Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12187739-B2
Publication Date
2025-01-07
Expiration Date
Abstract
This disclosure relates to polymorphs of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
Core Innovation
The disclosure concerns a crystalline polymorph form of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one, identified as polymorph form 1. The polymorph is characterized by powder X-ray diffraction data, including a peak at diffraction angle (2θ) of 27.4°±0.1 and additional peaks such as 9.4°±0.1, 16.1°±0.1, 16.5°±0.1, 18.8°±0.1, 21.2°±0.1, and 22.8°±0.1.
The PXRD pattern is tied to FIG. 1 and is stated to be substantially the same as shown in FIG. 1. The crystalline polymorph form 1 is also characterized by differential scanning calorimetry and a melting point value of 345.5 °C.
The document relates the polymorph to pharmaceutical compositions, including a capsule, and to methods of treating cancer and other diseases in mammals/humans. The methods are described for cancers mediated by ALK, ROS1, TRK, JAK2, SRC and/or FAK, including cancer subtypes.
Claims Coverage
The claim coverage includes one independent claim. It covers a pharmaceutical composition comprising a crystalline polymorph form of Compound I, defined by a PXRD peak at 2θ = 27.4°±0.1, with additional claim refinements across the claim family.
Crystalline polymorph form defined by a PXRD peak at 2θ = 27.4°±0.1
A pharmaceutical composition comprising a crystalline polymorph form of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one, wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising a peak at diffraction angle (2θ) of 27.4°±0.1.
The inventive concept is the identification of the crystalline polymorph form by PXRD-based characterization. The provided claim family also refines the polymorph with additional PXRD peaks, a substantially as shown in FIG. 1 characterization, and a DSC melting point constraint.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Pharmaceutical compositions, including a capsule.
Methods of treating cancer and other diseases in mammals/humans.
Methods for cancers mediated by ALK, ROS1, TRK, JAK2, SRC and/or FAK, including cancer subtypes.
Interested in licensing this patent?