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US 12,252,457 B2Granted
Compositions and methods for reducing tactile dysfunction, anxiety, and social impairment
AssigneePresident and Fellows of Harvard College
InventorsDavid D. Ginty, Lauren L. Orefice, Jinbo Lee
Life of this patent
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Abstract
The present invention features novel peripherally-restricted isoguvacine analogs with reduced blood brain barrier permeability and methods of use thereof for reducing tactile dysfunction, social impairment, and anxiety in a subject diagnosed with Autism Spectrum Disorder, Rett syndrome, Phelan McDermid syndrome, or Fragile X syndrome.
Claims22
A compound having the structure of Formula (I):
- wherein
- n=1, 2, 3, 4, 5, 6, 7, or 8;
- each of R1 and R2 is, independently, hydrogen, deuterium, optionally substituted C1-6 alkyl, or optionally substituted C3-6 cycloalkyl wherein R1 and R2 are covalently linked;
- each R4 is, independently, hydrogen, deuterium, halogen, optionally substituted C1-4 alkoxy, optionally substituted C1-6 alkyl, CF3, CH3S, CH3SO2, or NO2;
- and
- A is a carboxylic acid, or has the structure of:
- or a pharmaceutically acceptable salt thereof
- wherein when A is a carboxylic acid, and each occurrence of R4 is hydrogen, at least one of R1 and R2 is not hydrogen.
5 more elements
A compound of the structure 5a:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.