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Publication Number
US-10618918-B2
Publication Date
2020-04-14
Expiration Date
Abstract
Disclosed herein are antimicrobial compounds having the structure of the formula III′ pharmaceutical compositions, the use and preparation thereof. The compounds are of the class of boronic acid derivatives, useful for antimicrobial treatment.
Core Innovation
The invention relates to a compound of formula (III-2) or a pharmaceutically acceptable salt thereof, with variable groups J, L, and M as CR5 and broad substituent selections for R5, M', Y3, R1, R2, R3, and R4. The structural framework includes broad classes of alkyl, heteroalkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, halogen, and CN substituents, together with optional substitution rules controlled by parameters p and q.
A central structural aspect includes the motif (CH2)p-Y3-(CH2)q-M', where Y3 is selected from -CR1R2-, -NR1-, -O-, -S-, -S(O)-, and -S(O)2-, and p and q are each 0, 1, or 2. The disclosure also describes pharmaceutically acceptable salts, including alkali metal cation salts and ammonium salts, together with enantiomers, diastereomers, racemates, crystalline forms, amorphous forms, polymorphs, solvates, and hydrates.
The document further states that the compounds act as antimicrobial agents and/or potentiate antimicrobial agents. It includes pharmaceutical compositions comprising the compounds and pharmaceutically acceptable excipients, and methods for treating or preventing bacterial infections by administering a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof.
Claims Coverage
The independent claim set centers on a formula (III-2) compound or a pharmaceutically acceptable salt, with broad structural definitions across multiple variable groups. Across the consolidated items, the inventive features comprise formula-defined substituent selections, a linker motif, constrained R5 and M' selections, salt-form restrictions, and a therapeutic use claim; five inventive features are identified.
Formula (III-2) compound with defined variable substituents
A compound of formula (III-2) or a pharmaceutically acceptable salt thereof, wherein J, L, and M are each CR5; each R5 is independently selected from broad substituent groups including H, halogen, CN, C1-C6 alkyl, C1-C6 heteroalkyl, and multiple substituted and functionalized groups; and R1, R2, R3, R4, M', and p and q are defined by enumerated groups, ranges, and optional substitution rules.
Linker motif (CH2)p-Y3-(CH2)q-M'
At least one R5 group contains the structural motif (CH2)p-Y3-(CH2)q-M', with Y3 selected from -CR1R2-, -NR1-, -O-, -S-, -S(O)-, and -S(O)2-, and with p and q each being 0, 1, or 2.
Specific multiple R5 substituent selection
At least two R5 substituents are independently selected from specified options, including combinations involving F and OCH3 or involving Cl and OCH3.
Constrained M' substituent enumeration
At least one M' substituent is independently chosen from an explicitly enumerated set including CN, fluorinated carbon groups, sulfonyl-containing groups, hydroxyl-containing groups, amino-containing groups, and other listed substituents.
Therapeutic use for bacterial infection
A method for treating a bacterial infection in a subject by administering a therapeutically effective amount of a compound of formula (III-2) or a pharmaceutically acceptable salt thereof.
The claim coverage is centered on a formula (III-2) compound family defined by extensive substituent selection rules, the (CH2)p-Y3-(CH2)q-M' motif, specific R5 and M' limitations, salt-form restrictions, and a method of treating bacterial infection.
Stated Advantages
The compounds act as antimicrobial agents and/or potentiate antimicrobial agents.
The compounds are used for treating or preventing bacterial infections.
Documented Applications
Pharmaceutical compositions comprising the compounds and pharmaceutically acceptable excipients.
Treating a bacterial infection in a subject by administering a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof.
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