# US 8,785,502 B2 · Compositions and methods relating to proliferative diseases

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- Number: US 8,785,502 B2
- Document ID: US8785502B2
- Status: Granted
- Kind: B2
- Application number: 13/312,682
- Filed: 2011-12-06
- Published: 2012-06-07
- Granted: 2014-07-22
- Earliest claimed: 2010-12-06
- Assignees: The Penn State Research Foundation
- Applicants: Gavin P. Robertson; Chandagalu D. Raghavendragowda; SubbaRao V. Madhunapantula; Omer F. Kuzu; Gajanan S. Inamdar
- Inventors: Gavin P. Robertson; Chandagalu D. Raghavendragowda; SubbaRao V. Madhunapantula; Omer F. Kuzu; Gajanan S. Inamdar
- Web page: https://patentgrep.com/patent/US8785502B2

## CPC

- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 31/136: having the amino group directly attached to the aromatic ring, e.g. benzeneamine
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 31/17: having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine (isoureas, isothioureas A61K31/155; sulfonylureas A61K31/64)
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 31/195: having an amino group
- A61K 31/215: of carboxylic acids
- A61K 31/26: Cyanate or isocyanate esters; Thiocyanate or isothiocyanate esters
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- C07C 61/29: having a carboxyl group bound to a condensed ring system
- C07C 211/31: the six-membered aromatic ring being part of a condensed ring system formed by at least three rings
- C07C 229/38: having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
- C07C 265/08: the carbon skeleton containing rings
- C07C 275/24: containing six-membered aromatic rings
- C07C 279/04: having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
- C07C 331/24: the carbon skeleton containing six-membered aromatic rings
- C07C 335/02: Thiourea
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.

## Claims

### Claim 1

An anti-cancer pharmaceutical composition, comprising: liposome encapsulated leelamine, wherein the liposomes comprise L-alpha-phosphatidylcholine and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000 in an 80:20 mol % ratio and wherein the liposomes have a net neutral surface charge at physiological pH.

### Claim 2 (depends on 1)

A method of treating a subject having cancer, comprising:
administering a therapeutically effective amount of the anti-cancer pharmaceutical composition of claim 1 to the subject.

### Claim 3 (depends on 2)

The method of claim 2, wherein the anti-cancer pharmaceutical composition is effective to preferentially inhibit the PI3K, MAPK and STAT pathways in a cancer cell compared to a non-cancer cell.

### Claim 4 (depends on 2)

The method of claim 2, wherein the subject is human.

### Claim 5 (depends on 2)

The method of claim 2, further comprising administration of an adjunct anti-cancer treatment.