# US 12,215,112 B2 · CD151 inhibitors

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- Number: US 12,215,112 B2
- Document ID: US12215112B2
- Status: Granted
- Kind: B2
- Application number: 18/006,978
- Filed: 2021-07-27
- Published: 2023-11-16
- Granted: 2025-02-04
- Earliest claimed: 2020-07-27
- Assignees: Esfam Biotech Pty Ltd
- Applicants: Esfam Biotech Pty Ltd
- Inventors: John Thomas Feutrill; Jean-Marc Garnier; Albert George Frauman
- Web page: https://patentgrep.com/patent/US12215112B2

## CPC

- A61P 35/00: Antineoplastic agents
- C07D 487/04: Ortho-condensed systems
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention relates to compounds of formula (I) that have the ability to inhibit CD151.

## Claims

### Claim 1

A compound of Formula (I):
Formula (I)
wherein
R1, R2, and R3 are each independently selected from the group consisting of H and C1-C12alkyl,
R4 is selected from the group consisting of H and C1-C12alkyl,
R5 is selected from the group consisting of H, optionally substituted C6-C18aryl, optionally substituted C1-C18heteroaryl, optionally substituted C6-C18arylC1-C12alkyl-, and optionally substituted C1-C18heteroarylC1-C12alkyl-;
R6 is selected from the group consisting of H, C1-C12alkyl, C3-C6 cycloalkyl, and C1-C5 heterocycloalkyl,
R7 is selected from the group consisting of H and C1-C12alkyl;
R8 is selected from the group consisting of H, C1-C12alkyl, optionally substituted C6-C18aryl, optionally substituted C1-C18heteroaryl, optionally substituted C6-C18arylC1-C12alkyl-, and optionally substituted C1-C18heteroarylC1-C12alkyl-;
or R7 and R8 when taken together with the nitrogen atom to which they are attached form an optionally substituted C2-C12heterocyclic group;
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A compound according to claim 1, wherein R1 and R3 are H.

### Claim 3 (depends on 1)

A compound according to claim 1, wherein R2 is H.

### Claim 4 (depends on 1)

A compound according to claim 1, wherein R4 is H.

### Claim 5 (depends on 1)

A compound according to claim 1, wherein R5 is optionally substituted C6-C18aryl.

### Claim 6 (depends on 1)

A compound according to claim 1, wherein R5 is optionally substituted phenyl.

### Claim 7 (depends on 1)

A compound according to claim 1, wherein R6 is C1-C12alkyl.

### Claim 8 (depends on 1)

A compound according to claim 1, wherein R6 is isopropyl or tert-butyl.

### Claim 9 (depends on 1)

A compound according to claim 1, wherein R7 and R8 when taken together with the nitrogen atom to which they are attached form an optionally substituted C2-C12heterocyclic group.

### Claim 10 (depends on 9)

A compound according to claim 9, wherein the C2-C12heterocyclic group is a group of the formula:
wherein RD is independently selected from the group consisting of H, halogen, OH, NO2, CN, SH, NH2, CF3, OCF3, optionally substituted C1-C12alkyl, optionally substituted C1-C12haloalkyl, optionally substituted C2-C12alkenyl, optionally substituted C2-C12alkynyl, optionally substituted C2-C12heteroalkyl, optionally substituted C3-C12cycloalkyl, optionally substituted C3-C12cycloalkenyl, optionally substituted C2-C12heterocycloalkyl, optionally substituted C2-C12heterocycloalkenyl, optionally substituted C6-C18aryl, optionally substituted C1-C18heteroaryl, optionally substituted C1-C12alkyloxy, optionally substituted C2-C12alkenyloxy, optionally substituted C2-C12alkynyloxy, optionally substituted C2-C10heteroalkyloxy, optionally substituted C3-C12cycloalkyloxy, optionally substituted C3-C12cycloalkenyloxy, optionally substituted C2-C12heterocycloalkyloxy, optionally substituted C2-C12heterocycloalkenyloxy, optionally substituted C6-C18aryloxy, optionally substituted C1-C18heteroaryloxy, optionally substituted C1-C12alkylamino, SR9, SO3H, SO2NR9R10, SO2R9, SONR9R10, SOR9, COR9, COOH, COOR9, CONR9R10, NR9COR10, NR9COOR10, NR9SO2R10, NR9CONR9R10, NR9R10, and acyl,
and wherein each R9 and R10 are independently selected from the group consisting of H and C1-C12alkyl.

### Claim 11 (depends on 1)

A compound according to claim 1, selected from the group consisting of:
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or a pharmaceutically acceptable salt thereof.

### Claim 12 (depends on 1)

A pharmaceutical composition comprising a compound according to claim 1, and a pharmaceutically acceptable diluent, excipient, or carrier.

### Claim 13 (depends on 1)

A compound according to claim 1, wherein the compound is selected from the group consisting of:
and
or a pharmaceutically acceptable salt thereof.

### Claim 14 (depends on 1)

A compound according to claim 1, wherein the compound is:
or a pharmaceutically acceptable salt thereof.

### Claim 15 (depends on 1)

A compound according to claim 1, wherein the compound is:
or a pharmaceutically acceptable salt thereof.

### Claim 16 (depends on 1)

A compound according to claim 1, wherein the compound is:
or a pharmaceutically acceptable salt thereof.

### Claim 17 (depends on 1)

A compound according to claim 1, wherein the compound is:
or a pharmaceutically acceptable salt thereof.

### Claim 18 (depends on 1)

A compound according to claim 1, wherein the compound is:
or a pharmaceutically acceptable salt thereof.

### Claim 19 (depends on 1)

A compound according to claim 1, wherein the compound is:
or a pharmaceutically acceptable salt thereof.
