# US 11,028,055 B2 · Compounds for treating proliferative diseases

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 11,028,055 B2
- Document ID: US11028055B2
- Status: Granted
- Kind: B2
- Application number: 15/779,685
- Filed: 2016-11-30
- Published: 2020-06-25
- Granted: 2021-06-08
- Earliest claimed: 2015-11-30
- Assignees: Children's Medical Center Corporation; Beth Israel Deaconess Medical Center, Inc.
- Applicants: Children's Medical Center Corporation; Beth Israel Deaconess Medical Center, Inc.
- Inventors: Bruce R. Zetter; Lijun Sun
- Web page: https://patentgrep.com/patent/US11028055B2

## CPC

- C07D 235/32: Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
- A61K 31/4184: condensed with carbocyclic rings, e.g. benzimidazoles
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61P 35/00: Antineoplastic agents
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 401/14: containing three or more hetero rings
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- 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

The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

## Claims

### Claim 1

A compound of Formula (I):
or a pharmaceutically acceptable salt thereof, wherein:
R1 is substituted or unsubstituted alkyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl;
R2 is of the formula
RA2 is —N(RC)2, and each instance of RC is independently substituted or unsubstituted alkyl, or substituted or unsubstituted heterocyclyl;
RA3 is —N(RA4)2, and two instances of RA4 are joined to form a substituted or unsubstituted, heteroaryl ring;
RA6 is —N(RA7)2, and two instances of RA7 are joined to form a substituted or unsubstituted, heterocyclic ring, or substituted or unsubstituted, heteroaryl ring;
R3 is independently hydrogen, substituted or unsubstituted C1-6 alkyl, or a nitrogen protecting group; and
R4 is independently hydrogen, substituted or unsubstituted C1-6 alkyl, or a nitrogen protecting group.

### Claim 2 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R1 is of the formula:

### Claim 3 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R1 is substituted or unsubstituted C1-6 alkyl.

### Claim 4 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R1 is of the formula:
wherein:
each instance of RA1 is independently substituted or unsubstituted C1-6 alkyl; and
a is 1, 2, or 3.

### Claim 5 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R1 is —CH2CH2N(CH3)2 or —CH2CH2CH2N(CH3)2.

### Claim 6 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R2 is of the formula:
wherein:
RA2 is independently —N(RC)2; and
each instance of RC is independently substituted or unsubstituted alkyl, or substituted or unsubstituted heterocyclyl.

### Claim 7 (depends on 6)

The compound of claim 6, or a pharmaceutically acceptable salt thereof, wherein RA2 is of the formula:

### Claim 8 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R2 is of the formula:
wherein:
RA6 is —N(RA7)2, and
two instances of RA7 are joined to form a substituted or unsubstituted, heterocyclic ring, or substituted or unsubstituted, heteroaryl ring.

### Claim 9 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R2 is of the formula:
wherein:
RA3 is —N(RA4)2, and
two instances of RA4 are joined to form a substituted or unsubstituted, heteroaryl ring.

### Claim 10 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen.

### Claim 11 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen.

### Claim 12 (depends on 1)

The compound of claim 1, wherein the compound is of the formula:
or a pharmaceutically acceptable salt thereof.

### Claim 13 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt thereof, and optionally a pharmaceutically acceptable excipient.

### Claim 14 (depends on 1)

A kit comprising:
a compound of claim 1, a pharmaceutically acceptable salt thereof; and
instructions for using the compound.

### Claim 15 (depends on 1)

The compound of claim 1, wherein each instance of RC is different from one other.

### Claim 16 (depends on 1)

The compound of claim 1, wherein at least one instance of RC is substituted or unsubstituted heterocyclyl.

### Claim 17

A compound of the formula:
or a pharmaceutically acceptable salt thereof.

### Claim 18

A compound of the formula:
or a pharmaceutically acceptable salt thereof.