# US 10,766,905 B2 · [1,2,4]triazolo[4,3-B]pyridazines for use in the treatment of proliferative diseases

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- Number: US 10,766,905 B2
- Document ID: US10766905B2
- Status: Granted
- Kind: B2
- Application number: 16/528,738
- Filed: 2019-08-01
- Published: 2020-02-20
- Granted: 2020-09-08
- Earliest claimed: 2014-07-28
- Assignees: AstraZeneca AB
- Applicants: AstraZeneca AB
- Inventors: Robert Hugh Bradbury; Alfred Arthur Rabow; Michael James Waring; James Francis McCabe; Steven Christopher Glossop; Arshed Mahmood; Zoe Ann Cotter
- Web page: https://patentgrep.com/patent/US10766905B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- E21B 7/06: Deflecting the direction of boreholes
- E21B 7/062: {the tool shaft rotating inside a non-rotating guide travelling with the shaft (E21B7/067 and E21B7/068 take precedence)}
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- E21B: EARTH OR ROCK DRILLING; OBTAINING OIL, GAS, WATER, SOLUBLE OR MELTABLE MATERIALS OR A SLURRY OF MINERALS FROM WELLS
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.

## Claims

### Claim 1

A method of treating cancer in a human in need thereof, comprising administering to the human an effective amount of (R)-4-(2-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-one or a pharmaceutically acceptable salt thereof, wherein the cancer is selected from ovarian cancer, multiple myeloma (MM), and diffuse large B-cell lymphoma (DLBCL).

### Claim 2 (depends on 1)

The method of claim 1, wherein the cancer is ovarian cancer.

### Claim 3 (depends on 1)

The method of claim 1, wherein the cancer is multiple myeloma (MM).

### Claim 4

A method of treating cancer in a human in need thereof, comprising administering to the human an effective amount of a co-crystal of (R)-4-(2-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-1,3-dimethylpiperazin-2-one and the co-former molecule 6-hydroxy-2-naphthoic acid, wherein the cancer is selected from ovarian cancer, multiple myeloma (MM), and diffuse large B-cell lymphoma (DLBCL).

### Claim 5 (depends on 4)

The method of claim 4, wherein the cancer is ovarian cancer.

### Claim 6 (depends on 4)

The method of claim 4, wherein the cancer is multiple myeloma (MM).

### Claim 7 (depends on 1)

The method of claim 1, wherein the cancer is diffuse large B-cell lymphoma (DLBCL).

### Claim 8 (depends on 4)

The method of claim 4, wherein the cancer is diffuse large B-cell lymphoma (DLBCL).