Patent classifications
C07D333/18
ARYL COMPOUNDS AND POLYMERS AND METHODS OF MAKING AND USING THE SAME
Disclosed herein are embodiments of aryl compounds and polymers thereof that are made using methods that do not require harsh conditions or expensive reagents. The methods disclosed herein utilize precursor compounds that can be polymerized to form polycyclic aromatic hydrocarbons and polymers, such as carbon-based polymers like nanostructures (e.g., graphene or graphene-like nanoribbons).
Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer
Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: ##STR00001##
wherein W, X, Y, Z, x, R.sup.1, R.sup.2, R.sup.3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.
Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer
Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: ##STR00001##
wherein W, X, Y, Z, x, R.sup.1, R.sup.2, R.sup.3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.
IDO/TDO Inhibitor
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R.sup.1 and R.sup.2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R.sup.4 represents, for example, C(NH)HN.sub.2, and R.sup.6 represents, for example, a substituted or unsubstituted aryl group].
##STR00001##
IDO/TDO Inhibitor
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R.sup.1 and R.sup.2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R.sup.4 represents, for example, C(NH)HN.sub.2, and R.sup.6 represents, for example, a substituted or unsubstituted aryl group].
##STR00001##
Ion pair catalysis of tungstate and molybdate
D The present invention relates to ion pair catalysts (I) comprising the cationic bisguanidinium ligand (A) and diperoxomolybdate anion (B). The present invention also relates to ion pair catalysts (III) comprising the cationic bisguanidinium ligand (C) and peroxotungstate anion (D). It further relates to the use of the said catalysts in the manufacture of enantiomerically enriched sulfoxides. ##STR00001##
Ion pair catalysis of tungstate and molybdate
D The present invention relates to ion pair catalysts (I) comprising the cationic bisguanidinium ligand (A) and diperoxomolybdate anion (B). The present invention also relates to ion pair catalysts (III) comprising the cationic bisguanidinium ligand (C) and peroxotungstate anion (D). It further relates to the use of the said catalysts in the manufacture of enantiomerically enriched sulfoxides. ##STR00001##
METASTASIS-INHIBITING COMPOSITION OF NOVEL METHYLSULFONAMIDE DERIVATIVE COMPOUND
Provided is a metastasis-inhibiting composition containing a methylsulfonamide-based derivative compound as an active ingredient. More specifically, the compounds inhibit the activity of chromosome segregation 1-like (CSE1L), and suppress intracellular nuclear transport to inhibit the movement and/or invasion of cancer cells, and thus effectively inhibit metastasis.
METASTASIS-INHIBITING COMPOSITION OF NOVEL METHYLSULFONAMIDE DERIVATIVE COMPOUND
Provided is a metastasis-inhibiting composition containing a methylsulfonamide-based derivative compound as an active ingredient. More specifically, the compounds inhibit the activity of chromosome segregation 1-like (CSE1L), and suppress intracellular nuclear transport to inhibit the movement and/or invasion of cancer cells, and thus effectively inhibit metastasis.
Diarylethene compounds and uses thereof
A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a ring-closed isomer B is provided. For substitutent groups, Z is N, O or S; each R.sub.1 is independently selected from the group consisting of H, or halo; each R.sub.2 is independently selected from the group consisting of H, halo, a polymer backbone, alkyl or aryl; or, when both R.sub.2 together form CHCH and form part of a polymer backbone; each R.sub.3 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl; each R.sub.4 is aryl; and each R.sub.5 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl. ##STR00001##