Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: The present invention relates to A phenol compound according to Formula (I): wherein: R1 is selected from the group consisting of, optionally substituted, 2-pyridyl, 3-pyridiyl and 4-pyridyl groups, wherein R1 is at position 2 or 3 of the phenol ring; R2 is selected from the group consisting of, optionally substituted, 2-pyridyl, 3-pyridiyl, 4-pyridyl and phenyl groups, wherein R2 is at position 5 or 6 of the phenol ring; and the phenol ring is optionally substituted at one or two positions, independently selected from positions 2, 3, 5 and 6, with a halogen atom or a with an optionally substituted C6-C12 aryl group or an optionally substituted C1-C10 alkyl group. The present invention relates also to (co)polymers comprising the phenol compound according to Formula (I) and membranes and ionic resins comprising said (co)polymers.

Abstract: The invention relates to supramolecular ionomers. i.e. polymers having quadruple hydrogen bonding units (4H-units) and ionic groups or ionogenic groups within their structure. The supramolecular ionomers can be dispersed or solubilized in water at high solids contents while maintaining low viscosities, facilitating easy use and processing of the resulting aqueous formulations. The aqueous supramolecular ionomer compositions have excellent film-forming properties. Moreover, the polymer materials have good mechanical properties after drying, as they are not tacky, show high elasticity and low or no creep.

Abstract: The present invention relates to thioic acids according to formula (II) suitable as building block for polythioesters; Wherein X is O, N or S and whereby R1 is chosen from (—CH2—)2, —CH2—O—CH2— or (—CH2—)3, R2 is preferably chosen from a biodegradable oligomer or polymer chosen from poly(lactide) (PLLA), polyglycolide (PGA), co-oligomers or copolymers of PLA and PGA (PLGA), poly(anhydrides), poly(trimethylenecarbonates), poly(orthoesters), poly(dioxanones), poly(?-caprolactones) (PCL) or polyesteramides and n>1.

Abstract: The present invention relates to A phenol compound according to Formula (I): wherein: R1 is selected from the group consisting of, optionally substituted, 2-pyridyl, 3-pyridiyl and 4-pyridyl groups, wherein R1 is at position 2 or 3 of the phenol ring; R2 is selected from the group consisting of, optionally substituted, 2-pyridyl, 3-pyridiyl, 4-pyridyl and phenyl groups, wherein R2 is at position 5 or 6 of the phenol ring; and the phenol ring is optionally substituted at one or two positions, independently selected from positions 2, 3, 5 and 6, with a halogen atom or a with an optionally substituted C6-C12 aryl group or an optionally substituted C1-C10 alkyl group. The present invention relates also to (co)polymers comprising the phenol compound according to Formula (I) and membranes and ionic resins comprising said (co)polymers.

Abstract: The invention relates to the synthesis of siloxane polymers containing self-complementary quadruple hydrogen bonding groups (4H-units). The resulting polymers show unique new characteristics that result from the reversible, physical interactions between the polysiloxane chains that are based on the (supramolecular) interactions between the 4H-units. The polysiloxanes in this invention show unprecedented bulk material properties and are used as gelling agents for silicone fluids. The resulting gels are clear and display good material properties, while having unparalleled high silicone fluid contents.

Abstract: The invention relates to supramolecular ionomers. i.e. polymers having quadruple hydrogen bonding units (4H-units) and ionic groups or ionogenic groups within their structure. The supramolecular ionomers can be dispersed or solubilized in water at high solids contents while maintaining low viscosities, facilitating easy use and processing of the resulting aqueous formulations. The aqueous supramolecular ionomer compositions have excellent film-forming properties. Moreover, the polymer materials have good mechanical properties after drying, as they are not tacky, show high elasticity and low or no creep.