Patents by Inventor Marc Stefan Robillard
Marc Stefan Robillard 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: 9463256Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has one or more axial substituents.Type: GrantFiled: October 11, 2011Date of Patent: October 11, 2016Assignee: KONINKLIJKE PHILIPS N.V.Inventors: Johan Lub, Wolter Ten Hoeve, Raffaella Rossin, Sandra Martina Van Den Bosch, Marc Stefan Robillard
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Patent number: 9427482Abstract: Described is a method, and a combination of agents for used therein, by which an agent administered to a subject can be rapidly cleared from circulation. This is achieved by providing an Administration Agent (e.g. a probe for pretargeting) with a reactive group and providing a Clearing Agent with another reactive group, said reactive groups forming a bio-orthogonally reactive pair. Preferably, the reactive pair comprises a cyclooctene or cyclooctyn as one reactant, and a diene as the other reactant. The method and combination can be used for the removal of any bindable molecule from circulation, such as an excess of a pre-targeting probe in the course of a pre-targeting method, a targeting or imaging agent delivered, or the removal of any biomolecule already present in circulation.Type: GrantFiled: December 16, 2011Date of Patent: August 30, 2016Assignee: KONINKLIJKE PHILIPS N.V.Inventors: Raffaella Rossin, Tilman Laeppchen, Sandra Martina Van Den Bosch, Marc Stefan Robillard, Ronny Mathieu Versteegen
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Patent number: 9421274Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.Type: GrantFiled: May 16, 2012Date of Patent: August 23, 2016Assignee: Koninklijke Philips N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
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Publication number: 20160151505Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.Type: ApplicationFiled: May 16, 2012Publication date: June 2, 2016Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin, Freek Johannes Maria Hoeben
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Publication number: 20160106859Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.Type: ApplicationFiled: December 30, 2015Publication date: April 21, 2016Inventors: MARC STEFAN ROBILLARD, HENDRICUS MARIE JANSSEN, WOLTER TEN HOEVE, RONNY MATHIEU VERSTEEGEN, RAFFAELLA ROSSIN
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Publication number: 20150344514Abstract: Disclosed is the use of the reactive components of the inverse electron-demand Diels Alder reaction for chemical masking and unmasking in vitro. This can be applied in complex chemical reactions and, particularly in the synthesis of biomolecules, e.g. on solid supports. The reactive components are a dienophile, particularly a trans-cyclooctene, and a diene, particularly a tetrazine.Type: ApplicationFiled: November 22, 2013Publication date: December 3, 2015Inventors: Marc Stefan Robillard, Ronny Mathieu Versteegen, Wolter ten Hoeve, Raffaella Rossin
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Publication number: 20150297741Abstract: Disclosed is a kit for the administration and activation of a Prodrug. The kit comprises a Masking Moiety linked, directly or indirectly, to a Trigger moiety, which in turn is linked to a Drug, and an Activator for the Trigger moiety. The Trigger moiety comprises a dienophile and the Activator comprises a diene, whereby the dienophile is an eight-membered non-aromatic cyclic alkenylene group, preferably a cyclooctene group, and more preferably a trans-cyclooctene group. The Trigger and the Activator undergo a fast, bio-orthogonal reaction resulting in the release of the Masking Moiety, and activation of the drug.Type: ApplicationFiled: November 22, 2013Publication date: October 22, 2015Applicant: Tagworks Pharmaceuticals B.V.Inventor: Marc Stefan Robillard
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Publication number: 20150147273Abstract: A method for determining whether compound 0118 is a candidate treatment for a patient includes processing, via a processor, image data of tissue of interest of a patient including a cancer to determine whether a radiolabeled analog of compound 0118 is present in the tissue of interest represented in the image data and generating a signal indicating that compound 0118 is a candidate treatment for the patient in response to the determining that the radiolabeled analog of compound 0118 is present in a predetermined amount in the tissue of interest represented in the image data, wherein the presence of the radiolabeled analog of compound 0118 in the tissue of interest indicates presence of a sub-type of cancer having a galectin-1 molecular target, which is a sub-type of treatable by compound 0118.Type: ApplicationFiled: June 10, 2013Publication date: May 28, 2015Applicant: Koninklijke Philips N.V.Inventors: Tilman Lappchen, Holger Gruell, Marc Stefan Robillard, Johan Lub
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Publication number: 20140199331Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.Type: ApplicationFiled: May 16, 2012Publication date: July 17, 2014Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
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Publication number: 20140093450Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.Type: ApplicationFiled: May 7, 2012Publication date: April 3, 2014Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Johan Lub, Raffaella Rossin, Sandra Martina Van Ben Bosch, Ronny Mathieu Versteegen
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Publication number: 20140093522Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.Type: ApplicationFiled: May 16, 2012Publication date: April 3, 2014Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
