Vasopressin receptor antagonists and products and methods related thereto

Inventors

Jones, Robert M. • Urbano, Mariangela • Brandt, Gary • Hardick, David • Knight, Chris • Tierney, Jason

Assignees

Neumora Therapeutics Inc

Abstract

Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof: wherein A, B, G, R1, R1b, R1c, R2 and X are as defined herein.

Core Innovation

The invention relates to a method for treating an anxiety disorder by administering to a subject in need thereof an effective amount of a compound having a specified substituted structure, or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof. The compound structure is defined by enumerated substituent variables including X, R1, R1b, R1c, R2, R3, Q, R4, R5, R6, and an index n, each constrained to allowed chemical classes.

X is selected from halogen, lower alkyl, lower haloalkyl, lower alkoxy, or cyano. R1 is selected from hydrogen, lower alkyl-R6, haloalkyl, lower alkoxyalkyl, cycloalkyl-R6, alkyl-cycloalkyl-R6, aryl-R6, alkyl-aryl-R6, heterocyclyl-R6, alkyl-heterocyclyl-R6, lower haloalkyl, -alkyl-C(=O)R3, or -C(=O)R3, while R1b and R1c are independently hydrogen, lower alkyl, or spiroalkyl, with ring-forming relationships permitted for selected substituents.

R2 is selected from -Q-(R4)n, -S(=O)2R5, or -C(=O)R5, where Q is aryl or heteroaryl. R3 is selected from lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, cycloalkyl-R6, -O-cycloalkyl-R6, -O-heterocyclyl-R6, -NHR5, or -NR5R5, and each R4, R5, and R6 is independently selected from the enumerated substituent sets, with n being 0, 1, or 2.

Claims Coverage

The independent claim is a single method claim directed to treating an anxiety disorder by administering an effective amount of a compound defined by a substituted-structure specification. The coverage includes the compound variables X, R1/R1b/R1c, R2, R3, Q, R4, R5, R6, and n, and the claim also includes pharmaceutically acceptable isomers, racemates, hydrates, solvates, isotopes, or salts.

Overall, the claim coverage centers on treating an anxiety disorder by administering an effective amount of a compound defined by an enumerated substituted-structure framework, with permitted pharmaceutically acceptable forms and ring-forming relationships.

Stated Advantages

Documented Applications