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Publication Number
US-12649736-B2
Publication Date
2026-06-09
Expiration Date
Abstract
The present disclosure relates to a method of synthesizing a compound represented by formula I.
Core Innovation
The invention relates to a method for the preparation of a compound having a defined structure, or a pharmaceutically acceptable salt thereof. The method comprises reacting an intermediate with an acylation reagent to produce an intermediate, then reacting that intermediate with a further reagent to produce a further intermediate, and further hydrolyzing to produce the final compound or pharmaceutically acceptable salt thereof.
The disclosed subject matter further includes compounds within multiple chemical scaffold families, including formulas B, BI, BII, BIII, BIV, BV, BVI, BVII, C, CIa, and CI, and generic structural depiction of N-containing heterocycles having substituents R9 and R10. It also provides variable groups such as A, X, Y, R substituents, and n, together with classes of groups used in compound structures, including amine and amino, hydrocarbyl, aryl and heteroaryl, heterocycle and heterocyclyl, halo, sulfonamide, sulfonate, and sulfone, and pharmaceutically acceptable salts and prodrugs.
The document additionally describes chemical structures labeled JXL001 through JXL030, JXL005 through JXL030, and examples including JXL082 and JXL069. It further describes hydrolysis and deprotection to convert ester or alkyl ester intermediates to (E)-cyanoacrylic acid JXL069, and identifies dependent refinements that hydrolyze compound 4 to produce JXL069 with stated yield levels.
Claims Coverage
The independent claim is directed to a method of preparing a compound, or a pharmaceutically acceptable salt thereof, through acylation, reaction with a further reagent, and further hydrolysis. Dependent claims add inventive features by constraining an intermediate leaving group W and by specifying hydrolysis yield for production of JXL069.
Method for preparing a compound by acylation, further reaction, and hydrolysis
Reacting an intermediate with an acylation reagent to produce an intermediate, reacting the intermediate with a further reagent to produce a further intermediate, and further hydrolyzing to produce the compound or a pharmaceutically acceptable salt thereof.
Hydrolyzing compound 4 to produce JXL069 with high yield
Hydrolyzing compound 4 to produce JXL069 with more than 90% yield and in 95% yield.
Intermediate leaving group W
The intermediate includes W as a leaving group.
Leaving group W as halo
W is a halo group.
Leaving group W as bromo
W is bromo.
Across the claims, the core method sequence is acylation of an intermediate, reaction with a further reagent to produce a further intermediate, and further hydrolysis to produce the target compound or pharmaceutically acceptable salt. Dependent claim coverage narrows an intermediate leaving group W, including halo and bromo, and specifies hydrolysis of compound 4 to JXL069 at stated yields.
Stated Advantages
Yields for producing JXL069 are specified as more than 90% and 95% in connection with hydrolyzing compound 4.
Documented Applications
Hair-growth related compounds characterized as MPC inhibitors are referenced in the description context, including compounds intended to be prepared by the described synthesis method.
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