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US 2026/0308175 A1Published application
Imidazolium salt macrocyclic compound and preparation method therefor and use thereof
AssigneeFudan University
InventorsZhanting LI, Danwei ZHANG, Wei ZHOU, Jingyu YANG, Yan WU, Yueyang LIU, Hui WANG
Life of this patent
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Abstract
An imidazolium salt macrocyclic compound, and a preparation method therefor, and a use thereof are provided. The macrocyclic compound as shown in formula (I) or a pharmaceutically acceptable salt, a hydrate, or a solvate thereof can be used in a composition with a pharmaceutically acceptable carrier, which is capable of producing neuromuscular junction block in the preparation of muscle relaxants.
Claims12
An imidazolium salt macrocyclic compound of formula I, or a pharmaceutically acceptable salt, a hydrate, or a solvate thereof, characterized in that,
- each R1 is independently selected from the group consisting of:
- H, D, substituted or unsubstituted C1-10 alkyl, substituted or unsubstituted 1-10 membered heteroalkyl containing 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C2-10 alkenyl, substituted or unsubstituted 2-10 membered heteroalkenyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C2-10 alkynyl, substituted or unsubstituted 2-10 membered heteroalkynyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C3-10 cycloalkyl, substituted or unsubstituted 3-10 membered heterocyclyl containing 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur;
- each R2 is independently selected from the group consisting of:
- H, substituted or unsubstituted C1-10 alkyl, substituted or unsubstituted 1-10 membered heteroalkyl containing 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C2-10 alkenyl, substituted or unsubstituted 2-10 membered heteroalkenyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C2-10 alkynyl, substituted or unsubstituted 2-10 membered heteroalkynyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, or two adjacent R2 together with their attached carbon atoms form a group selected from the group consisting of:
- substituted or unsubstituted C3-10 cycloalkyl, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 3-10 membered heterocyclyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, and substituted or unsubstituted 5-10 membered heteroaryl containing 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur;
- each Y is independently selected from the group consisting of:
- null, substituted or unsubstituted C1-10 alkylene, substituted or unsubstituted 1-10 membered heteroalkylene containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C3-10 cycloalkylene, substituted or unsubstituted C5-10 arylene, substituted or unsubstituted Ar1-L-Ar2, and substituted or unsubstituted 5-10 membered heteroarylene;
- each Z is independently selected from the group consisting of:
- substituted or unsubstituted Ar1-L-Ar2, and substituted or unsubstituted 5-10 membered heteroarylene;
- L is selected from the group consisting of:
- null, O, NH, C1-6 alkylene, S, and phenylene;
- Ar1 and Ar2 are each independently null, phenylene, or 5 membered heteroarylene;
- X is a pharmaceutically acceptable anion charge-balanced with the tetravalent cationic imidazolium macrocycle in the structure of formula I;
- unless otherwise specified, the “substituted” refers to the substitution of one or more hydrogens on a group by a group selected from the group consisting of:
- halogen, nitro, amino, cyano, hydroxyl, amido, trifluoromethyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, phenyl, benzyl, 3-6 membered heterocyclyl, and C1-6alkoxycarbonyl.
12 more elements
11-13. (canceled)
A method for relaxing skeletal muscles, comprising steps of:
- administering to a subject in need thereof a therapeutically effective amount of the imidazolium salt macrocyclic compound of formula I, or a pharmaceutically acceptable salt, a hydrate, or a solvate thereof, or the pharmaceutical composition comprising the imidazolium salt macrocyclic compound of formula I, or a pharmaceutically acceptable salt, a hydrate, or a solvate thereof:
- each R1 is independently selected from the group consisting of:
- H, D, substituted or unsubstituted C1-10 alkyl, substituted or unsubstituted 1-10 membered heteroalkyl containing 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C2-10 alkenyl, substituted or unsubstituted 2-10 membered heteroalkenyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C2-10 alkynyl, substituted or unsubstituted 2-10 membered heteroalkynyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C3-10 cycloalkyl, and substituted or unsubstituted 3-10 membered heterocyclyl containing 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur;
- each R2 is independently selected from the group consisting of:
- H, substituted or unsubstituted C1-10 alkyl, substituted or unsubstituted 1-10 membered heteroalkyl containing 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C2-10 alkenyl, substituted or unsubstituted 2-10 membered heteroalkenyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C2-10 alkynyl, substituted or unsubstituted 2-10 membered heteroalkynyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, or two adjacent R2 together with their attached carbon atoms form a group selected from the group consisting of:
- substituted or unsubstituted C3-10 cycloalkyl, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 3-10 membered heterocyclyl containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, and substituted or unsubstituted 5-10 membered heteroaryl containing 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur;
- each Y and Z are independently selected from the group consisting of:
- null, substituted or unsubstituted C1-10 alkylene, substituted or unsubstituted 1-10 membered heteroalkylene containing 1 to 3 heteroatoms selected from nitrogen, oxygen, and sulfur, substituted or unsubstituted C3-10 cycloalkylene, substituted or unsubstituted C5-10 arylene, substituted or unsubstituted Ar1-L-Ar2, and substituted or unsubstituted 5-10 membered heteroarylene;
- L is selected from the group consisting of:
- null, O, S, NH, C1-6 alkylene, and phenylene;
- Ar1 and Ar2 are each independently null, phenylene, or 5-membered heteroarylene;
- X is a pharmaceutically acceptable anion charge-balanced with the tetravalent cationic imidazolium macrocycle in the structure of formula I;
- unless otherwise specified, the “substituted” refers to the substitution of one or more hydrogens on a group by a group selected from the group consisting of:
- halogen, nitro, amino, cyano, hydroxyl, amido, trifluoromethyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, phenyl, benzyl, 3-6 membered heterocyclyl, and C1-6alkoxycarbonyl.
11 more elements
Dependencies are inferred from the claim text.