Griseofulvin compound and pharmaceutical use thereof
Inventors
Saito, Keiji • Nakajima, Katsuyoshi • Ogawa, Yasuyuki • Makino, Mitsuhiro • Ito, Kaori • Nagata, Seiko • Hirasawa, Makoto
Assignees
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Publication Number
US-12692258-B2
Publication Date
2026-07-28
Expiration Date
Abstract
The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem. [R1: a C1-C6 alkyl group or the like, R2: a C1-C6 alkyl group or the like, A: a 5-membered aromatic hetero-ring or the like, R3, R3′: a C1-C6 alkyl group or the like].
Core Innovation
The invention relates to a method for treating a central inflammatory disease in a subject in need thereof by delivering a compound of general formula (1) or a pharmacologically acceptable salt thereof. The compound scope is defined by specific substituent choices for R1, R2, A, and R3/R3', including multiple allowed ring types for A and multiple allowed substituent groups for R1 and R2. The formula-related constraints are further limited by an explicit exclusion of compounds of general formula (Z).
In the claimed chemical definition, A is selected from a 5-membered aromatic heterocyclic ring, a 6-membered aromatic heterocyclic ring, an 8-10 membered condensed aromatic heterocyclic ring, a 5-7 membered unsaturated heterocyclic ring, a 4-7 membered saturated heterocyclic ring, a benzene ring, -CH=, or a cyano group, with corresponding limitations for R3 and R3'. When A is a cyano group, R3 and R3' do not exist, while otherwise R3 and R3' are each independently selected from hydrogen, halogen, cyano, hydroxy, oxo, alkyl/alkoxy/alkenyl/alkynyl, cycloalkyl, amino, alkoxycarbonyl, carbamoyl, phenyl, and various aromatic/heteroaromatic and ring-forming options subject to the conditional condensation described in the formula definition.
The compound definition also specifies that substituent group X and substituent group Y each include defined sets of functional groups, including halogen atom, cyano, hydroxy, oxo, C1-C6 alkyl/alkoxy and haloalkyl/haloalkoxy, cycloalkyl/halocycloalkyl, and multiple carbonyl- and sulfonamide-related groups. The claimed subject matter thus centers on a structured family of spiro/benzofused aromatic bicyclic scaffolds exemplified in the described compound examples, while providing characterization data for multiple specific numbered compounds.
Claims Coverage
The document includes one independent claim (clm-00001). The core inventive features cover delivering a compound of general formula (1) or a pharmacologically acceptable salt for treating a central inflammatory disease, the broad structural definition of the compound, and an explicit exclusion of compounds of general formula (Z).
Treating a central inflammatory disease by delivering general formula (1) compounds
Delivering to the subject a compound of general formula (1) or a pharmacologically acceptable salt thereof for treating a central inflammatory disease, wherein the compound is defined by substituent selections for R1, R2, A, and R3/R3' including conditional presence or absence when A is a cyano group, and wherein a compound of general formula (Z) is excluded based on defined characteristics of R1, R2, A, and R3.
General formula (1) structural definitions for R1, R2, and ring A
R1 and R2 are each defined as a C1-C6 alkyl group, a C3-C6 cycloalkyl group, or a 4-7 membered saturated heterocyclic group optionally substituted with substituent group X, and A is selected from specified aromatic heterocyclic rings, a benzene ring, -CH=, or a cyano group, with corresponding limitations for R3 and R3'.
Allowed substituents for R3, substituent group X, and ring-condensation options
R3 and R3' are each independently selected from hydrogen, halogen, cyano, hydroxy, oxo, alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, amino, alkoxycarbonyl, carbamoyl, phenyl, and various aromatic or saturated heterocycles, with the additional condition that R3 and R3' may form a ring that binds to each other and condenses with A; substituent group X is defined through an enumerated set of allowed substituents.
Explicit exclusion of a compound of general formula (Z)
A compound or a pharmacologically acceptable salt thereof of general formula (Z) is excluded, where for general formula Z: R1 is a C1-C6 alkyl group or a hydroxy C1-C6 alkyl group, R2 is a C1-C6 alkyl group, A is a 5-membered aromatic heterocyclic ring, and R3 is a C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, or a C1-C6 alkoxy C1-C6 alkyl group.
Overall, the claim coverage is centered on a treatment method for a central inflammatory disease by delivering a compound of general formula (1) or a pharmacologically acceptable salt, with broad structural definitions for R1, R2, ring A, and substituent group X, while explicitly excluding specified general formula (Z) compounds.
Stated Advantages
Improved anti-inflammatory activity.
Improved drug properties, including bioavailability.
Improved drug properties, including stability.
Improved drug properties, including toxicity.
Improved drug properties, including drug interaction.
Documented Applications
Treating central inflammatory diseases in a subject in need thereof.
Prophylaxis and/or treatment of central inflammatory diseases by delivering compounds of general formula (1) or pharmacologically acceptable salts.
Treatment of central inflammatory disease indications including neurodegenerative disorders, encephalopathy-related disorders, and psychiatric and related disorders.
The document enumerates central inflammatory disease indications including neurological and psychiatric disorders such as Alzheimer's disease, Parkinson's disease, Lewy body dementia, multiple system atrophy, Pick's disease, progressive supranuclear palsy, and others listed in the partial content.
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