# US 2014/0193518 A1 · Kinase inhibitor compounds

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- Number: US 2014/0193518 A1
- Document ID: US20140193518A1
- Status: Published application
- Kind: A1
- Application number: 13/730,779
- Filed: 2012-12-28
- Published: 2014-07-10
- Earliest claimed: 2007-06-06
- Assignees: University of Florida Research Foundation, Inc.
- Inventors: Peter P. Sayeski; Gyorgy M. Keseru
- Web page: https://patentgrep.com/patent/US20140193518A1

## CPC

- A61K 31/05: Phenols {(cannabinoids A61K31/658)}
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- C07C 215/50: with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
- C07C 249/02: of compounds containing imino groups
- C07D 213/50: Ketonic radicals
- C07D 217/16: substituted by oxygen atoms
- C07F 9/141: Esters of phosphorous acids
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)

## Abstract

The invention relates to kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating disorders, especially cancer.

## Claims

### Claim at position 1

1-18. (canceled)

### Claim 19

A method of treating cancer in a subject comprising administering to the subject identified as in need thereof a compound of Table 1 or Table 2, or a salt, hydrate or solvate thereof.

### Claim 20 (depends on 19)

The method of claim 19, wherein the cancer is selected from the group consisting of: leukemias, lymphomas, myelomas, and solid tumors.

### Claim 21 (depends on 20)

The method of claim 20, wherein the leukemia is selected from the group consisting of: chronic myelogenous leukemia (CML), acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).

### Claim at position 5

22-24. (canceled)

### Claim 25

A method of inhibiting JAK2 in a subject identified as in need of such treatment, comprising: administering a compound of Table 1 or Table 2, or a salt, hydrate or solvate thereof.

### Claim 26 (depends on 19)

The method of claim 19, wherein the compound is 2-(diethylaminomethyl)-4-[4-[3-(diethylaminomethyl)-4-hydroxy-phenyl]hex-3-en-3-yl]phenol (G6), or a derivative thereof.

### Claim 27 (depends on 26)

The method of claim 26, wherein the G6 derivative is a compound selected from Table 2, or a salt, hydrate or solvate thereof.

### Claim 28 (depends on 27)

The method of claim 27, wherein the G6 derivative compound is selected from the group consisting of: D4, D5, D28 and D30.

### Claim 29 (depends on 19)

The method of claim 19, wherein the compound or a salt, hydrate or solvate thereof, is an inhibitor of the Jak2-V617F mutant.

### Claim 30 (depends on 19)

The method of claim 19, wherein the compound or a salt, hydrate or solvate thereof, inhibits Jak2 autophosphorylation.

### Claim 31 (depends on 30)

The method of claim 30, wherein the compound or a salt, hydrate or solvate thereof does not inhibit c-Src or Tyk2 autophosphorylation as effectively as Jak2 autophosphorylation.

### Claim at position 13

32-39. (canceled)

### Claim 40

A kit comprising a compound of Table 1 or Table 2, and instructions for use in treating cancer.

### Claim at position 15

41-43. (canceled)