# US 2021/0330670 A1 · Coumarin derivative for therapy or prophylaxis of a cell proliferative disorder

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- Number: US 2021/0330670 A1
- Document ID: US20210330670A1
- Status: Published application
- Kind: A1
- Application number: 16/764,242
- Filed: 2018-05-16
- Published: 2021-10-28
- Earliest claimed: 2017-11-16
- Assignees: The Institute of Cancer Research: Royal Cancer Hospital; The Royal Marsden NHS Foundation Trust
- Applicants: The Institute of Cancer Research: Royal Cancer Hospital; The Royal Marsden NHS Foundation Trust
- Inventors: Udai BANERJI
- Web page: https://patentgrep.com/patent/US20210330670A1

## CPC

- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/37: Coumarins, e.g. psoralen
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- 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 invention provides a medicament for the treatment or prevention of a cell proliferative disorder, the medicament comprising as an active ingredient a compound represented by formula or a pharmaceutically acceptable salt thereof, wherein the medicament is used in such a manner that: (a) said compound or salt is administered twice weekly for 3 weeks, (b) administration of said compound or salt is paused for the following 1 week, and (c) steps (a) and (b) are subsequently repeated at least once.

## Claims

### Claim at position 1

-17. (canceled)

### Claim 18

A method for the treatment or prevention of a cell proliferative disorder, the method comprising:
(a) administering a compound represented by formula (I):
or a pharmaceutically acceptable salt thereof twice weekly for 3 weeks,
(b) pausing administration of said compound or salt for the following 1 week, and
(c) subsequently repeating steps (a) and (b) at least once.

### Claim 19 (depends on 18)

The method according to claim 18, wherein a potassium salt of a compound represented by formula (I) is administered.

### Claim 20 (depends on 18)

The method according to claim 18, wherein the cell proliferative disorder is cancer.

### Claim 21 (depends on 18)

The method according to claim 18, wherein the cell proliferative disorder is a KRAS mutant cancer.

### Claim 22 (depends on 18)

The method according to claim 18, wherein the cell proliferative disorder is a solid cancer.

### Claim 23 (depends on 18)

The method according to claim 18, wherein the dose per administration in step (a) is 3.2 mg.

### Claim 24 (depends on 23)

The method according to claim 23, wherein the method comprises, prior to step (a):
(1) administering said compound or salt twice weekly at a dose of 3.2 mg per administration; or
(2)
(2a) administering said compound or salt twice weekly for 3 weeks at a dose of 4 mg per administration,
(2b) pausing administration of said compound or salt for the following 1 week, and
(2c) subsequently repeating steps (2a) and (2b) at least once.

### Claim 25 (depends on 24)

The method according to claim 24, wherein the method comprises, prior to step (1) or (2), administering said compound or salt twice weekly at a dose of 4 mg per administration.

### Claim 26 (depends on 18)

The method according to claim 18:
wherein the method comprises:
(A) first, administering said compound or salt twice weekly at a dose of 4 mg per administration,
(B1) next, administering said compound or salt twice weekly at a dose of 3.2 mg per administration, and
(C) then:
(Ca) administering said compound or salt twice weekly for 3 weeks at a dose of 3.2 mg per administration,
(Cb) pausing administration of said compound or salt for the following 1 week, and
(Cc) subsequently repeating steps (Ca) and (Cb) at least once; or
wherein the method comprises:
(A) first, administering said compound or salt twice weekly at a dose of 4 mg per administration, and
(B2) next:
(B2a) administering said compound or salt twice weekly for 3 weeks at a dose of 4 mg per administration,
(B2b) pausing administration of said compound or salt for the following 1 week, and
(B2c) subsequently repeating steps (B2a) and (B2b) at least once; or
wherein the method comprises:
(A) first, administering said compound or salt twice weekly at a dose of 4 mg per administration,
(B2) next:
(B2a) administering said compound or salt twice weekly for 3 weeks at a dose of 4 mg per administration,
(B2b) pausing administration of said compound or salt for the following 1 week, and
(B2c) subsequently repeating steps (B2a) and (B2b) at least once, and
(C) then:
(Ca) administering said compound or salt twice weekly for 3 weeks at a dose of 3.2 mg per administration,
(Cb) pausing administration of said compound or salt for the following 1 week, and
(Cc) subsequently repeating steps (Ca) and (Cb) at least once.

### Claim 27 (depends on 18)

The method according to claim 18, wherein the cell proliferative disorder is multiple myeloma.

### Claim 28 (depends on 27)

The method according to claim 27, wherein the dose per administration in step (a) is 4 mg.

### Claim 29 (depends on 27)

The method according to claim 27, wherein the cell proliferative disorder is an NRAS mutant cancer.

### Claim 30 (depends on 27)

The method according to claim 27, wherein said compound or salt is used in combination with dexamethasone, and wherein the method comprises administering said compound or salt before, simultaneously with or after administration of dexamethasone.

### Claim 31 (depends on 30)

The method according to claim 30, wherein dexamethasone is administered once weekly at a dose of 20 mg per administration.

### Claim 32 (depends on 18)

The method according to claim 18, wherein the administration of said compound or salt is oral administration.