- BIO-ORTHOGONAL DRUG ACTIVATION
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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.
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- Clicking 1,2,4,5-tetrazine and cyclooctynes with tunable reaction rates
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Substituted tetrazines have been found to undergo facile inverse electron demand Diels-Alder reactions with "tunable" reaction rates.
- Chen, Weixuan,Wang, Danzhu,Dai, Chaofeng,Hamelberg, Donald,Wang, Binghe
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p. 1736 - 1738
(2012/03/09)
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- TETRAZINE-BASED BIO-ORTHOGONAL COUPLING REAGENTS AND METHODS
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Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and/or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.
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Page/Page column 20
(2009/02/11)
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- Diels-Alder Reactions of 3,6-Diphenyl-1,2,4,5-Tetrazine and 3,6-Di(2-pyridyl)-1,2,4,5-tetrazine with some 1-Morpholinocycloalkenes
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The reactions of 3,6-diphenyl-1,2,4,5-tetrazine 1 and 3,6-di(2-pyridyl)-1,2,4,5-tetrazine 2 with the enamines 3a-d derived from morpholine and the 5-,6-,7- and 8-membered cyclic ketones have been investigated.A number of pyridazine derivatives 4-7 most of
- Atfah, M. Adnan
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p. 717 - 719
(2007/10/02)
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- Kinetic Investigations of Diels - Alder - Reactions of Cyclooctyne with Consecutive Aromatization
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The tricyclic compounds 3a - g, generated from cyclooctyne (1) and the cyclic dienes 2a - g, show a totally different stability. 3a, b, f, and g decompose spontaneously.By elimination of CO2, SO2, CO, and N2, respectively, the aromatic systems 4a - c are formed. 3c loses C2H4 on heating. 3e is thermally cleaved only to a very small extent, but efficiently in the photolysis and finally 3d is stable against aromatization.Detailed kinetical measurements are performed of the thermal elimination of ethylene and of the photochemical bisdecarbonylation.
- Molz, Thomas,Koenig, Peter,Goes, Robert,Gauglitz, Guenter,Meier, Herbert
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p. 833 - 839
(2007/10/02)
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- REAKTIVITAET VON STICKSTOFF-HETEROCYCLEN GEGENUEBER CYCLOOCTIN ALS DIENOPHIL
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The cycloaddition rate of cyclooctyne to a number of N-containing heterocyclic compounds can be correlated with the reduction potentials of these dienes provided steric substituent effects are approximately equal.
- Balcar, J.,Chrisam, G.,Huber, F. X.,Sauer, J.
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p. 1481 - 1484
(2007/10/02)
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