US2022306586A1PendingUtilityA1

Cannabinoid receptor modulators

Assignee: ARENA PHARM INCPriority: Aug 28, 2009Filed: Nov 8, 2021Published: Sep 29, 2022
Est. expiryAug 28, 2029(~3.1 yrs left)· nominal 20-yr term from priority
C07D 401/04A61P 29/00A61K 31/4439C07D 405/14A61K 31/497C07D 401/14C07D 403/04A61K 31/416C07D 231/54A61P 19/02C07F 9/65583C07D 401/12C07D 413/12C07D 231/56C07D 403/12C07D 413/14
77
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Claims

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

exact text as granted — not AI-modified
1 - 56 . (canceled) 
     
     
         57 . A method for treating or preventing a disease in an individual in need thereof, wherein the disease is selected from Alzheimer's disease, stroke, dementia, amyotropic lateral sclerosis (ALS), multiple sclerosis (MS), Parkinson's disease, and a central nervous system (CNS) tumor, wherein the method comprises administering to the individual a therapeutically effective amount 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, or a pharmaceutically acceptable salt thereof. 
     
     
         58 . The method of  claim 57 , wherein the disease is Alzheimer's disease. 
     
     
         59 . The method of  claim 57 , wherein the disease is stroke. 
     
     
         60 . The method of  claim 57 , wherein the disease is dementia. 
     
     
         61 . The method of  claim 57 , wherein the disease is amyotropic lateral sclerosis (ALS). 
     
     
         62 . The method of  claim 57 , wherein the disease is multiple sclerosis (MS). 
     
     
         63 . The method of  claim 57 , wherein the disease is Parkinson's disease. 
     
     
         64 . The method of  claim 57 , wherein the disease is a central nervous system (CNS) tumor. 
     
     
         65 . A method for treating or preventing a disease in an individual in need thereof, wherein the disease is selected from Alzheimer's disease, stroke, dementia, amyotropic lateral sclerosis (ALS), multiple sclerosis (MS), Parkinson's disease, and a central nervous system (CNS) tumor, wherein the method comprises administering to the individual a pharmaceutical composition comprising (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, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. 
     
     
         66 . The method of  claim 65 , wherein the disease is Alzheimer's disease. 
     
     
         67 . The method of  claim 65 , wherein the disease is stroke. 
     
     
         68 . The method of  claim 65 , wherein the disease is dementia. 
     
     
         69 . The method of  claim 65 , wherein the disease is amyotropic lateral sclerosis (ALS). 
     
     
         70 . The method of  claim 65 , wherein the disease is multiple sclerosis (MS). 
     
     
         71 . The method of  claim 65 , wherein the disease is Parkinson's disease. 
     
     
         72 . The method of  claim 65 , wherein the disease is a central nervous system (CNS) tumor.

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