# US 8,772,318 B2 · Methods and compositions related to targeting monoacylglycerol lipase

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- Number: US 8,772,318 B2
- Document ID: US8772318B2
- Status: Granted
- Kind: B2
- Application number: 12/998,642
- Filed: 2009-11-10
- Published: 2011-11-10
- Granted: 2014-07-08
- Earliest claimed: 2008-11-14
- Assignees: The Scripps Research Institute
- Applicants: Benjamin F. Cravatt; Jonathan Z. Long; Weiwei Li; Daniel K. Nomura
- Inventors: Benjamin F. Cravatt; Jonathan Z. Long; Weiwei Li; Daniel K. Nomura
- Web page: https://patentgrep.com/patent/US8772318B2

## CPC

- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 23/00: Anaesthetics
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- 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 27/06: Antiglaucoma agents or miotics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C12N 15/1137: {against enzymes (viral enzymes C12N15/1131; receptors C12N15/1138)}
- C12N 2310/14: interfering nucleic acids [NA]
- C12N 2310/531: Stem-loop; Hairpin
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.

## Claims

### Claim 1

A compound of formula I shown below:
wherein X is CH, R1 is H or OH, and R2 and R3 each have the structure

### Claim 2 (depends on 1)

The compound of claim 1, wherein X is CH, R1 is OH, and R2 and R3 each have the structure shown below

### Claim 3 (depends on 1)

A method for inhibiting growth of an aggressive tumor cell, comprising contacting the cell with a therapeutically effective amount of a compound of claim 1, thereby inhibiting growth of the tumor cell.

### Claim 4 (depends on 3)

The method of claim 3, wherein X is CH, R1 is OH, and R2 and R3 each have the structure shown below