Formulations of influenza therapeutics
Inventors
Zhao, Tianjing • Mao, Liang • Jacobson, Irina C. • Lee, Sam S K
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Assignees
Shanghai SynTheAll Pharmaceutical Co Ltd • Cocrystal Pharma Inc
Member
Cocrystal PharmaCocrystal Pharma is a clinical-stage biotechnology company specializing in the discovery and development of novel antiviral therapeutics for serious and chronic viral diseases such as influenza, COVID-19, hepatitis C, norovirus, and other respiratory viruses. The company leverages structure-based drug discovery technology and expertise in structural biology to design direct viral replication inhibitors with broad-spectrum activity. Its pipeline includes candidates in preclinical and clinical development, addressing unmet needs in antiviral medicine.
Cocrystal Pharma is a clinical-stage biotechnology company specializing in the discovery and development of novel antiviral therapeutics for serious and chronic viral diseases such as influenza, COVID-19, hepatitis C, norovirus, and other respiratory viruses. The company leverages structure-based drug discovery technology and expertise in structural biology to design direct viral replication inhibitors with broad-spectrum activity. Its pipeline includes candidates in preclinical and clinical development, addressing unmet needs in antiviral medicine.
Publication Number
US-12156876-B2
Publication Date
2024-12-03
Expiration Date
Abstract
Provided herein are compositions of an antiviral therapeutic to treat influenza suitable for administration via inhalation.
Core Innovation
The disclosed invention relates to crystalline 3-(2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-7H-pyrrolo[2,3-d]pyrimidin-7-yl)bicyclo[2.2.2]octane-2-carboxylic acid (Compound 1) in a micronized crystal form. The crystalline Compound 1 is designated Form B by an x-ray powder diffraction pattern exhibiting specified 2θ values at 5.6, 6.8, 8.4, 10.1, 10.6, 11.3, 15.1, 15.8, 18.0, 18.5, 19.1, 20.4, and 20.9 ±0.2°.
The invention further provides an inhalable formulation comprising the micronized crystalline Compound 1 (Form B) together with a filler. The formulation is adapted as an inhalable formulation and is described in the context of pulmonary delivery for influenza.
The problem being solved is the need for an inhalable formulation for influenza treatment or prevention that uses a specific solid form of Compound 1 identified as Form B, including its micronized crystal form and defined solid-state characteristics. The disclosed material also emphasizes pulmonary delivery rationale and exposure advantages, including lung-to-plasma concentration ratios, supported by documented solid-form characterization and pulmonary pharmacokinetic evaluation.
Claims Coverage
The document provides two independent claim scopes: (i) an inhalable formulation defined by Form B micronized Compound 1 with an XRPD-defined 2θ set and a filler, and (ii) crystalline Compound 1 itself defined as Form B by the same XRPD-defined 2θ set. Across the independent scopes, the core inventive features are centered on the Form B XRPD identification and, for the formulation claim, the presence of a filler and adaptation as an inhalable formulation.
Inhalable formulation with Form B micronized Compound 1 and XRPD-defined peaks
A formulation comprising crystalline Compound 1 (Form B) having an XRPD pattern exhibiting 2θ values of 5.6, 6.8, 8.4, 10.1, 10.6, 11.3, 15.1, 15.8, 18.0, 18.5, 19.1, 20.4, and 20.9 ±0.2°, wherein the crystalline Compound 1 is present as a micronized crystal form.
Filler in an inhalable formulation adapted for inhalation administration
A filler in the formulation, wherein the formulation is adapted as an inhalable formulation.
Crystalline Compound 1 designated Form B by XRPD-defined peaks
A crystalline Compound 1 designated Form B, having an XRPD pattern exhibiting 2θ values of 5.6, 6.8, 8.4, 10.1, 10.6, 11.3, 15.1, 15.8, 18.0, 18.5, 19.1, 20.4, and 20.9 ±0.2°.
Overall, claim coverage is grounded in solid-state identification of Compound 1 as Form B through a specific XRPD 2θ peak set and, for the formulation independent claim, combining that Form B micronized material with a filler in an inhalable formulation adapted for pulmonary administration.
Stated Advantages
Exposure advantages via pulmonary delivery, including lung-to-plasma concentration ratios.
Documented Applications
Treatment or prevention of influenza virus infection or replication by administering the inhalable formulation in an effective amount.
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