C07D257/08

Cross-linked polycarboxylated polysaccharides and methods of use thereof

The present invention is directed to a polymer comprising a first hyaluronic acid (HA) chain and a second HA chain crosslinked via a linker comprising an unsaturated moiety or a derivative thereof coupled to a tetrazine moiety or a derivative thereof. In some embodiments, the polymer of the invention is characterized by having a crosslinking degree of 0.2 to 4%.

Cross-linked polycarboxylated polysaccharides and methods of use thereof

The present invention is directed to a polymer comprising a first hyaluronic acid (HA) chain and a second HA chain crosslinked via a linker comprising an unsaturated moiety or a derivative thereof coupled to a tetrazine moiety or a derivative thereof. In some embodiments, the polymer of the invention is characterized by having a crosslinking degree of 0.2 to 4%.

BIO-ORTHOGONAL DRUG ACTIVATION

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.

BIO-ORTHOGONAL DRUG ACTIVATION

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.

BIOORTHOGONAL LINKERS AND REACTIONS
20240058455 · 2024-02-22 ·

The present disclosure provides bioorthogonal linkers and reagents, including trans-cyclooctene (TCO)- and tetrazine (Tz)-containing compounds. In a general aspect, the present disclosure provides reagents, conjugates, and bioactive molecules containing a trans-cyclooctene (TCO) fragment. Examples of TCO fragments include: Formulae (I) and (II).

##STR00001##

BIO-ORTHOGONAL DRUG ACTIVATION

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.

BIO-ORTHOGONAL DRUG ACTIVATION

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.

NOVEL COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING THE SAME

Provided is a compound of Chemical Formula 1 or 2:

##STR00001## wherein: R.sub.1 to R.sub.4 are each independently hydrogen or deuterium; n1 to n4 are an integer of 1 to 4; L.sub.1 and L.sub.2 are each independently a direct bond or a substituted or unsubstituted C.sub.6-60 arylene; and Ar.sub.1 and Ar.sub.2 are each independently a substituent of Chemical Formula 3:

##STR00002## wherein X.sub.1 to X.sub.5 are each independently N or C(R.sub.5), wherein at least two of X.sub.1 to X.sub.5 are N; and each R.sub.5 is independently hydrogen, deuterium, a substituted or unsubstituted C.sub.1-20 alkyl, a substituted or unsubstituted C.sub.6-60 aryl, or a substituted or unsubstituted C.sub.2-60 heteroaryl containing at least one of N, O and S, or two adjacent R.sub.5s combine to form a benzene ring; and an organic light emitting device including the same. The device exhibits significantly superior efficiency and lifespan.

NOVEL COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING THE SAME

Provided is a compound of Chemical Formula 1 or 2:

##STR00001## wherein: R.sub.1 to R.sub.4 are each independently hydrogen or deuterium; n1 to n4 are an integer of 1 to 4; L.sub.1 and L.sub.2 are each independently a direct bond or a substituted or unsubstituted C.sub.6-60 arylene; and Ar.sub.1 and Ar.sub.2 are each independently a substituent of Chemical Formula 3:

##STR00002## wherein X.sub.1 to X.sub.5 are each independently N or C(R.sub.5), wherein at least two of X.sub.1 to X.sub.5 are N; and each R.sub.5 is independently hydrogen, deuterium, a substituted or unsubstituted C.sub.1-20 alkyl, a substituted or unsubstituted C.sub.6-60 aryl, or a substituted or unsubstituted C.sub.2-60 heteroaryl containing at least one of N, O and S, or two adjacent R.sub.5s combine to form a benzene ring; and an organic light emitting device including the same. The device exhibits significantly superior efficiency and lifespan.

INHIBITORS OF CREATINE TRANSPORT AND USES THEREOF
20190315680 · 2019-10-17 ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.