# US 11,110,067 B2 · Inhibition of mammalian target of rapamycin

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- Number: US 11,110,067 B2
- Document ID: US11110067B2
- Status: Granted
- Kind: B2
- Application number: 16/552,380
- Filed: 2019-08-27
- Published: 2020-02-20
- Granted: 2021-09-07
- Earliest claimed: 2008-11-11
- Assignees: Board of Regents, The University of Texas System; Southwest Research Institute
- Applicants: The Board of Regents of the University of Texas System; Southwest Research Institute
- Inventors: Zelton Dave Sharp; John R. Strong; Veronica Galvan; Salvatore Oddo; Herbert G. Wheeler
- Web page: https://patentgrep.com/patent/US11110067B2

## CPC

- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/5026: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 35/00: Antineoplastic agents
- A61P 39/06: Free radical scavengers or antioxidants
- 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

Disclosed are microcapsules that include an inhibitor of the mammalian target of rapamycin (mTOR) within the microcapsules, and pharmaceutical compositions and kits that include the microcapsules. Also disclosed are methods for treating or preventing an age-related disease, condition, or disorder in a subject that involve administering to a subject a pharmaceutically effective amount of microcapsules that includes an inhibitor of mTOR within the microcapsules.

## Claims

### Claim 1

A microcapsule consisting essentially of a core component comprising at least 5% by weight of an inhibitor of mammalian target of rapamycin (mTOR) which is rapamycin or a rapamycin analog, wherein said core component is microencapsulated and encased in a coating that includes a methyl methacrylate-methacrylic acid copolymer.

### Claim 2 (depends on 1)

The microcapsule of claim 1, wherein the coating is Eudragit® S100.

### Claim 3 (depends on 1)

The microcapsule of claim 1, wherein the microcapsule comprises rapamycin.

### Claim 4 (depends on 1)

The microcapsule of claim 1, wherein the microcapsule comprises an analog of rapamycin that is everolimus, tacrolimus, CCI-779, ABT-578, AP-23675, AP-23573, AP23841, 7-epi-rapamycin, 7-thiomethyl-rapamycin, 7-epi-trimethoxyphenyl-rapamycin, 7-epithiomethyl-rapamycin, 7-demethoxy-rapamycin, 32-demethoxy-rapamycin, 2-desmethylrapamycin, or 42-0-(2-hydroxy)ethyl rapamycin.

### Claim 5 (depends on 1)

The microcapsule of claim 1, wherein the core component further comprises a second compound that is vitamin E, vitamin A, an antibacterial antibiotic, an antioxidant, L-carnitine, lipoic acid, metformine, resveratrol, leptine, a non-steroid anti-inflammatory drug, or a COX inhibitor.

### Claim 6

A kit comprising a first sealed container comprising a microcapsule, wherein the microcapsule is comprised of a core component comprising at least 5% by weight of an inhibitor of mammalian target of rapamycin (mTOR) which is rapamycin or a rapamycin analog, wherein said core component is microencapsulated and encased in a coating that includes a methyl methacrylate-methacrylic acid copolymer.

### Claim 7 (depends on 1)

A pharmaceutical or nutraceutical composition comprising a microcapsule as defined in claim 1 for treating or preventing cancer in a mammalian subject, wherein the lifespan expectancy of the mammalian subject is prolonged.