Patents by Inventor Kerstin Moehle
Kerstin Moehle has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 9518092Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.Type: GrantFiled: September 24, 2014Date of Patent: December 13, 2016Assignees: POLYPHOR LTD., UNIVERSITAT ZURICHInventors: Jürg Zumbrunn, Steven J. Demarco, Sergio Lociuro, Jan Wim Vrijbloed, Frank Gombert, Reshmi Mukherjee, Kerstin Moehle, Daniel Obrecht, John Anthony Robinson, Heiko Henze, Barbara Romagnoli, Christian Ludin
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Patent number: 9512139Abstract: Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the ?-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.Type: GrantFiled: August 3, 2010Date of Patent: December 6, 2016Assignee: POLYPHOR AGInventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Franck Lach, Anatol Luther, Karsten Marx, Kerstin Möhle
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Publication number: 20160333051Abstract: Template-fixed ?-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: June 1, 2016Publication date: November 17, 2016Inventors: Steven J. Demarco, Kerstin Moehle, Heiko Henze, Odile Sellier, Francoise Jung, Frank Gombert, Daniel Obrecht, Christian Ludin
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Publication number: 20150087577Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: September 24, 2014Publication date: March 26, 2015Applicants: Universität Zürich, POLYPHOR LTD.Inventors: Jürg Zumbrunn, Steven J. Demarco, Sergio Lociuro, Jan Wim Vrijbloed, Frank Gombert, Reshmi Mukherjee, Kerstin Moehle, Daniel Obrecht, John Anthony Robinson, Heiko Henze, Barbara Romagnoli, Christian Ludin
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Publication number: 20150080317Abstract: The template-fixed B-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activityType: ApplicationFiled: November 28, 2014Publication date: March 19, 2015Applicants: Universitaet Zuerich, POLYPHOR LTD.Inventors: Daniel OBRECHT, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
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Patent number: 8921325Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where Cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or, in particular, for stem cell mobilization of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.Type: GrantFiled: February 11, 2013Date of Patent: December 30, 2014Assignees: Polyphor Ltd., Universität ZürichInventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
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Patent number: 8895695Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.Type: GrantFiled: July 1, 2010Date of Patent: November 25, 2014Assignees: Polyphor Ltd., Universität ZürichInventors: Jürg Zumbrunn, Steven J. Demarco, Sergio Lociuro, Jan Wim Vrijbloed, Frank Gombert, Reshmi Mukherjee, Kerstin Moehle, Daniel Obrecht, John Anthony Robinson, Heiko Henze, Barbara Romagnoli, Christian Ludin
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Publication number: 20140213531Abstract: Template-fixed ?-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: December 9, 2013Publication date: July 31, 2014Applicants: Universitat Zurich, Polyphor Ltd.Inventors: Steven J. Demarco, Kerstin Moehle, Heiko Henze, Odile Sellier, Francoise Jung, Frank Gombert, Daniel Obrecht, Christian Ludin
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Patent number: 8658604Abstract: Template-fixed ?-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.Type: GrantFiled: February 17, 2005Date of Patent: February 25, 2014Assignees: Polyphor Ltd, Universitat ZurichInventors: Steven J. DeMarco, Kerstin Moehle, Heiko Henze, Odile Sellier, Françoise Jung, Frank Gombert, Daniel Obrecht, Christian Ludin
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Publication number: 20130150299Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where Cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or, in particular, for stem cell mobilisation of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.Type: ApplicationFiled: February 11, 2013Publication date: June 13, 2013Inventors: Daniel OBRECHT, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
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Patent number: 8450284Abstract: The invention relates to lipopeptide building blocks consisting of a peptide chain comprising a coiled-coil domain, linked covalently to a lipid moiety comprising long alkyl or alkenyl chains, and optionally linked to an antigen; and to helical lipopeptide bundles and synthetic virus-like particles formed by aggregation. The nanometer size and shape of these bundles and particles, their stability under aqueous physiological conditions, their chemical composition, the possibility to incorporate B- and T-cell epitopes, and their production by chemical synthesis, make them highly suitable as vaccine delivery vehicles.Type: GrantFiled: December 6, 2007Date of Patent: May 28, 2013Assignee: Universitaet ZuerichInventors: Francesca Boato, Anabelle Freund, Arin Ghasparian, Kerstin Möhle, John A. Robinson, Richard M. Thomas
