results of the sample analysis are used to create a database containing profiles of normal and abnormal gastrointestinal secretions. As the database is created and specific secretion level abnormalities are identified, patients may be diagnosed with these abnormalities and be treated by adjusting the levels of specific secretions.Type: ApplicationFiled: March 7, 2012Publication date: July 5, 2012Inventor: Thomas M. Donndelinger
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Publication number: 20120135931Abstract: The present invention relates to a method of modifying serine protease inhibitors in order to acquire or enhance any one of a variety of desired properties, including extent of inhibition, maintenance of inhibition following cleavage of the serine protease inhibitor by the target serine protease, speed of binding to the serine protease, neutralisation, and binding affinity. The present invention also relates to the products of such modifications and the uses of such products, in particular, their use in therapy.Type: ApplicationFiled: May 5, 2010Publication date: May 31, 2012Applicant: NATURAL ENVIRONMENT RESEARCH COUNCILInventors: R. Manjunatha Kini, Cho Yeow Koh, Kunchithapadam Swaminathan, Kumar Sundramurthy
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Publication number: 20120129765Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HCV in human patients or other animal hosts.Type: ApplicationFiled: October 28, 2011Publication date: May 24, 2012Applicants: GENOSCIENCE, RFS Pharma, LLCInventors: Jerome Courcambeck, Philippe Halfon, Mourad Bouzidi, Steven J. Coats, Richard Anthony Whitaker
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Publication number: 20120094931Abstract: Embodiments herein illustrate methods and compositions for treating inflammatory bowel disorders. In certain embodiments, compositions and methods relate to reducing, inhibiting or modulating progression of an inflammatory bowel disorder in a subject. Other embodiments herein relate to compounds including naturally occurring and synthetic mutant compositions of alpha-1 antitrypsin.Type: ApplicationFiled: June 28, 2011Publication date: April 19, 2012Inventors: Colm COLLINS, Jesus RIVERA-NIEVES, Charles A. DINARELLO
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Publication number: 20120083445Abstract: Disclosed herein, in certain embodiments, is an HC•HA complex comprising hyaluronan and a heavy chain of I?I, wherein the transfer of the heavy chain of I?I is catalyzed by TSG-6. Further disclosed herein, in certain embodiments, is an HC•HA complex comprising hyaluronan and a heavy chain of I?I, wherein the transfer of the heavy chain of I?I is catalyzed by the TSG-6 like protein.Type: ApplicationFiled: April 26, 2010Publication date: April 5, 2012Applicant: TissueTech, Inc.Inventors: Scheffer Tseng, Hua He
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Publication number: 20120082676Abstract: One aspect of the present invention provides a method of treating or preventing angioedema in a patient in need thereof comprising administering to the patient a therapeutically effective amount of an agent that is capable of inhibiting the interaction of HK with gC1q-R. One aspect of the present invention provides a method of treating or preventing vascular permeability in a patient in need thereof comprising administering to the patient a therapeutically effective amount of an agent that is capable of inhibiting the interaction of HK with gC1q-R.Type: ApplicationFiled: March 29, 2010Publication date: April 5, 2012Applicant: The Research Foundation of State University of New YorkInventor: Berhane Ghebrehiwet
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Patent number: 8148330Abstract: C1q is shown to be expressed in neurons, where it acts as a signal for synapse elimination. Methods are provided for protecting or treating an individual suffering from adverse effects of synapse loss. These findings have broad implications for a variety of clinical conditions, including Alzheimer's disease.Type: GrantFiled: December 8, 2006Date of Patent: April 3, 2012Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Ben A. Barres, Beth A. Stevens
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Publication number: 20120053113Abstract: The present invention provides compositions and pharmaceutical formulations of IaIp derived from plasma. Also provided are methods for the manufacture of the IaIp compositions and formulations, as well as method for the treatment of diseases associated with IaIp dysfunction.Type: ApplicationFiled: July 22, 2011Publication date: March 1, 2012Applicants: Baxter Healthcare S.A., Baxter International Inc.Inventors: Shawn F. Bairstow, Jennifer Hutsell, Sindhu Ramachandran
