Therapeutic compounds and compositions
Inventors
Chrusciel, Robert A. • Gadwood, Robert C. • Hayward, Neil J. • Melnick, Michael J. • Navia, Manuel A. • Poel, Toni J. • Stassen, Frans L. • Stewart, Catherine A.
Assignees
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Publication Number
US-10259785-B2
Publication Date
2019-04-16
Expiration Date
Abstract
The present invention provides compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and composition.
Core Innovation
The disclosure concerns pharmaceutically acceptable salt forms of compounds having a specified structure, and the claim set narrows the salt identity to hydrochloride salt. The material also presents multiple chemical structure depictions for related compounds that share complex core scaffolds while varying substituents such as halogenated phenyl or pyridyl groups, fluorinated substituents, ether or ester variants, and other aromatic and heteroaryl substituents.
The chemical structure depictions include compounds with common bicyclic, heterocyclic, azetidine-based, beta-lactam/core motifs, and peptidomimetic core features, together with multiple carbonyl functionalities such as carboxylic acid, amide, urea-like, and lactam-like groups. The disclosed embodiments vary through amino-substituted pyridine-like groups, aminothiophene-like groups, phenyl substituents, chlorophenyl groups, and sulfonyl-containing groups.
The document also describes therapeutic Factor XIa or kallikrein inhibitors and associated dosing regimens, including intravenous infusion, intravenous bolus dosing, maintenance dose, and intermittent treatment concepts. The disclosed subject matter further states that the compounds can be evaluated for modulating Factor XIa and/or kallikrein and frames the compounds as therapeutic agents for thrombotic and inflammatory or angioedema-related disorders, including hereditary angioedema.
Claims Coverage
The provided independent claims are directed to pharmaceutically acceptable salts of a compound having a specified structure. Across the claim families, the recurring inventive feature is the salt form, and the dependent claims narrow that salt identity to hydrochloride salt, giving one principal inventive feature across the set.
Pharmaceutically acceptable salt of a compound having a specified structure
A pharmaceutically acceptable salt of a compound having the structure recited in the claim.
Hydrochloride salt form
The pharmaceutically acceptable salt is a hydrochloride salt.
The claim coverage is centered on pharmaceutically acceptable salts of compounds defined by a specified structure, with the only explicit refinement in the dependent claims being the hydrochloride salt form.
Stated Advantages
Purported safer antithrombotic profile with less/no effect on bleeding.
Prevents or treats undesired thrombosis.
Prevents or treats angioedema.
Addresses hereditary angioedema.
Documented Applications
Thromboembolic indications, including stroke risk reduction.
Ischemia and transient ischemic event.
Systemic embolism and non-central nervous system systemic embolism.
Deep vein thrombosis for treatment and/or prophylaxis.
Pulmonary embolism for treatment and/or prophylaxis.
Therapeutic utility for thrombotic disorders.
Therapeutic utility for inflammatory or angioedema-related disorders, including hereditary angioedema.
Prevention or treatment of undesired thrombosis using Factor XIa or kallikrein inhibitors.
Prevention or treatment of angioedema, including hereditary angioedema, using Factor XIa or kallikrein inhibitors.
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