The present invention relates to a process for the preparation of the compounds of formula II ##STR00001##
using a lanthanoid salt.

A compound represented by the following formula (1).

##STR00001##

(In the formula (1), A is a group containing a heteroatom; R.sup.1 is a 2n-valent group having 1 to 30 carbon atoms and optionally having a substituent; R.sup.2 to R.sup.5 are each independently a linear, branched or cyclic alkyl group having 1 to 30 carbon atoms and optionally having a substituent, an aryl group having 6 to 30 carbon atoms and optionally having a substituent, an alkenyl group having 2 to 30 carbon atoms and optionally having a substituent, an alkynyl group having 2 to 30 carbon atoms and optionally having a substituent, an alkoxy group having 1 to 30 carbon atoms and optionally having a substituent, a halogen atom, a nitro group, an amino group, a carboxylic acid group, a crosslinkable group, a dissociation group, a thiol group or a hydroxy group, wherein the alkyl group, the aryl group, the alkenyl group and the alkoxy group each optionally contain an ether bond, a ketone bond or an ester bond and at least one R.sup.4 and/or at least one R.sup.5 is a hydroxy group and/or a thiol group; m.sup.2 and m.sup.3 are each independently an integer of 0 to 8; m.sup.4 and m.sup.5 are each independently an integer of 0 to 9; n is an integer of 1 to 4; and p.sup.2 to p.sup.5 are each independently an integer of 0 to 2.)

A compound represented by the following formula (1).

##STR00001##

(In the formula (1), A is a group containing a heteroatom; R.sup.1 is a 2n-valent group having 1 to 30 carbon atoms and optionally having a substituent; R.sup.2 to R.sup.5 are each independently a linear, branched or cyclic alkyl group having 1 to 30 carbon atoms and optionally having a substituent, an aryl group having 6 to 30 carbon atoms and optionally having a substituent, an alkenyl group having 2 to 30 carbon atoms and optionally having a substituent, an alkynyl group having 2 to 30 carbon atoms and optionally having a substituent, an alkoxy group having 1 to 30 carbon atoms and optionally having a substituent, a halogen atom, a nitro group, an amino group, a carboxylic acid group, a crosslinkable group, a dissociation group, a thiol group or a hydroxy group, wherein the alkyl group, the aryl group, the alkenyl group and the alkoxy group each optionally contain an ether bond, a ketone bond or an ester bond and at least one R.sup.4 and/or at least one R.sup.5 is a hydroxy group and/or a thiol group; m.sup.2 and m.sup.3 are each independently an integer of 0 to 8; m.sup.4 and m.sup.5 are each independently an integer of 0 to 9; n is an integer of 1 to 4; and p.sup.2 to p.sup.5 are each independently an integer of 0 to 2.)

Disclosed herein are substituted indane derivatives useful as HIF-2 inhibitors. Pharmaceutical compositions comprising said indane derivatives and methods of using said indane derivatives for treating proliferative diseases, such as renal cell carcinoma and von Hippel-Lindau disease, and other conditions associated with HIF-2 activity are also disclosed.

Disclosed herein are substituted indane derivatives useful as HIF-2 inhibitors. Pharmaceutical compositions comprising said indane derivatives and methods of using said indane derivatives for treating proliferative diseases, such as renal cell carcinoma and von Hippel-Lindau disease, and other conditions associated with HIF-2 activity are also disclosed.

This disclosure relates to benzhydrol derivatives for managing conditions related to the Hypoxia Inducible Factor (HIF) pathway such as uses in treating cancer. In certain embodiment, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiment, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof.

This disclosure relates to benzhydrol derivatives for managing conditions related to the Hypoxia Inducible Factor (HIF) pathway such as uses in treating cancer. In certain embodiment, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiment, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof.

A compound is provided according to structure 4, (4) wherein n has a value from 0 to 48 and Z is hydroxyl or a benzene ring bearing substituents R.sub.11-R.sub.15, wherein R.sub.1-R.sub.15 are each individually selected from the group consisting of H, allyl, alkyl, alkoxy, phenyl, phenoxy, halide, hydroxyl, glycidyl, (meth)acryloyl, 3-(meth)acryloyl-2-hydroxy-1-propoxy, 2,3-epoxypropyl, maleate, and structure (a) wherein at least one of R.sub.1-R.sub.5, at least one of R.sub.6-R.sub.10, and at least one of R.sub.11-R.sub.15 is hydroxyl or an ether or ester derived from it and one of the R.sub.6-R.sub.10 groups is replaced by a direct bond to the CXY group. ##STR00001##

A compound is provided according to structure 4, (4) wherein n has a value from 0 to 48 and Z is hydroxyl or a benzene ring bearing substituents R.sub.11-R.sub.15, wherein R.sub.1-R.sub.15 are each individually selected from the group consisting of H, allyl, alkyl, alkoxy, phenyl, phenoxy, halide, hydroxyl, glycidyl, (meth)acryloyl, 3-(meth)acryloyl-2-hydroxy-1-propoxy, 2,3-epoxypropyl, maleate, and structure (a) wherein at least one of R.sub.1-R.sub.5, at least one of R.sub.6-R.sub.10, and at least one of R.sub.11-R.sub.15 is hydroxyl or an ether or ester derived from it and one of the R.sub.6-R.sub.10 groups is replaced by a direct bond to the CXY group. ##STR00001##

The present invention relates to a process for the preparation of the compounds of formula II

##STR00001##

using a lanthanoid salt.