Heterocyclic compound and use thereof
Inventors
Li, Jinping • Guo, Xiaodan • Zhou, Feng • Lou, Jun • Liu, Li • Chen, Xiaoya • ZHANG, YIHAN • CHEN, Yongkai • Wang, Chaodong
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Assignees
Wuhan LL Science and Technology Development Co Ltd
Member
Glycos Biomedical LtdWe are UK/US entity with a team based in Maryland and North Carolina comprising an expert team that has linked triggers to disease states including TBI and acute injuries associated with radiation, acute lung injury and infection.
We are UK/US entity with a team based in Maryland and North Carolina comprising an expert team that has linked triggers to disease states including TBI and acute injuries associated with radiation, acute lung injury and infection.
Publication Number
US-12624041-B2
Publication Date
2026-05-12
Expiration Date
Abstract
Disclosed is a heterocyclic compound as represented by formula (I), a tautomer thereof, or a pharmaceutically acceptable salt thereof. The compound has better inhibitory activity on TRPC5, has good metabolic stability in liver micro-particles, and has good clinical pharmacokinetic properties.
Core Innovation
The invention relates to a heterocyclic compound represented by formula I, including a tautomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, and a solvate of the pharmaceutically acceptable salt. Formula I is defined by specific structural variables and substituent definitions with extensive allowable classes, including m, A, X, Z, Y, p, and the R positions, together with ring and heteroaryl options and optional substitution patterns.
The disclosed heterocyclic compounds are TRPC5 inhibitors and are used for TRPC5 inhibition. The compound class includes pharmaceutically acceptable acid or base salts and solvates, and the disclosure positions the heterocyclic scaffold as an inhibitor for TRPC5-mediated disease.
The disclosure also provides methods of inhibiting TRPC5 in a subject in need thereof by administering an effective amount of substance Y, where substance Y is a heterocyclic compound of formula I. The method coverage further includes TRPC5-mediated diseases selected from psychiatric, neurological, neurodegenerative, and nephropathy conditions.
Claims Coverage
The independent claims identified in the provided claim set are the heterocyclic compound of formula I and the method of inhibiting TRPC5. Across these claims, the inventive features are the formula I heterocyclic compound definition with tautomer, salt, and solvate coverage, and the use of the compound as a TRPC5 inhibitor for treating or preventing TRPC5-mediated disease.
Heterocyclic compound of formula I with tautomer, pharmaceutically acceptable salt, and solvate forms
A heterocyclic compound represented by formula I, a tautomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof or a solvate of the pharmaceutically acceptable salt thereof, with defined variables including m, A, X, Z, Y, p, and the R positions, and extensive substituent options and constraints.
TRPC5 inhibition by administering formula I compound
A method for inhibiting TRPC5 in a subject in need thereof by administering an effective amount of substance Y, where substance Y is the heterocyclic compound of formula I, including its tautomer, pharmaceutically acceptable salt, solvate, or solvate of the salt.
The claim coverage is anchored by formula I heterocyclic compounds, including tautomers, pharmaceutically acceptable salts, and solvates, and by a method that administers substance Y to inhibit TRPC5 in a subject.
Stated Advantages
Improved TRPC5 inhibitory activity.
Good metabolic stability in liver microsomes.
Favorable clinical pharmacokinetic properties.
Documented Applications
A medicament for treating and/or preventing TRPC5-mediated psychiatric, neurological, neurodegenerative, and nephropathy diseases.
Treatment and/or prevention of psychiatric conditions including depression and anxiety disorders, with examples including major depression and bipolar disorder.
Treatment and/or prevention of neurodegenerative and neurological conditions.
Treatment and/or prevention of nephropathies, including focal segmental glomerulosclerosis, minimal change nephropathy, and diabetic nephropathy.
Manufacture of a TRPC5 inhibitor and a medicament for use in treating and/or preventing TRPC5-mediated diseases.
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