# US 2013/0158087 A1 · Tg2 inhibitors and uses thereof

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- Number: US 2013/0158087 A1
- Document ID: US20130158087A1
- Status: Published application
- Kind: A1
- Application number: 13/806,257
- Filed: 2011-06-21
- Published: 2013-06-20
- Earliest claimed: 2010-06-21
- Assignees: Board of Regents, The University of Texas System
- Inventors: Kapil Mehta; Anupam Kumar; Jansina Fok; Shuxing Zhang
- Web page: https://patentgrep.com/patent/US20130158087A1

## CPC

- C07D 333/04: not substituted on the ring sulphur atom
- A61K 31/381: having five-membered rings
- A61K 31/41: having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61P 35/00: Antineoplastic agents
- C07D 259/00: Heterocyclic compounds containing rings having more than four nitrogen atoms as the only ring hetero atoms
- C07D 333/24: Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D 333/34: Sulfur atoms
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype.

## Claims

### Claim 1

A method of treating drug resistance in a subject in need thereof comprising the step of administering to the subject a therapeutic amount of a compound of the structural Formula I
wherein R1, R2, R3 and R4 are each independently hydrido, halo, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, dialkylamino, carbamoyl, nitro, cyano, perfluoroalkyl, trifluoromethylalkyl, hydroxyl, thiol, hydroxycarbonyl, or alkylcarbonyl.

### Claim 2

A method of treating drug resistance in a subject in need thereof comprising the step of administering to the subject a therapeutic amount of a compound of the structural Formula II
wherein R5 is H or methyl, and R7, R7, R8 and R9 are independently selected from hydrido, halo, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, dialkylamino, carbamoyl, nitro, cyano, perfluoroalkyl, trifluoromethylalkyl, hydroxyl, thiol, hydroxycarbonyl, alkylcarbonyl, or may constitute a 5- or 6-membered heterocyclic ring containing one or two oxygen atoms.

### Claim 3

A method of treating drug resistance in a subject in need thereof comprising the step of administering to the subject a therapeutic amount of a compound of the structural Formula III
wherein R10, R11, R12 and R13 are independently selected from hydrido, halo, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, dialkylamino, carbamoyl, nitro, cyano, perfluoroalkyl, trifluoromethylalkyl, hydroxyl, thiol, hydroxycarbonyl, or alkylcarbonyl.

### Claim 4

A compound useful in treating metastasis of cancer cells wherein the compound is of the structural formula, Formula I:
wherein R1, R2, R3 and R4 are each independently hydrido, halo, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, dialkylamino, carbamoyl, nitro, cyano, perfluoroalkyl, trifluoromethylalkyl, hydroxyl, thiol, hydroxycarbonyl, or alkylcarbonyl.

### Claim 5

A compound useful in treating metastasis of cancer cells wherein the compound is of the structural formula, Formula II
wherein R5 is H or methyl, and R7, R7, R8 and R9 are independently selected from hydrido, halo, alkoxy, amino, alkylamino, alkylcarbonylamino, dialkylamino, carbamoyl, nitro, cyano, perfluoroalkyl, trifluoromethylalkyl, hydroxyl, thiol, hydroxycarbonyl, alkylcarbonyl, or may constitute a 5- or 6-membered heterocyclic ring containing one or two oxygen atoms.

### Claim 6

A compound useful in treating metastasis of cancer cells wherein the compound is of the structural formula, Formula III
wherein R10, R11, R12 and R13 are independently selected from hydrido, halo, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, dialkylamino, carbamoyl, nitro, cyano, perfluoroalkyl, trifluoromethylalkyl, hydroxyl, thiol, hydroxycarbonyl, or alkylcarbonyl.

### Claim 7 (depends on 4, 5)

Use of the compound of claim 4, 5, or 6 for the manufacture of a medicament for treating cancer.

### Claim 8 (depends on 1, 2)

The method of claim 1, 2, or 3, wherein the compound treats cancer.