IP Library › Granted Patent US 11,214,548
Granted Patent B2
US 11,214,548 · App. 16/580,697 · Granted Jan 4, 2022

Cannabinoid receptor modulators

Inventors: Robert M. Jones (San Diego, CA); Sangdon Han (San Diego, CA); Lars Thoresen (San Diego, CA); Jae-Kyu Jung (San Diego, CA); Sonja Strah-Pleynet (Newton, MA); Xiuwen Zhu (San Diego, CA); Yifeng Xiong (San Diego, CA); Dawei Yue (San Diego, CA)
Assignee: Arena Pharmaceuticals, Inc.
C07D231/54C07D401/04C07D401/12C07D401/14C07D403/04C07D403/12C07D405/14C07D413/12C07D413/14C07F9/65583
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Quick Facts
Patent No.
US 11,214,548
App. No.
16/580,697
Granted
Jan 4, 2022
Kind
B2
Abstract

The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

Claims (8)

1. A compound selected from (1aS,5aS)-2-(4-Oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (2,2,2-trifluoro-1,1-dimethyl-ethyl)-amide (Compound 919) and pharmaceutically acceptable salts thereof.

2. A compound selected from (1aS,5aS)-2-(4-Oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (2,2,2-trifluoro-1,1-dimethyl-ethyl)-amide (Compound 919) and solvates thereof.

3. The compound (1aS,5aS)-2-(4-Oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (2,2,2-trifluoro-1,1-dimethyl-ethyl)-amide (Compound 919).

4. A pharmaceutically acceptable salt of (1aS,5aS)-2-(4-Oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (2,2,2-trifluoro-1,1-dimethyl-ethyl)-amide.

5. A solvate of (1aS,5aS)-2-(4-Oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (2,2,2-trifluoro-1,1-dimethyl-ethyl)-amide.

6. A pharmaceutical composition comprising a compound according to claim 3 and a pharmaceutically acceptable carrier.

7. A pharmaceutical composition comprising the compound according to claim 4 and a pharmaceutically acceptable carrier.

8. A pharmaceutical composition comprising a compound according to claim 5 and a pharmaceutically acceptable carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 17, 2019
From: JONES, ROBERT M.; HAN, SANGDON; THORESEN, LARS; JUNG, JAE-KYU; STRAH-PLEYNET, SONJA; ZHU, XIUWEN; XIONG, YIFENG; YUE, DAWEI
To: ARENA PHARMACEUTICALS, INC.
Reel/Frame 050746/0850 →
Continuity (7)
Continuation 15912700 · Mar 6, 2018
Division 13616918 · Sep 14, 2012
Division 13392074
Provisional Application 61400146 · Jul 22, 2010
Provisional Application 61396588 · May 28, 2010
Provisional Application 61275506 · Aug 28, 2009
Related Publication 20200017448A1 · Jan 16, 2020
Cited By (1)
US 12,201,633