Processes for the preparation of uracil derivatives
Inventors
Gallagher, Donald J. • Treiber, Laszlo R. • Hughes, Robert Michael • Campopiano, Onorato • Wang, Peng • Zhao, Yuxin • Chou, Shine K. • Ouellette, Michael Allen • Hettinger, Donald Nicholas
Assignees
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Publication Number
US-11459305-B2
Publication Date
2022-10-04
Expiration Date
Abstract
The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
Core Innovation
The invention is directed to formulations containing a compound of formula 5-1 as an amorphous co-solution with an excipient or other carrier. In one aspect, the amorphous co-solution is spray-dried to produce a spray-dried amorphous co-solution. The co-solution is formed with the excipient or other carrier to support the amorphous presentation of the compound of formula 5-1.
In another aspect, the invention is directed to a formulation comprising an amorphous co-solution of the compound of formula 5-1 with an excipient or other carrier, without limiting to spray-drying. The excipient or other carrier includes mannitol, polyvinyl pyrrolidone, and/or hydroxypropylmethylcellulose, including embodiments where the excipient or other carrier is a polymer.
The document further describes process/formulation examples for converting the compound into an amorphous solid or amorphous mixtures. Spray drying is used to produce an amorphous solid, and the amorphous nature is characterized as spray-dried amorphous co-solution, including trials supported by XRPD and DSC characterization.
Claims Coverage
The partial content provides two independent formulation claims, with additional dependent claims that specify excipient/carrier selections and include administering-based treatment methods for named conditions. Across the independent claims, the inventive focus centers on amorphous co-solution formulations of compound 5-1, including spray-dried amorphous co-solution in one claim and amorphous co-solution in the other claim.
Spray-dried amorphous co-solution formulation
A formulation comprising a spray-dried amorphous co-solution of a compound of formula 5-1 and an excipient or other carrier.
Amorphous co-solution formulation
A formulation comprising an amorphous co-solution of a compound of formula 5-1 and an excipient or other carrier.
Overall claim coverage is directed to amorphous co-solution formulations of compound 5-1 with an excipient or other carrier, where one independent claim specifically requires a spray-dried amorphous co-solution and the other requires an amorphous co-solution. Dependent claims further narrow the formulation by specifying excipients/carriers including mannitol, polyvinyl pyrrolidone, and hydroxypropylmethylcellulose, and embodiments where the carrier is a polymer.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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