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Publication number: 20120045449Abstract: Embodiments of the present invention relate to compositions and methods for treatment of subjects in need of or having a bone marrow transplant. Certain embodiments describe compositions and methods for treatment of conditions associated with bone marrow transplantations in a subject, for example, Graft versus Host Disease (GvHD) or bone marrow transplantation rejection. Some embodiments concern early or immediate bone marrow transplantation rejection. Certain embodiments relate to compositions and uses of alpha1-antitrypsin (?1-antitrypsin, AAT) and carboxyterminal peptide derivatives thereof and/or compositions and uses of serine protease inhibitors, immunomodulators or anti-inflammatory agent activity similar to that of AAT.Type: ApplicationFiled: August 12, 2011Publication date: February 23, 2012Inventors: Charles A. Dinarello, Eli C. Lewis
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Patent number: 8119602Abstract: Methods of treating, preventing or ameliorating one or more symptoms of hepatitis C in a subject comprising the step of administering at least one HCV protease inhibitor in combination with food are provided. Also provided are methods of increasing bioavailability of an HCV protease inhibitor and methods of increasing serum levels of an HCV protease inhibitor in a subject. All methods comprise adminstering at least one HCV protease inhibitor in combination with food, the at least one HCV protease inhibitor selected from the group consisting of compounds of Formulae I-XXVI, described herein. Administration of compounds of the present invention in combination with food provides improved bioavailability and increased peak serum levels of the compounds as compared to administration without food.Type: GrantFiled: May 31, 2006Date of Patent: February 21, 2012Assignee: Schering CorporationInventors: Jenny Zhang, Samir K. Gupta
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Patent number: 8106002Abstract: The present invention provides anti-cancer agents comprising protein C inhibitor (PCI) or derivatives thereof as an active ingredient. The anti-cancer agents of the present invention have activities of suppressing cancer cell growth, and cancer metastasis, infiltration, and angiogenesis. Further, the present invention has shown that derivatives containing a heparin-binding domain of PCI inhibit the growth, metastasis and angiogenesis of cancer cells. Therefore, according to the present invention, PCI or derivatives thereof are useful for inhibiting the growth, metastasis and angiogenesis of cancer.Type: GrantFiled: April 18, 2006Date of Patent: January 31, 2012Assignees: Chugai Seiyaku Kabushiki Kaisha, Mie UniversityInventor: Koji Suzuki
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Patent number: 8088738Abstract: The present invention relates to a thermostable alpha-1-antitrypsin mutein with a disulfide bond and a preparation method of the same, more precisely an alpha-1-antitrypsin mutein with improved thermostability, compared with the conventional thermostable alpha-1-antitrypsin mutein (Korean Patent No. 133252), resulted from the process of substituting the 168th and 189th amino acids of the alpha-1-antitrypsin with cysteines which are then linked by a disulfide bond, with keeping its alpha-1-antitrypsin activity unchanged, and a preparing method of the same. The thermostable alpha-1-antitrypsin mutein with a disulfide bond of the invention can be effectively used for a protein based therapeutic agent which is very stable in vivo, and can be applied further in various fields including in the development of a diagnostic reagent and in the preparation of an affinity column.Type: GrantFiled: November 22, 2007Date of Patent: January 3, 2012Assignee: Korea Institute of Science and TechnologyInventors: Myeong-Hee Yu, Je-Hyun Baek, Cheolju Lee
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Publication number: 20110312873Abstract: The invention refers to multibasic, N-terminally modified tetrapeptide mimetics with a C-terminal P1-arginine mimetic, methods for their production and use for therapy and prophylaxis of diseases, caused by bacterial pathogens or viruses, as well as for therapy and prophylaxis of diabetes, arteriosclerosis, cancer, Alzheimer's or the onset of obesity, as well as the use of these compounds as inhibitors of the proprotein convertases which cleave behind basic P1 residues, especially for inhibition of the protease furin.Type: ApplicationFiled: October 29, 2009Publication date: December 22, 2011Applicant: PHILIPPS-UNIVERSITAT MARBURGInventors: Torsten Steinmetzer, Gero Becker, Wolfgang Garten
