Patents by Inventor Roger Schibli

Roger Schibli 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).

  • Patent number: 10434180
    Abstract: The present application relates to methods for the enzymatic functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
    Type: Grant
    Filed: July 19, 2016
    Date of Patent: October 8, 2019
    Assignees: INNATE PHARMA, PAUL SCHERRER INSTITUT
    Inventors: Delphine Bregeon, Patrick Dennler, Christian Belmant, Laurent Gauthier, François Romagne, Eliane Fischer, Roger Schibli
  • Publication number: 20190255200
    Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the 18F isotope is linked via a prosthetic group, more specifically via a prosthetic group having a saccharide group, such as a cyclic mono- or oligosaccharide, preferably based on a pyranoside or furanoside, which is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
    Type: Application
    Filed: May 1, 2019
    Publication date: August 22, 2019
    Applicant: MERCK & CIE
    Inventors: Roger SCHIBLI, Rudolf MOSER, Christina Magdalena MULLER, Simon Mensah AMETAMEY, Cindy Ramona FISCHER, Viola GROEHN
  • Publication number: 20190240360
    Abstract: A gastrin analogue shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analogue PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH2, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogues with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine.
    Type: Application
    Filed: October 11, 2018
    Publication date: August 8, 2019
    Applicant: Paul Scherrer Institut
    Inventors: Martin Behe, Roger SCHIBLI
  • Patent number: 10357576
    Abstract: The present invention is directed towards new 18F-folate/antifolate analog radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F-heterocycle, their precursors, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: July 23, 2019
    Assignee: MERECK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Mueller, Simon Mensah Ametamey, Thomas Betzel, Viola Groehn
  • Publication number: 20190194641
    Abstract: Site-specific modification of proteins with microbial transglutaminase (MTG) is a powerful and versatile strategy for a controlled modification of proteins under physiological conditions. Solid-phase microbead-immobilization is used to site-specifically and efficiently attach different functional molecules important for further downstream applications to proteins of therapeutic relevance including scFV, Fab-fragment and antibodies. MTG remained firmly immobilized with no detectable column bleeding and enzyme activity was sustained during continuous operation. Immobilized MTG shows enhanced selectivity towards a certain residue in the presence of several reactive residues which are all targeted when the conjugation was carried out in solution. The generation of dual site-specifically conjugated IgG1 with immobilized and MTG in solution is reported, i.e. site-specific conjugation to glutamine and lysine residues of IgG1 antibody.
    Type: Application
    Filed: July 11, 2017
    Publication date: June 27, 2019
    Inventors: PHILIPP RENE SPYCHER, MARTIN BEHE, ROGER SCHIBLI, DAVID HURWITZ
  • Patent number: 10322195
    Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the 18F isotope F is linked via a prosthetic group, more specifically via a prosthetic group having a saccharide group, such as a cyclic mono- or oligosaccharide, preferably based on a pyranoside or furanoside, which is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
    Type: Grant
    Filed: August 21, 2012
    Date of Patent: June 18, 2019
    Assignee: Merck & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Cindy Ramona Fischer, Viola Groehn
  • Patent number: 10130724
    Abstract: A gastrin analog shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analog PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH2, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogs with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine.
    Type: Grant
    Filed: October 23, 2014
    Date of Patent: November 20, 2018
    Assignee: Paul Scherrer Institut
    Inventors: Martin Behe, Roger Schibli
  • Patent number: 10132799
    Abstract: Provided is a method for the functionalization of immunoglobulins through the use of transglutaminase, including methods for screening functionalized antibodies for characteristics of interest, antibody compositions comprising a plurality of functionalized antibodies, and functionalized antibodies with rodent constant regions.
    Type: Grant
    Filed: July 10, 2013
    Date of Patent: November 20, 2018
    Assignees: INNATE PHARMA, PAUL SCHERRER INSTITUT
    Inventors: Christian Belmant, Delphine Bregeon, Patrick Dennler, Eliane Fischer, François Romagne, Roger Schibli, Laurent Gauthier
  • Publication number: 20180193476
    Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
    Type: Application
    Filed: September 12, 2017
    Publication date: July 12, 2018
    Inventors: Patrick Dennler, Delphine Bregeon, Laurent Gauthier, François Romagné, Christian Belmant, Eliane Fischer, Roger Schibli
  • Publication number: 20180072734
    Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein fluorine-18 is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of therapy of cancer and inflammatory and autoimmune diseases.