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Patent number: 8399611Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or for treating inflammation, or, in particular, for stem cell mobilization of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor.Type: GrantFiled: February 28, 2007Date of Patent: March 19, 2013Assignees: Polyphor Ltd., Universitaet ZuerichInventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
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Publication number: 20120270881Abstract: Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the ?-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.Type: ApplicationFiled: August 3, 2010Publication date: October 25, 2012Applicant: POLYPHOR AGInventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Franck Lach, Anatol Luther, Karsten Marx, Kerstin Möhle
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Publication number: 20120202821Abstract: Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.Type: ApplicationFiled: August 5, 2009Publication date: August 9, 2012Applicant: POLYPHOR AGInventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Franck Lach, Anatol Luther, Karsten Marx, Kerstin Möhle
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Publication number: 20110245155Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collections of peripheral blood stem cells. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: July 1, 2010Publication date: October 6, 2011Applicants: Polyphor Ltd., Universität ZürichInventors: Jürg Zumbrunn, Steven J. Demarco, Sergio Lociuro, Jan Wim Vrijbloed, Frank Gombert, Reshmi Mukherjee, Kerstin Moehle, Daniel Obrecht, John Anthony Robinson, Heiko Henze, Barbara Romagnoli, Christian Ludin
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Publication number: 20110230426Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 8 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly or Pro or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have agonizing or antagonizing activity against urotensin II or show inhibition of the STAT6/NCoA-1 interaction and can be used for preventing or treating diseases or disorders related to urotensin II, STAT6 and NCoA-1. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: August 8, 2008Publication date: September 22, 2011Applicants: POLYPHOR AG, UNIVERSITAT ZURICHInventors: Daniel Obrecht, Frank Gombert, Markus Seitz, Ludovic T. Maillard, Roba Mounme, Kerstin Moehle, John Anthony Robinson, Odile Sellier-Kessler, Heiko Henze, Christian Bisang, Alexander Lederer
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Patent number: 7838496Abstract: Template-fixed ?-hairpin peptidomimetics of the General Formula (I); wherein Z1 and Z2 are template-fixed chains of 4 and 6 or 5 and 7 ?-amino acid residues and salts thereof. They have CXCR4-antagonizing properties and can be used as medicaments. These ?-sheet peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.Type: GrantFiled: May 2, 2003Date of Patent: November 23, 2010Assignees: Polyphor AG/Ltd., Universität ZürichInventors: Jürg Zumbrunn, Steven J. Demarco, Sergio Lociuro, Jan Wim Vrijbloed, Frank Gombert, Reshmi Mukherjee, Kerstin Moehle, Daniel Obrecht, Barbara Romagnoli, John Anthony Robinson
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Patent number: 7786078Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid—and solution phase synthetic strategy.Type: GrantFiled: April 29, 2004Date of Patent: August 31, 2010Assignees: Polyphor Ltd., Universität ZürichInventors: Jürg Zumbrunn, Steven J. Demarco, Sergio Lociuro, Jan Wim Vrijbloed, Frank Gombert, Reshmi Mukherjee, Kerstin Moehle, Daniel Obrecht, John Anthony Robinson, Heiko Henze, Barbara Romagnoli, Christian Ludin
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Publication number: 20100048463Abstract: The template-fixed B-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where Cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or, in particular, for stem cell mobilisation of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.Type: ApplicationFiled: February 28, 2007Publication date: February 25, 2010Applicants: POLYPHOR Ltd., Universitaet ZuerichInventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
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Publication number: 20100015173Abstract: The invention relates to lipopeptide building blocks consisting of a peptide chain comprising a coiled-coil domain, linked covalently to a lipid moiety comprising long alkyl or alkenyl chains, and optionally linked to an antigen; and to helical lipopeptide bundles and synthetic virus-like particles formed by aggregation. The nanometer size and shape of these bundles and particles, their stability under aqueous physiological conditions, their chemical composition, the possibility to incorporate B- and T-cell epitopes, and their production by chemical synthesis, make them highly suitable as vaccine delivery vehicles.Type: ApplicationFiled: December 6, 2007Publication date: January 21, 2010Applicant: UNIVERSITÄT ZÓRICH PROREKTORAT FORSCHUNGInventors: Francesca Boato, Annabelle Freund, Arin Ghasparian, Kerstin Moehle, John A. Robinson, Richard M. Thomas