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Patent number: 8071551Abstract: The instant invention provides a method of treating an animal suffering a disease characterized by excessive apoptosis by administering a therapeutically effective amount of at least one serine protease inhibitor and thereafter monitoring a decrease in apoptosis. The inhibitor of the invention includes ?1-antitrypsin or an ?1-antitrypsin-like agent, including, but not limited to oxidation-resistant variants of ?1-antitrypsin, and peptoids with antitrypsin activity. The diseases treatable by the invention include cancer, autoimmune disease, sepsis neurodegenerative disease, myocardial infarction, stroke, ischemia-reperfusion injury, toxin induced liver injury and AIDS. The method of the invention is also suitable for the prevention or amelioration of diseases characterized by excessive apoptosis.Type: GrantFiled: March 19, 2008Date of Patent: December 6, 2011Assignee: BioHolding, Inc.Inventor: Leland Shapiro
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Publication number: 20110262396Abstract: Provided are methods and compositions for using protease binding proteins in combination with other therapeutic agents to treat inflammatory disorders such as rheumatoid arthritis, psoriasis, multiple sclerosis, systemic sclerosis, asthma, chronic obstructive pulmonary disease, inflammatory bowel disease (e.g., Crohn's and ulcerative colitis). The use of the protease binding protein allows a lower dose of the other therapeutic agents to be used in the methods and compositions, such that side effects of the other therapeutic agents are reduced or removed.Type: ApplicationFiled: October 22, 2009Publication date: October 27, 2011Applicant: DYAX CORP.Inventor: Clive R. Wood
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Publication number: 20110251136Abstract: The present invention relates to methods and compositions for sealing localized regions of damaged lung tissue to reduce overall lung volume. The glue compositions provide a glue featuring an adhering moiety coupled to one or more other moieties including, for example, a cross-linkable moiety and/or one other adhering moiety. The methods and compositions of the invention find use, for example, in treating pulmonary conditions, such as emphysema.Type: ApplicationFiled: April 19, 2011Publication date: October 13, 2011Applicant: PneumRx, Inc.Inventors: Glen Gong, Ronald Dieck
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Patent number: 8008263Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: October 10, 2008Date of Patent: August 30, 2011Assignee: Novartis AGInventors: Shawn D. Britt, Lech Andrzej Ciszewski, Jiping Fu, Subramanian Karur, Yugang Liu, Peichao Lu, David Thomas Parker, Mahavir Prashad, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng
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Publication number: 20110200555Abstract: Conjugates of hydroxyalkyl starch and a protein are provided herein. The conjugates are formed by a convalent linkage between the hydroxyalkyl starch or a derivative of the hydroxyalkyl starch and the protein. Methods of producing the conjugates and the use of the conjugates also are provided herein.Type: ApplicationFiled: February 1, 2011Publication date: August 18, 2011Applicant: FRESENIUS KABI DEUTSCHLAND GMBHInventors: Wolfram Eichner, Martin Schimmel, Frank Hacket, Elmar Kraus, Norbert Zander, Ronald Frank, Harald Conradt, Klaus Langer, Michele Orlando, Klaus Sommermeyer
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Publication number: 20110172163Abstract: The invention relates to KLK protease inhibitors. In particular, the invention is directed to KLK4 protease inhibitors and their uses in the treatment of a cancer, such as prostate cancer.Type: ApplicationFiled: August 11, 2009Publication date: July 14, 2011Applicant: QUEENSLAND UNIVERSITY OF TECHNOLOGYInventors: Jonathan M. Harris, Joakim E. Swedberg
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Publication number: 20110171175Abstract: This invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof wherein C* represents a diastereomeric carbon comprising a mixture of R and S isomers wherein the R isomer is greater than 50% of the mixture.Type: ApplicationFiled: March 18, 2011Publication date: July 14, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Steven Lyons, Robert B. Perni
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Publication number: 20110083201Abstract: The present invention is related to the discovery that serpina3n, a secreted protein, binds to and inhibits granzyme B activity. The invention thus provides cells that include a polynucleotide encoding a granzyme B inhibitory serpin, pharmaceutical compositions including a granzyme B inhibitory serpin or a polynucleotide encoding a granzyme B inhibitory serpin, methods for treating a patient in need of immunosuppression by administration of a granzyme B inhibitory serpin, and methods of transplanting cells (e.g., islet cells) expressing a granzyme B inhibitory serpin.Type: ApplicationFiled: September 7, 2010Publication date: April 7, 2011Inventors: Ray V. Rajotte, R. Chris Bleackley, Greg Korbutt, Sarah J. Lord, Simonetta Sipione, Katia Carmine-Simmen, Fabrizio Giuliani