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Patent number: 8623325Abstract: The present invention describes the modification of polypeptides, more particularly channel proteins with a thiol reactive agent so as to introduce an azide group. The present invention further describes vesicles comprising channel proteins modified according to the invention, which upon reaction with a phosphine open up thereby releasing the content of the vesicles. The reagents, polypeptides and vesicles described in the present invention have in vivo and in vitro applications in both drug delivery and imaging.Type: GrantFiled: May 26, 2009Date of Patent: January 7, 2014Assignee: Koninklijke Philips N.V.Inventors: Marc Stefan Robillard, George Thomas Robillard, Armagan Kocer
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Publication number: 20130272959Abstract: Described is a method, and a combination of agents for used therein, by which an agent administered to a subject can be rapidly cleared from circulation. This is achieved by providing an Administration Agent (e.g. a probe for pretargeting) with a reactive group and providing a Clearing Agent with another reactive group, said reactive groups forming a bio-orthogonally reactive pair. Preferably, the reactive pair comprises a cyclooctene or cyclooctyn as one reactant, and a diene as the other reactant. The method and combination can be used for the removal of any bindable molecule from circulation, such as an excess of a pre-targeting probe in the course of a pre-targeting method, a targeting or imaging agent delivered, or the removal of any biomolecule already present in circulation.Type: ApplicationFiled: December 16, 2011Publication date: October 17, 2013Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V.Inventors: Raffaella Rossin, Tilman Laeppchen, Sandra Martina Van Den Bosch, Marc Stefan Robillard, Ronny Mathieu Versteegen
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Publication number: 20130189184Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has one or more axial substituents.Type: ApplicationFiled: October 11, 2011Publication date: July 25, 2013Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V.Inventors: Johan Lub, Wolter Ten Hoeve, Raffaella Rossin, Sandra Martina Van Den Bosch, Marc Stefan Robillard
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Publication number: 20120039803Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an alkene or alkyne dienohile.Type: ApplicationFiled: April 12, 2010Publication date: February 16, 2012Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V.Inventors: Marc Stefan Robillard, Raffaella Rossin, Johan Lub, Pascal Renart Verkerk, Dirk Burdinski
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Publication number: 20120034161Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other a cyclooctene or cyclooctyne.Type: ApplicationFiled: April 12, 2010Publication date: February 9, 2012Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V.Inventors: Marc Stefan Robillard, Raffaella Rossin, Johan Lub, Pascal Renart Verkerk, Dirk Burdinski
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Publication number: 20110064667Abstract: The present invention describes the modification of polypeptides, more particularly channel proteins with a thiol reactive agent so as to introduce an azide group. The present invention further describes vesicles comprising channel proteins modified according to the invention, which upon reaction with a phosphine open up thereby releasing the content of the vesicles. The reagents, polypeptides and vesicles described in the present invention have in vivo and in vitro applications in both drug delivery and imaging.Type: ApplicationFiled: May 26, 2009Publication date: March 17, 2011Inventors: Marc Stefan Robillard, George Thomas Robillard, Armagan Kocer
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Publication number: 20100227798Abstract: The invention provides methods and tools for the in vivo self-assembly of drugs. This makes it possible to reduce problems associated with the lack of selectivity, reduced solubility and other disadvantages of intact drugs.Type: ApplicationFiled: March 20, 2007Publication date: September 9, 2010Applicant: Koninklijke Philips Electronics N.V.Inventors: Marc Stefan Robillard, Holger Cruell
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Publication number: 20080274057Abstract: The Staudinger reaction can be used for activation of prodrugs or pro-imaging probes. The invention relates to a method of preparing and activating prodrugs or pro-imaging probes by using the Staudinger reaction and to kits for medical imaging and/or therapy comprising at least one prodrug and/or pro-imaging probe comprising at least one azide and/or phosphine group.Type: ApplicationFiled: October 2, 2006Publication date: November 6, 2008Applicant: KONINKLIJKE PHILIPS ELECTRONICS, N.V.Inventors: Marc Stefan Robillard, Holger Gruell
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Publication number: 20080267878Abstract: The use of a selective chemical and bioorthogonal reaction providing a covalent ligation such as the [3+2] cycloaddition, in targeted molecular imaging and therapy is presented, more specifically with interesting applications for pre-targeted imaging or therapy. Current pre-targeted imaging is hampered by the fact that it relies solely on natural/biological targeting constructs (biotin/streptavidin). Size considerations and limitations associated with their endogenous nature severely limit the number of applications. The present invention describes how the use of an abiotic, bio-orthogonal reaction which forms a stable adduct under physiological conditions, by way of a small or undetectable bond, can overcome these limitations.Type: ApplicationFiled: September 29, 2006Publication date: October 30, 2008Applicant: KONINKLIJKE PHILIPS ELECTRONICS, N.V.Inventors: Marc Stefan Robillard, Holger Gruell