Compounds, devices, and uses thereof
Inventors
Veiseh, Omid • Heidebrecht, Richard • Wotton, Paul Kevin • Oberli, Matthias Alexander • Miller, Robert James
Assignees
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Publication Number
US-11945786-B2
Publication Date
2024-04-02
Expiration Date
Abstract
The present invention provides compounds, e.g., compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are implantable elements (e.g., devices and materials) comprising the same, as well as methods of use thereof, e.g., for treating or preventing a disease, disorder, or condition.
Core Innovation
The invention provides compounds of Formula (II-k) and salts thereof, where Z1 is heterocyclyl or aryl, each optionally substituted with 1-5 R5. The structure further includes R2a, R2b, R2c, and R2d, which are independently hydrogen or alkyl, or selected pairs are taken together to form an oxo group, together with RC as hydrogen or alkyl and RD as hydrogen, alkyl, or alkenyl, with alkyl and alkenyl optionally substituted with 1-6 R6.
The Formula (II-k) framework defines R6 as alkyl, alkenyl, halogen or oxo, and defines R3 and R5 as independently alkyl, alkenyl, alkynyl, heteroalkyl, halogen, cyano, azido, oxo, or substituted-linkage options including —ORA1, —C(O)ORA1, —C(O)RB1, —OC(O)RB1, —N(RC1)(RD1), —N(RC1)C(O)RB1, —C(O)N(RC1)(RD1), and SRE1, as well as cycloalkyl, heterocyclyl, aryl, heteroaryl, or monocyclic heteroaryl.
The structural definitions further include R7 as alkyl, alkenyl, alkynyl, heteroalkyl, halogen, cyano, oxo, hydroxyl, cycloalkyl, or heterocyclyl, with each of m and n equal to 1, p equal to 0, 1, 2, 3, or 4, and q an integer from 1 to 25. A narrower embodiment defines Z1 as 6-membered heterocyclyl optionally substituted with 1-5 R5, and the disclosure also includes pharmaceutical compositions comprising the compound and a pharmaceutically acceptable excipient.
Claims Coverage
The provided text includes two independent claims, clm-00001 and clm-00008. Both independent claims define a compound of Formula (II-k) or a salt thereof through the same core variable framework, with the main distinction being the scope of Z1 and associated dependent restrictions; in total, the claims present four merged inventive features.
Compound of Formula (II-k) with heterocyclyl or aryl Z1
A compound of Formula (II-k) or a salt thereof, wherein Z1 is heterocyclyl or aryl optionally substituted with 1-5 R5, and each of R2a, R2b, R2c, and R2d is independently hydrogen or alkyl, or selected pairs are taken together to form an oxo group.
Substituent framework for RC, RD, R6, R3 and R5
RC is hydrogen or alkyl; RD is hydrogen, alkyl, or alkenyl optionally substituted with 1-6 R6; R6 is alkyl, alkenyl, halogen or oxo; and R3 and R5 are independently alkyl, alkenyl, alkynyl, heteroalkyl, halogen, cyano, azido, oxo, —ORA1, —C(O)ORA1, —C(O)RB1, —OC(O)RB1, —N(RC1)(RD1), —N(RC1)C(O)RB1, —C(O)N(RC1)(RD1), SRE1, cycloalkyl, heterocyclyl, aryl, heteroaryl, or monocyclic heteroaryl.
Defined R-group substitution counts and integer constraints
RA1, RB1, RC1, RD1, and RE1 are independently hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl, each optionally substituted with 1-6 R7; R7 is alkyl, alkenyl, alkynyl, heteroalkyl, halogen, cyano, oxo, hydroxyl, cycloalkyl, or heterocyclyl; and each of m and n is 1, p is 0, 1, 2, 3, or 4, and q is an integer from 1 to 25.
Compound of Formula (II-k) with 6-membered heterocyclyl Z1
A compound of Formula (II-k) or a salt thereof, wherein Z1 is 6-membered heterocyclyl optionally substituted with 1-5 R5, with the same R2a-R2d, RC, RD, R6, R3, R5, RA1, RB1, RC1, RD1, RE1, R7, m, n, p, and q framework.
Across the independent claims, the inventive core is the Formula (II-k) compound or salt defined by selectable Z1, broad substituent-variable definitions for R2a-R2d, RC, RD, R3, R5, R6, R7, and the RA1/RB1/RC1/RD1/RE1 groups, together with the fixed integer constraints m = 1, n = 1, p = 0-4, and q = 1-25.
Stated Advantages
Modulates immune responses by up-regulating or down-regulating immune response pathways.
Can be used to reduce fibrosis and inflammation at implanted cells or devices in implantable-device contexts.
Provides compounds, compositions, and devices for prevention and treatment by modulating immune response.
Documented Applications
A pharmaceutical composition including the compound of claim 1 together with a pharmaceutically acceptable excipient.
A pharmaceutical composition including the compound and a pharmaceutically acceptable excipient.
Treating or preventing disease, disorder, or condition in a subject using immunomodulatory compounds.
Use in implantable devices in which the compound is disposed on or covalently attached to a device surface, with stated potential to reduce fibrosis and inflammation at implanted cells or devices.
Treatment or prevention across disease categories including neurodegenerative diseases, autoimmune diseases, cancer, lysosomal storage diseases, diabetes, blood clotting disorders, amino acid metabolism disorders, and fatty acid metabolism disorders.
Prevention and treatment by modulating immune response.
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