Substituted phenyl sulfonyl phenyl triazole thiones and uses thereof

Inventors

Wrasidlo, Wolfgang J. • Stocking, Emily M. • Natala, Srinivasa Reddy • PRICE, Diana Luz

Assignees

Neuropore Therapies Inc

Abstract

The present disclosure relates to substituted phenyl sulfonyl phenyl triazole thiones, pharmaceutical compositions containing them, and methods of using them.

Core Innovation

The disclosure describes pharmaceutical compositions that include at least one compound of Formula (I), optionally as a pharmaceutically acceptable salt, together with a pharmaceutically acceptable excipient. Formula (I) is defined by substituents R1, R2, and R3, where each is independently hydrogen, hydroxy, halogen, optionally substituted C1-4 alkyl, optionally substituted C1-4 alkoxy, —CN, —C(O)Rx, —C(O)ORx, —S(O)2Rx, or —NRyRz, with Rx, Ry, and Rz further defined as H or optionally substituted C1-4 alkyl and with the option that Ry and Rz taken together with the nitrogen form an optionally substituted monocyclic heterocycloalkyl ring.

The composition excipient is selected from polymeric agent, CMC, HPC, HEC, HPMC, gelatin, gelatin hydrolysate, sucrose, dextrose, PVP, PEG, vinyl pyrrolidone copolymers, pregelatinized starch, sorbitol, glucose, Kollidon, and polyacrylates. The pharmaceutical composition can be provided in a spray dry dispersion (SDD) form.

The described chemical space includes substituted 2,4-dihydro-3H-1,2,4-triazole-3-thione derivatives within the Formula (I) framework, including Compound 1 described as 4-(4-((4-chloro-3-(trifluoromethyl)phenyl)sulfonyl)phenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione. Additional enumerated derivatives are described as substitutions of this scaffold, with specific substituent motifs on the phenylsulfonyl portion and on the aromatic system.

Claims Coverage

The claim coverage centers on one independent claim directed to a pharmaceutical composition comprising a Formula (I) compound, or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable excipient selected from a specified list. The claim set is further narrowed by specific Formula (I) substituent selections, specific excipients, and a spray dry dispersion formulation.

Overall, the claim coverage is directed to a pharmaceutical composition combining a Formula (I) compound, or a pharmaceutically acceptable salt, with a defined excipient selection. Additional claim refinements narrow the scaffold and excipients and include an SDD formulation.

Stated Advantages

Documented Applications