# US 10,245,240 B2 · Treatment of prostate carcinoma

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- Number: US 10,245,240 B2
- Document ID: US10245240B2
- Status: Granted
- Kind: B2
- Application number: 16/015,105
- Filed: 2018-06-21
- Published: 2018-10-18
- Granted: 2019-04-02
- Earliest claimed: 2010-08-04
- Assignees: Pellficure Pharmaceuticals, Inc.
- Applicants: Pellficure Pharmaceuticals, Inc.
- Inventors: Per Borgström
- Web page: https://patentgrep.com/patent/US10245240B2

## CPC

- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K 31/05: Phenols {(cannabinoids A61K31/658)}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/277: having a ring, e.g. verapamil
- A61K 31/4166: having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/565: not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 31/6615: Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
- A61K 38/09: Luteinising hormone-releasing hormone [LHRH] {, i.e. Gonadotropin-releasing hormone [GnRH]}; Related peptides
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 5/28: Antiandrogens
- A61P 13/08: of the prostate
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- G01N 33/5011: {for testing antineoplastic activity}
- G01N 33/5088: {of vertebrates}
- 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
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

Disclosed herein are naphthoquinone analogs, such as plumbagin, pharmaceutical compositions that include naphthoquinone analogs, such as plumbagin, and methods of treating diseases and/or conditions such as cancer with naphthoquinone analogs, such as plumbagin. Also included are combination therapies wherein a naphthoquinone analog, such as plumbagin, and a hormone therapy agent are provided to a subject suffering from a condition such as cancer.

## Claims

### Claim 1

A method of inhibiting or delaying the growth of prostate cancer, comprising administering to a human having prostate cancer a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt of Formula (I):
wherein:
R1 is methyl;
R2 is hydrogen;
R3 is —OH;
R4 is hydrogen;
R5 is hydrogen;
R6 is hydrogen; and
wherein the compound of Formula (I) is administered to the human in combination with, subsequent to, or concomitantly with, an androgen deprivation therapy that reduces production of dihydrotestosterone (DHT), androsterone, androstenediol, androstenedione, dehydroepiandrosterone (DHEA), or dehydroepiandrosterone sulfate (DHEA-S); and wherein the growth of prostate cancer is inhibited or delayed.

### Claim 2 (depends on 1)

The method of claim 1, wherein the androgen deprivation therapy decreases the DHT in the human.

### Claim 3 (depends on 1)

The method of claim 1, wherein the androgen deprivation therapy blocks the production of DHT.

### Claim 4 (depends on 1)

The method of claim 1, wherein the androgen deprivation therapy is administration of finasteride.

### Claim 5 (depends on 1)

The method of claim 1, wherein said method inhibits the growth of prostate cancer.

### Claim 6 (depends on 1)

The method of claim 1, wherein said method inhibits or delays the onset of castration-resistant prostate cancer.

### Claim 7 (depends on 1)

The method of claim 1, wherein the compound of Formula (I) is administered to the human orally.

### Claim 8 (depends on 1)

The method of claim 1, wherein the androgen deprivation therapy is administered to the human orally.

### Claim 9 (depends on 1)

The method of claim 1, wherein the compound of Formula (I) and the androgen deprivation therapy are administered to the human orally.

### Claim 10 (depends on 1)

The method of claim 1, wherein said prostate cancer is androgen dependent prostate cancer.

### Claim 11 (depends on 1)

The method of claim 1, wherein said prostate cancer is castration-resistant prostate cancer.

### Claim 12 (depends on 1)

The method of claim 1, wherein the method results in a decrease in prostate cancer tumor size.