Therapeutic compounds and compositions
Inventors
Salituro, Francesco G. • Saunders, Jeffrey O. • Yan, Shunqi
Assignees
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Publication Number
US-12428376-B2
Publication Date
2025-09-30
Expiration Date
Abstract
Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
Core Innovation
The disclosure provides compounds of formula (I) or pharmaceutically acceptable salts thereof that modulate and activate PKM2. In this structure, W, X, Y, and Z represent CH or N, D and D1 represent a bond or NRb, and A is an optionally substituted bicyclic heteroaryl. The genus defines linker L alongside permitted selections for substituents R1, R3, Ra, Rb, Rc, and Rd, as well as designated values for n, m, h, and g.
Exemplary embodiments comprise quinoline-8-sulfonamide compounds with piperazine or 1,4-diazepane cores, piperazine-1-carbonyl derivatives, and reverse-sulfonamide variants bearing varied aryl, heteroaryl, benzyl, and cyclic substituents. Reported compounds include sodium and mesylate salts characterized by proton NMR, LCMS, and HPLC purity metrics. In addition, the text reports categorical screening results, including AC50 activity ratings, across evaluated structural variations.
Because background, summary, and abstract sections are omitted from the provided patent text, the specific technical problem addressed by the invention is not explicitly described in patent. The available disclosure focuses directly on chemical synthesis, structural characterization, isolated yields, and comparative categorical screening results across the synthesized compound series.
Claims Coverage
The claims identify one independent claim and four dependent claims, reciting three inventive features.
Compound of formula (I) or pharmaceutically acceptable salt
Claim 1 covers a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein W, X, Y, and Z are independently CH or N; D and D1 are independently a bond or NRb; A is optionally substituted bicyclic heteroaryl; L is selected from specified linker groups; and R1, R3, Ra, Rb, Rc, Rd, n, m, h, and g are defined by the recited structural alternatives.
Selected structural limitations
Dependent claims 2–4 narrow selected structural features by specifying W, X, Y, and Z as CH; D as NRb and D1 as a bond; and limiting L to a bond or listed linker groups.
Pharmaceutical composition
Dependent claim 5 recites a pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof.
The claims define a genus of formula (I) compounds and pharmaceutically acceptable salts, specify narrower structural embodiments, and recite a pharmaceutical composition comprising the compound or salt.
Stated Advantages
Not explicitly described in patent.
Documented Applications
A pharmaceutical composition comprising the compound of formula (I) or a pharmaceutically acceptable salt thereof.
Therapeutic applications for cancer and other PKM2-related disorders, including obesity, diabetes, autoimmune disorders, and benign prostatic hyperplasia.
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