C09B29/0048

Ink set and thermal transfer recording sheet

An ink set contains a first ink containing a compound in which a pyrazolone ring and a thiazole ring are bonded and a second ink containing a compound in which a pyrazolone ring and a pyridinedione ring are bonded. A thermal transfer recording sheet has a first ink layer containing a compound in which a pyrazolone ring and a thiazole ring are bonded and a second ink layer containing a compound in which a pyrazolone ring and a pyridinedione ring are bonded.

Small Molecules That Covalently Modify Transthyretin
20170190660 · 2017-07-06 ·

A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and

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reacts chemoselectively with one or two of four Lys-15 -amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.

AZOARYLS AS REVERSIBLY MODULATABLE TUBULIN INHIBITORS

The invention concerns a new class of tubulin polymerisation inhibitors and their applications in research and medicine, notably in chemotherapy. The invention proposes new azoaryl derivatives of formula (I):

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as defined in Claim 1, which may be fully reversibly interconverted between non-tubulin-binding trans and tubulin-binding as isomeric forms, either by irradiation or spontaneously. The invention also concerns compounds with a azoaryl structure for use in studying the cytoskeleton and/or its associated processes, or in the treatment of a disease for which a tubulin polymerisation inhibition activity has a beneficial effect, wherein the compound is administered to the cell, organism or patient in need of such treatment in the trans form of the diazenyl bond, and where this trans form is inactive as regards a tubulin polymerisation inhibition effect, and where after photoisomerisation in vitro, in cellulo or in vivo to an azoaryl compound in its cis isomeric form of the diazenyl bond by the application of light, optionally with modification in vitro, in cellulo or in vivo of one or more substituents, the resultant cis form is active as regards a tubulin polymerisation inhibition effect.