Methods for treating post traumatic stress disorder
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Publication Number
US-9987265-B2
Publication Date
2018-06-05
Expiration Date
Abstract
Compounds and compositions are described herein for treating post traumatic stress disorder.
Core Innovation
The invention relates to vasopressin V1a-selective antagonists as therapeutic agents. The disclosed approach treats a patient having intermittent explosive disorder by administering a therapeutically effective amount of one or more compounds of a defined formula and/or salts thereof.
The compound definition specifies A as a carboxylic acid, an ester, or an amide; and specifies B as a carboxylic acid, an ester, or an amide, or B as an alcohol or thiol or a derivative thereof. Additional substituent definitions include R1 as hydrogen or C1-C6 alkyl; R2 as hydrogen or multiple substituted or unsubstituted categories including alkyl, alkenyl, alkynyl, alkoxy, alkylthio, halo, haloalkyl, cyano, formyl, alkylcarbonyl, and substituents selected from —CO2R8, —CONR8R8′, and —NR8(COR9); and R3 and R4 selected from multiple nitrogen-containing or carbon substituent classes.
The invention additionally positions the compounds as V1a receptor-selective and includes human V1a receptor competitive binding assay data and receptor selectivity data for illustrative compounds. The method further applies to a patient who also has one or more specified mental health disorders, including impulse control or anger disorders, general or related anxiety disorders, depression disorders, or a combination thereof.
Claims Coverage
The independent claim is directed to treating intermittent explosive disorder by administering a therapeutically effective amount of one or more compounds of a defined formula, or salts thereof. The claim set includes broad structural features based on A, B, and R1-R4 substituent definitions, with dependent refinements that add V1a selectivity and narrow the structural scope. The inventive features are concentrated in the treatment method, the V1a receptor-selective compound, and the additional structural limitations.
Treating intermittent explosive disorder with formula compounds or salts
A method for treating a patient having intermittent explosive disorder by administering a therapeutically effective amount of one or more compounds of the formula or salts thereof, with A and B and substituent variables R1-R4 defined by extensive substituent classes.
V1a receptor selectivity
The method is characterized by using a compound that is selective for the V1a receptor.
Additional psychiatric comorbidities
The method further applies to a patient who also has one or more specified mental health disorders, including impulse control or anger disorders, general or related anxiety disorders, depression disorders, or a combination thereof.
Constraining structural variable n
Further limitations include that n is 1 or 2.
Constraining structural variable Q to oxygen or sulfur
A structural limitation specifies that Q is oxygen or sulfur.
The claim coverage centers on a treatment method for intermittent explosive disorder using therapeutically effective amounts of broadly defined formula compounds or salts, with V1a receptor selectivity as a key pharmacological constraint. Provided refinements narrow structural scope via parameters such as n and Q, and expand patient eligibility to selected comorbid mental health disorder categories.
Stated Advantages
Provides treatment for a patient having intermittent explosive disorder.
Uses a compound that is selective for the V1a receptor.
CNS/BBB penetration is stated as a potential advantage.
V1a selectivity versus V1b/V2 is stated as an advantage.
Safety/performance advantages are stated, including receptor panel inactivity.
Reduced behavioral effects on sexual behavior are stated.
Context-dependent fear recall effects are stated.
Dosing compatibility is stated (e.g., b.i.d. or q.d.).
Documented Applications
Treatment of a patient having intermittent explosive disorder by administering therapeutically effective amounts of formula compounds or salts thereof.
Patients who also have one or more specified mental health disorders, including impulse control or anger disorders, general or related anxiety disorders, depression disorders, or combinations thereof.
Treating a patient having intermittent explosive disorder using vasopressin V1a-selective antagonist compounds.
Treating a patient having intermittent explosive disorder with additional mental health disorders including impulse control or anger disorders, general or related anxiety disorders, depression disorders, or a combination thereof.
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