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Publication number: 20110038917Abstract: The present invention relates to therapeutic compositions and methods of treatment that contain or employ at least two of: an oligomeric proanthocyanidin; a protease inhibitor; and/or a lactoferrin. The compositions of this invention may be in various forms depending upon the disease or condition to be treated. The compositions and methods of this invention are useful to treat a patient suffering from or susceptible to gram negative bacterial infections, including those associated with cystic fibrosis, ear infections and with wounds.Type: ApplicationFiled: May 7, 2008Publication date: February 17, 2011Inventors: Jeff Kappers, Mark Glenn Hearn, Robert Qui
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Publication number: 20100331261Abstract: The present invention relates to the use of alpha-1-antitrypsin for the preparation of effective drugs for the treatment of chronic fatigue syndrome. In addition, the present invention relates to the use of plasma or other therapeutic forms with an alpha-1-antitrypsin content sufficient to obtain a dose of 6 mg or more of alpha-1-antitrypsin per kg of body weight at a frequency of between 1 and 31 days.Type: ApplicationFiled: June 24, 2010Publication date: December 30, 2010Applicant: GRIFOLS, S.A.Inventors: Ana Garcia Quintana, José Alegre Martin
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Publication number: 20100330109Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: ApplicationFiled: December 16, 2009Publication date: December 30, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Kevin M. Cottrell, John J. Court, David D. Deininger, Luc J. Farmer, Janos Pitlik, Robert B. Perni
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Publication number: 20100333236Abstract: The present invention relates to a method to limit insect and/or mite damage in plants, by the use of mutant plant proteinase inhibitors. More specifically, it relates to the use of mutant serpins of which the reactive center loop has been replaced by an artificial sequence. Preferably, the mutant serpins use an Arabidopsis thaliana serpin-1 backbone, or a homologue thereof. The mutant serpins have a specificity other than the wild-type serpins, and by modulating the reactive loop center, specific inhibitors against specific insect and/or mite proteases can be developed. Those mutant serpins can be used to inhibit or limit insect and/or mite damage, such as the damage caused by insect feeding.Type: ApplicationFiled: October 30, 2008Publication date: December 30, 2010Inventors: Frank Van Breusegem, Dominique Vercammen, Guy Smagghe, Fernando Alvarez
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Publication number: 20100303901Abstract: Enteric coated capsules or tablets for oral delivery of a protein, polypeptide or peptide drug, in particular for oral delivery of insulin, are provided, comprising microparticles of the protein, polypeptide or peptide drug, microparticles of a protease inhibitor and, optionally, microparticles of an absorption enhancer. The protease inhibitor and the absorption enhancer may be together in the same microparticles. The microparticles of each component are embedded in an enteric polymer matrix.Type: ApplicationFiled: April 27, 2008Publication date: December 2, 2010Inventors: Eyal Shimoni, Ory Ramon, Isaiah J. Kopelman, Shimon Mizrahi, Nir Salzmann, Yaakov Nahmias, Aharon Oren
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Publication number: 20100279923Abstract: The subject of the present invention is, in the most general aspect, the therapeutic application of the Kazal-type serine protease inhibitor Infestin or domains thereof or modified Kazal-type serine protease inhibitors based on Infestin homologs, which prevent the formation and/or stabilization of three-dimensional arterial or venous thrombi by interfering with proteins involved in activation of the so-called intrinsic coagulation pathway. In particular the present invention relates to the use of said Kazal-type serine protease inhibitors or fragments thereof or modified Kazal-type serine protease inhibitors, in the treatment or prophylaxis of a condition or disorder related to arterial thrombus formation, i. e.Type: ApplicationFiled: February 11, 2008Publication date: November 4, 2010Inventors: Stefan Schulte, Ulrich Kronthaler, Stefan Schmidbauer, Thomas Weimer, Kay Hofmann