    Type: Application
    Filed: September 21, 2017
    Publication date: March 15, 2018
    Applicant: MERCK & CIE
    Inventors: Roger SCHIBLI, Rudolf MOSER, Cristina Magdalena MULLER, Simon Mensah AMETAMEY, Tobias Ludwig ROSS, Viola GROEHN
  • Publication number: 20180071402
    Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
    Type: Application
    Filed: July 19, 2017
    Publication date: March 15, 2018
    Inventors: Delphine Bregeon, Patrick Dennler, Christian Belmant, Eliane Fischer, Laurent Gauthier, Francois Romagné, Roger Schibli
  • Patent number: 9764038
    Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: September 19, 2017
    Assignees: INNATE PHARMA, PAUL SCHERRER INSTITUT
    Inventors: Patrick Dennler, Delphine Bregeon, Laurent Gauthier, François Romagné, Christian Belmant, Eliane Fischer, Roger Schibli
  • Patent number: 9717803
    Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: August 1, 2017
    Assignees: INNATE PHARMA, PAUL SCHERRER INSTITUT
    Inventors: Delphine Bregeon, Patrick Dennler, Christian Belmant, Eliane Fischer, Laurent Gauthier, Francois Romagné, Roger Schibli
  • Publication number: 20170128599
    Abstract: The present invention is directed towards novel folate-conjugates of formula I wherein F is a folate or derivative thereof, Z1, Z2, Z3 are independently of each other C or N, S1 to S4 are independently of each other a single bond or a spacer, Ra, Ra?, and Rb are donor groups and/or another group F, Rc is optionally another group F and n is 1 or 2. The invention further contemplates the corresponding metal-chelate complexes as well as pharmaceutical compositions thereof, and their uses in diagnostic imaging and radiotherapy.
    Type: Application
    Filed: November 22, 2016
    Publication date: May 11, 2017
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Roger SCHIBLI, Cristina Magdalena MULLER, Viola GROEHN, Urs MICHEL, Christoph SPARR, Thomas Leighton MINDT
  • Publication number: 20160331842
    Abstract: The present application relates to methods for the enzymatic functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
    Type: Application
    Filed: July 19, 2016
    Publication date: November 17, 2016
    Inventors: Delphine Bregeon, Patrick Dennler, Christian Belmant, Laurent Gauthier, François Romagne, Eliane Fischer, Roger Schibli
  • Publication number: 20160256580
    Abstract: A gastrin analogue shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analogue PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH2, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogues with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine.
    Type: Application
    Filed: October 23, 2014
    Publication date: September 8, 2016
    Inventors: MARTIN BEHE, ROGER SCHIBLI
  • Patent number: 9427478
    Abstract: The present application relates to methods for the enzymatic functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: August 30, 2016
    Assignees: Innate Pharma, Paul Scherrer Institut
    Inventors: Delphine Bregeon, Patrick Dennler, Christian Belmant, Laurent Gauthier, François Romagne, Eliane Fischer, Roger Schibli
  • Patent number: 9295739
    Abstract: The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: March 29, 2016
    Assignee: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Harriet Struthers, Viola Groehn, Simon Mensah Ametamey, Cindy Ramona Fischer
  • Patent number: 9265746
    Abstract: Method for selective targeting of one or more effector moiety such as diagnostic or a therapeutic agent to a cell or population of cells expressing a folate-receptor comprising simultaneous or sequential administration of an antifolate with a folate- or pteroate-conjugate comprising said one or more effector moiety.
    Type: Grant
    Filed: May 31, 2006
    Date of Patent: February 23, 2016
    Assignee: MERCK & CIE
    Inventors: Rudolf Moser, Viola Groehn, Roger Schibli, Cristina Magdalena Mueller
  • Publication number: 20150346195
    Abstract: Provided is a method for the functionalization of immunoglobulins through the use of transglutaminase, including methods for screening functionalized antibodies for characteristics of interest, antibody compositions comprising a plurality of functionalized antibodies, and functionalized antibodies with rodent constant regions.
    Type: Application
    Filed: July 10, 2013
    Publication date: December 3, 2015
    Inventors: Christian Belmant, Delphine Bregeon, Patrick Dennler, Eliane Fischer, François Romagne, Roger Schibli