# US 10,765,665 B2 · Composition comprising combination of rapamycin and an activator of AMP kinase and use thereof for treating diseases

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- Number: US 10,765,665 B2
- Document ID: US10765665B2
- Status: Granted
- Kind: B2
- Application number: 15/241,312
- Filed: 2016-08-19
- Published: 2017-05-25
- Granted: 2020-09-08
- Earliest claimed: 2015-11-24
- Applicants: Jeffrey Melin
- Inventors: Jeffrey M. Melin
- Web page: https://patentgrep.com/patent/US10765665B2

## CPC

- A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/0087: {Galenical forms not covered by A61K9/02 - A61K9/7023}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- 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 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61P 17/00: Drugs for dermatological disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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

A formulation, especially one that is topically administered, comprising a combination of rapamcycin and metformin in a molar ratio of about 20:1, 10:1, 5:1, 4:1, 3:1, or 1:1. The topical formulation may be a gel, an ointment, a cream or a lotion. The topical formulation may be used to treat any disease associated with inflammation and/or any inflammatory skin disease.

## Claims

### Claim 1

A method for treating symptoms of inflammatory arthritis in a subject, wherein the method comprises locally administering an effective amount of a topical formulation directly over an inflamed joint affected by inflammatory arthritis, the topical formulation comprising a combination of rapamycin and metformin, wherein the molar ratio of rapamycin to metformin is in the range of about 20:1 to about 1:1, and wherein metformin acts as an adjuvant to enhance efficacy of rapamycin in the topical formulation.

### Claim 2 (depends on 1)

The method of claim 1, wherein the molar ratio of rapamycin to metformin is in the range of about 15:1 to about 3:1.

### Claim 3 (depends on 1)

The method of claim 1, wherein the molar ratio of rapamycin to metformin is in the range of about 10:1 to about 4:1.

### Claim 4 (depends on 1)

The method of claim 1, wherein the molar ratio of rapamycin to metformin is about 5:1 to about 3:1.

### Claim 5 (depends on 1)

The method of claim 1, wherein the molar ratio of rapamycin to metformin is about 5:1 to about 4:1.

### Claim 6 (depends on 1)

The method of claim 1, wherein the inflammatory arthritis is osteoarthritis.

### Claim 7

A method for treating the symptoms of inflammatory arthritis in a subject comprising administering an effective amount of a formulation comprising a combination of rapamycin and metformin to a subject with inflammatory arthritis, wherein the molar ratio of rapamycin to metformin is in the range of about 20:1 to about 1:1.

### Claim 8 (depends on 7)

The method of claim 7, wherein the molar ratio of rapamycin to metformin is in the range of about 15:1 to about 3:1.

### Claim 9 (depends on 7)

The method of claim 7, wherein the molar ratio of rapamycin to metformin is in the range of about 10:1 to about 4:1.

### Claim 10 (depends on 7)

The method of claim 7, wherein the molar ratio of rapamycin to metformin is about 5:1 to about 3:1.

### Claim 11 (depends on 7)

The method of claim 7, wherein the ratio of rapamycin to metformin is about 5:1 to about 4:1.

### Claim 12 (depends on 7)

The method of claim 7, wherein the inflammatory arthritis is osteoarthritis.

### Claim 13 (depends on 7)

The method of claim 7, wherein the formulation is administered orally.

### Claim 14 (depends on 7)

The method of claim 7, wherein the formulation is administered topically.