The present invention relates to a novel compound comprising a galactose trigger moiety and cyclopropabenzindole (CBI), and an antibody-drug conjugate prepared by using same.

A glycosyl donor represented by formula (I) is used for preparing an S-glycoside compound represented by formula (III), an O-glycoside compound represented by formula (V), and a C-glycoside compound represented by formula (V). The glycosyl donor is a raw material in the preparation of O-glycoside, S-glycoside, and C-glycoside compounds by means of a free radical reaction, most of which have a special α configuration.

A compound of Formula (I):

##STR00001##

or anyone of its metabolites or a pharmaceutically acceptable salt thereof, for use for treating and/or preventing an inflammatory disease, disorder or condition, wherein each R is independently hydrogen, halogen, —CN, hydroxyl, (C.sub.1-C.sub.3)fluoroalkyl, (C.sub.1-C.sub.3)fluoroalkoxy, (C.sub.3-C.sub.6)cycloalkyl, —NO.sub.2, —NR.sub.1R.sub.2, (C.sub.1-C.sub.4)alkoxy, phenoxy, —NR.sub.1—SO.sub.2—NR.sub.1R.sub.2, —NR.sub.1—SO.sub.2—R1, —NR.sub.1—C(═O)—R.sub.1, —NR.sub.1—C(═O)—NR.sub.1R.sub.2, —SO.sub.2—NR.sub.1R.sub.2, —SO.sub.3H, —O—SO.sub.2—OR.sub.3, —O—P(═O)—(OR.sub.3)(OR.sub.4), —O—CH.sub.2—COOR.sub.3, (C.sub.1-C.sub.3)alkyl; each R′ is independently hydrogen, (C1-C3)alkyl, hydroxyl, halogen, —NO.sub.2, —NR.sub.1R.sub.2, morpholinyl, morpholino, N-methylpiperazinyl, (C.sub.1-C.sub.3)fluoroalkyl, (C.sub.1-C.sub.4)alkoxy, —O—P(═O)—(OR.sub.3)(OR.sub.4), —CN, a —NH—SO.sub.2—N(CH.sub.3).sub.2 group, or other groups and further relates to A compound of formula (IV):

##STR00002##

or a pharmaceutically acceptable salt thereof, for use for treating and/or preventing an inflammatory disease, disorder or condition, wherein V, Z, R, R′, n, and n′ are as described above.

In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

The present application provides, in some aspects, methods of treating cancers, such as homologous recombination (HR)-deficient cancers. In some embodiments, the disclosure provides a method for treating cancer by administering to a subject a compound of Formula (I):(I), or a pharmaceutically acceptable salt thereof. ##STR00001##

The present application provides, in some aspects, methods of treating cancers, such as homologous recombination (HR)-deficient cancers. In some embodiments, the disclosure provides a method for treating cancer by administering to a subject a compound of Formula (I):(I), or a pharmaceutically acceptable salt thereof. ##STR00001##

This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P.sub.2Y.sub.6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.

This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P.sub.2Y.sub.6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.

Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.