Inhibitors of cysteine proteases and methods of use thereof
Inventors
Arnold, Lee D. • Jennings, Andy • Keung, Walter
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-11174231-B1
Publication Date
2021-11-16
Expiration Date
Abstract
The disclosure provides compounds with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.
Core Innovation
The invention relates to compounds represented by structural representations shown as one of two or more drawing or structure options, together with pharmaceutically acceptable salts thereof. The disclosed subject matter includes multiple chemical structure depictions supporting broad compound families defined by shared scaffolds with amide, urea-like, heterocyclic, bicyclic, and polycyclic features, together with stereochemical variants and variable substituents.
The structures and examples include viral protease inhibitor compounds and related analogs with indole-2-carboxamide, benzimidazole-2-carboxamide, pyrrolidine, piperidine, azaspiro, cyclopropyl, bicyclic heteroaryl, and other heteroaromatic motifs. Variations explicitly shown include halogen, methoxy, fluorinated, cyano, sulfone, sulfonamide-like, and nitrile-containing substituents, with some embodiments described as carboxamides, carbamoyl/cyano derivatives, or late-stage analogs.
The disclosed material also includes multi-step synthetic sequences and characterization for representative compounds, including chiral separation, deprotection, coupling, and functional group conversion to nitrile-bearing derivatives. Across the provided content, the compound families are presented through named examples, structural depictions, and associated chemical structure files, while the claim scope remains centered on the represented compound and its pharmaceutically acceptable salts.
Claims Coverage
The consolidated claim coverage centers on compounds defined by structural representations and explicitly includes pharmaceutically acceptable salts. Across the input items, the number of inventive features identified in the independent claim is 2: the compound as represented by a structural depiction and the corresponding pharmaceutically acceptable salt form.
Compound represented by a structural representation
A compound represented by one of two or more drawing or structure options, covering the structurally depicted compound family.
Pharmaceutically acceptable salts
The compound is also claimed in the form of a pharmaceutically acceptable salt thereof.
The claims are broadly directed to structurally represented compound families and their pharmaceutically acceptable salts, without further claim refinements in the provided material.
Stated Advantages
Inhibits viral transmission, viral replication, viral protein expression, and viral release.
Provides methods for treating or ameliorating viral infections, including coronavirus infections such as SARS-CoV-2.
Enables pharmaceutical compositions and kit formats for administration via pharmaceutically acceptable carriers and different administration routes.
Documented Applications
Treatment or amelioration of viral infections, including coronavirus infections such as SARS-CoV-2.
Inhibition of viral transmission, viral replication, viral protein expression, and viral release.
Use in connection with respiratory disorders.
Use in connection with cathepsin-dependent conditions, including Cathepsin K.
Combination therapy with other antivirals and supportive therapies.
Viral protease inhibition against example targets including Cathepsin K, coronavirus Mpro, Caspase 3, Calpain 1, and Cathepsin S.
Interested in licensing this patent?