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Cannabinoid Receptor Meditating Compounds for Metabolic Disease

19:00 EST 10 Dec 2014 | NIH

There is evidence that the metabolic effects of endocannabinoids are mediated by CB1 receptors in peripheral tissues. While prior attempts at generating CB1 receptor blockers have had serious neuropsychiatric side effects, inventors at NIH have discovered compounds that block CB1 receptors with reduced brain penetrance. In addition, some of these compounds also have a direct inhibitory effect on inducible nitric oxide synthase (iNOS), whereas another group of the compounds directly activates AMP kinas. These dual-target compounds may be useful for treating metabolic disease and related conditions such as obesity and diabetes and their complications, including liver or kidney fibrosis, without the dangerous the side effects.

IC: 
NIAAA
NIH Ref. No.: 
E-140-2014/0
TAB No: 
TAB-2897
Advantages: 
  • Cannabinoid receptor blockers with reduced brain penetrance relative to older drugs of this class, also having secondary target for improved therapeutic efficacy.
Applications: 
  • Treatment of metabolic disease and related conditions such as diabetes, obesity and fibrotic disease.
Development Status: 

Early-stage

Provider Technology ID: 
2897
Updated On: 
Aug 23, 2017
Provider Classifications: 
Date Published: 
Thursday, December 11, 2014
Publications: 
Patent Application: 
15/309,728
61/991,333
PCT/US2015/029946
Patent Authority: 
US
US
PCT
Licensing Contacts: 
Lead Inventor: 
Inventor IC: 
NIAAA
NIAAA
NIAAA
NIDA
Inventor Lab URL: 
http://irp.nih.gov/pi/george-kunos
http://irp.nih.gov/pi/kenner-rice
LPM FIrst Name: 
Betty
LPM Last Name: 
Tong
LPM Address: 
12 South Drive, Building 12A, Room 3011
LPM City: 
Bethesda
Inv Is lead: 
LPM Zip: 
20892
LPM State: 
MD
LPM Phone: 
301-451-7836
LPM Suffix: 
Ph.D.
LPM Organization: 
NIH Office of Technology Transfer
DTDT Classification: 
Therapeutics
Other
Diabetes
Hyperlipidemia
Therapeutic (small molecule)
Early-stage
DTDT Description: 
Internal Medicine - Therapeutics
Internal Medicine - Therapeutics: Other
Diabetes
Hyperlipidemia
Therapeutic (small molecule)
Early-stage
Pat Filing Date: 
2016-11-08
2014-05-09
2015-05-08
Application Term: 
Disease Area Term: 
Development Stage Term: 
Collaboration Sought: 
Yes
Institute or Center: 
Related Patents: 
8,293,724
Related Patent Publish Date: 
1223614800
1192165200
1270530000
1350277200
1352786400
1384236000
1431406800
1372136400
1403586000
1450764000
1502341200
1502341200
Related Patent Application: 

PCT/US2008/011657

60/998,661

12/755,227

13/652,324

61/725,949

PCT/US2013/069686

14/442,383

61/839,239

PCT/US2014/043924

14/900,951

15/674,333

15/674,365

Related Patent Authority: 
PCT
US
US
US
US
PCT
US
US
PCT
US
US
US
Related Invention: 
E-211-2006/0
E-282-2012/0
E-103-2013/0
E Number Only: 
E-140-2014
Inventor First Name: 
George
Malliga
Resat
Kenner
Inventor Last Name: 
Kunos
Iyer
Cinar
Rice

Original Article: Cannabinoid Receptor Meditating Compounds for Metabolic Disease

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