Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

The present invention relates to linker molecules of formula (1), X-T.sub.b-V.sub.a—U—Y—Z (1) and a method for purifying peptides using said linker molecules. The linker molecule can be coupled to a purification resin via the moiety X and to a peptide via the moiety Y under the release of the leaving group Z. T is an optional spacer moiety and V is an optional electron withdrawing moiety. U is an aryl or 5- or 6-membered heteroaryl moiety bound to at least one electron withdrawing moiety V, W or E. The linker is stable under acidic conditions and releases the peptide upon addition of a reducing agent.

A compound represented by general formula (I) (in the formula, all symbols are as described in the description) or a salt thereof has a potent nerve-protecting and/or -repairing activity, and therefore can be used as a therapeutic agent for neuropathy (e.g., chronic inflammatory demyelinating polyneuropathy, Guillain-Barre syndrome, periarteritis nodosa, allergic vasculitis, diabetic peripheral neuropathy, entrapment neuropathy, peripheral neuropathy associated with the administration of a chemotherapeutic drug, or peripheral neuropathy associated with Charcot-Marie-Tooth disease).

##STR00001##

Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.

Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.

Provided is a compound of Formula (I): ##STR00001## wherein the variable groups are defined herein.

A compound represented by formula (I) ##STR00001## or an N-oxide compound thereof is provided with excellent control efficacies against harmful arthropods, wherein A.sup.1 represents a nitrogen atom or a CR.sup.4; R.sup.4 represents a hydrogen atom, a OR.sup.27, a NR.sup.27R.sup.28, a cyano group, a nitro group, or a halogen atom; ##STR00002##
hereinafter referred to as “Het”, represents Het-1, Het-2, Het-3, or Het-4: ##STR00003## wherein #.sup.1 represents the binding position of Het and T, and #.sup.2 represents the binding position of Het and ##STR00004## T represents T-1, T-2, T-3, T-4, T-5, T-6, or T-7: ##STR00005## R.sup.1 represents a C1-C10 chain hydrocarbon group having one or more halogen atoms or the like; and R.sup.2 represents a C1-C6 alkyl group optionally having one or more halogen atoms or the like.

A compound represented by formula (I) ##STR00001## or an N-oxide compound thereof is provided with excellent control efficacies against harmful arthropods, wherein A.sup.1 represents a nitrogen atom or a CR.sup.4; R.sup.4 represents a hydrogen atom, a OR.sup.27, a NR.sup.27R.sup.28, a cyano group, a nitro group, or a halogen atom; ##STR00002##
hereinafter referred to as “Het”, represents Het-1, Het-2, Het-3, or Het-4: ##STR00003## wherein #.sup.1 represents the binding position of Het and T, and #.sup.2 represents the binding position of Het and ##STR00004## T represents T-1, T-2, T-3, T-4, T-5, T-6, or T-7: ##STR00005## R.sup.1 represents a C1-C10 chain hydrocarbon group having one or more halogen atoms or the like; and R.sup.2 represents a C1-C6 alkyl group optionally having one or more halogen atoms or the like.

A compound of formula (I), or an N-oxide thereof is provided. In the compound of formula (I), Het.sup.1 represents Het.sup.1-1, Het.sup.1-2, Het.sup.1-3, Het.sup.1-4, Het.sup.1-5, Het.sup.1-6, Het.sup.1-7, Het.sup.1-8, or Het.sup.1-9, and the remaining variable groups are as defined in the specification. The compound of formula (I), or N-oxide thereof has a superior effect in controlling arthropod pests. ##STR00001##