Granted Patent
B2
US 12,246,012 · App. 18/125,612 · Granted Mar 11, 2025
Method for treating nervous system injuries using boldine and derivatives thereof
Inventors:
Christopher Cardozo (Bronx, NY); Carlos A. Toro Chacon (Bronx, NY); Zachary Graham (Birmingham, AL); Wei Zhao (Bronx, NY); Juan C. Saez (Vina del Mar, CL)
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Abstract
Provided are methods of treating an injury to the nervous system in a subject comprising administering to the subject an effective amount of boldine, a boldine analog, or a pharmaceutically-acceptable salt thereof. Also provided are methods of improving voluntary muscle control and methods of treating neuropathic pain in a subject having an injury to the nervous system. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Claims (14)
1. A method of improving voluntary muscle control in a subject having an injury to the nervous system, comprising administering to the subject an effective amount of a compound represented by the formula:
wherein R 1 is selected from hydrogen and C1-C4 alkyl;
wherein R 2 is selected from hydrogen, halogen, —CN, —NH 2 , —OH, —NO 2 , C1-C4 alkyl, C2-C4 alkenyl, C1-C4 haloalkyl, C1-C4 cyanoalkyl, C1-C4 hydroxyalkyl, C1-C4 haloalkoxy, C1-C4 alkoxy, C1-C4 alkylamino, (C1-C4)(C1-C4) dialkylamino, and C1-C4 aminoalkyl;
wherein each of R 3 and R 4 is independently selected from hydrogen, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 haloalkyl, C1-C4 cyanoalkyl, C1-C4 hydroxyalkyl, C1-C4 haloalkoxy, C1-C4 alkoxy, C1-C4 alkylamino, (C1-C4)(C1-C4) dialkylamino, and C1-C4 aminoalkyl; or wherein R 3 and R 4 join together to form a ring having 5-7 atoms;
wherein each of R 5 and R 6 is independently selected from hydrogen, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 haloalkyl, C1-C4 cyanoalkyl, C1-C4 hydroxyalkyl, C1-C4 haloalkoxy, C1-C4 alkoxy, C1-C4 alkylamino, (C1-C4)(C1-C4) dialkylamino, and C1-C4 aminoalkyl; or wherein R 5 and R 6 join together to form a ring having 5-7 atoms; and
wherein R 7 is selected from hydrogen, halogen, —CN, —NH 2 , —OH, —NO 2 , C1-C4 alkyl, C2-C4 alkenyl, C1-C4 haloalkyl, C1-C4 cyanoalkyl, C1-C4 hydroxyalkyl, C1-C4 haloalkoxy, C1-C4 alkoxy, C1-C4 alkylamino, (C1-C4)(C1-C4) dialkylamino, and C1-C4 aminoalkyl;
or a pharmaceutically acceptable salt thereof, thereby improving voluntary muscle control in the subject.
2. The method of claim 1 , wherein each of R 1 , R 4 , and R 5 is independently selected from hydrogen, methyl, ethyl, and propyl; wherein each of R 2 and R 7 is independently selected from hydrogen and halogen; and wherein each of R 3 and R 6 is hydrogen.
3. The method of claim 1 , wherein each of R 1 , R 4 , and R 5 is methyl; wherein each of R 2 and R 7 is independently selected from hydrogen and halogen; and wherein each of R 3 and R 6 is hydrogen.
4. The method of claim 1 , wherein each of R 1 , R 4 , and R 5 is independently selected from hydrogen, methyl, ethyl, and propyl; and wherein each of R 2 , R 3 , R 6 , and R 7 is hydrogen.
5. The method of claim 1 , wherein the compound is represented by the formula:
6. The method of claim 1 , wherein the injury to the nervous system is a spinal cord injury (SCI), spinal cord contusion, nerve crush injury, or traumatic brain injury (TBI).
7. The method of claim 1 , wherein a symptom of the injury to the nervous system is neuropathic pain.
8. The method of claim 1 , wherein improving voluntary muscle control comprises improving locomotor function.
Continuity (4)
Provisional Application
63043572
· Jun 24, 2020
Provisional Application
62971757
· Feb 7, 2020
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