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Publication Number
US-12194034-B2
Publication Date
2025-01-14
Expiration Date
Abstract
The present invention is directed to compounds and compositions comprising thereof. Further, methods of use such as for the treatment and prevention of a neutrophil-associated disease or condition in a subject in need thereof are also provided.
Core Innovation
The invention relates to compound candidates, including any stereoisomer or a salt thereof, represented by Formula I or by Formula (IIb). The structures are expressed through variables including A, Y, n, X, and substituent definitions for each R and R-variants, with specific classes of alkyl, cycloalkyl, heteroatom-containing groups, heteroaryl, heterocyclyl, and rings, including connectivity rules that form optionally substituted 4 to 8-membered rings.
The compound definitions include Y being absent or selected from N, NH, NR1, CH, HCR1, CH2, S, SH, and O, and define n as an integer between 0 and 5, or between 1 and 5 in an alternative formula set as stated. The framework further defines R1 and R2 as independently selected from hydrogen, C1–C20 alkyl, optionally substituted aminoalkyl, heteroatom-containing alkyl, substituted alkyl, haloalkyl, and aminoalkyl variants, including ring-forming interconnections with Y or with R2 to form an optionally substituted 4 to 8-membered ring.
The disclosure further includes therapeutic embodiments involving delivery and formulation. A nanoparticle is described as having a core comprising the compound and a shell made of a lipid layer comprising a phospholipid and a sterol, and the formulation can be configured as a liposome or micelle with a size range of 50–500 nm, optionally including a peptide with amino acid sequences identified by SEQ ID NO: 1–13.
The disclosure includes pharmaceutical compositions for treating neutrophil-associated diseases using administration routes that include systemic, intravenous, topical, intratumoral, and local administration. Additional embodiments include alternative compound structures associated with Formula IV, IVa, IVb and additional numbered forms, emphasizing substituent flexibility and stereoisomer coverage as stated in the provided content.
Claims Coverage
The claim coverage centers on broad compound definitions by Formula I or Formula (IIb), including stereoisomers and salts, with multiple structural variables and substituent classes. Additional coverage includes a nanoparticle lipid-layer architecture, optional peptide attachment using specified SEQ ID NOs, and treatment of neutrophil-associated diseases.
Formula I or Formula (IIb) compound architecture
A compound, including any stereoisomer or a salt thereof, wherein the compound is represented by Formula I or by Formula (IIb).
Variable constraints for A, Y, n and X
A represents a selected group of methyl, isopropyl, tert-butyl, linear or branched C1–C10 alkyl and related substituted alkyl, optionally substituted cycloalkyl and heteroatom-containing alkyl, haloalkyl, alkylhydroxy, halo, alkoxy, cycloalkyl, heteroaryl, heterocyclyl, bicyclic aromatic ring, unsaturated aliphatic ring, and bicyclic aliphatic ring; Y is absent or selected from N, NH, NR1, CH, HCR1, CH2, S, SH, and O; n is an integer between 0 and 5, or between 1 and 5 as stated in the alternative formula set; X is hydrogen or represents a substituent selected from a group including halo, methyl, isopropyl, C2–C10 alkyl, substituted C2–C10 alkyl, alkoxy, amino, and hydroxy.
Substituent selection for each R and ring-forming R/R1/R2 connectivity rules
Each R independently is absent or represents one or more substituents each independently comprising one of a listed set of functional groups, including halo, oxo, NO2, amino, hydroxy, cyano, carbonyl amides, ureas and related nitrogen-containing groups, sulfur-containing groups, and other heteroatom substituents as listed; each R2 independently represents hydrogen or selected substituent groups as allowed by valency; R1 and R2 are each independently selected from hydrogen, C1–C20 alkyl, optionally substituted linear or branched aminoalkyl and heteroatom-containing variants, substituted C1–C20 alkyl, haloalkyl, and aliphatic linear or branched C3–C20 aminoalkyl variants, or wherein R1 and Y are interconnected to form an optionally substituted 4 to 8-membered ring, or wherein R1 and R2 are interconnected to form an optionally substituted 4 to 8-membered ring optionally comprising one or more heteroatoms.
R3 and R4 selectable substituents with optional interconnection to A or Y
R3 is hydrogen, or is absent, or represents a methyl group, isopropyl group, C2–C10 alkyl and related substituted, hydroxy, haloalkoxy, amino, thio and other listed groups, or any combination thereof, or wherein R3 and A are interconnected to form an optionally substituted 4 to 8-membered ring; or R3 and Y are interconnected to form an optionally substituted 4 to 8-membered ring and R4 is absent, hydrogen, or represents a methyl group, isopropyl group, C2–C10 alkyl and related substituted, hydroxy, haloalkoxy, cycloalkyl, heteroaryl, heterocyclyl and related listed groups, or wherein R3 and R4 are interconnected to form an optionally substituted 4 to 8-membered ring.
Nanoparticle with compound core and lipid-layer shell
A nanoparticle having a core containing the compound and a shell made of a lipid layer comprising a phospholipid and a sterol, optionally configured as a liposome or micelle.
Nanoparticle with optional peptide selected from SEQ ID NO: 1-13
The nanoparticle further including a peptide with an amino acid sequence selected from SEQ ID NO: 1–13.
Treating neutrophil-associated disease
A method of treating a neutrophil-associated disease or condition by administering the nanoparticle or pharmaceutical composition.
The claim coverage is grounded in a broad compound definition using Formula I or Formula (IIb) with extensive substituent choice and optional interconnections forming optionally substituted 4 to 8-membered rings. Additional features include a lipid-layer nanoparticle with optional peptide sequences and treatment of neutrophil-associated diseases.
Stated Advantages
Documented Applications
No documented applications found
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