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US 2025/0367129 A1Published application
Lipid Compounds and Uses Thereof
AssigneePfizer Inc.
InventorsMatthew Frank Brown, Daniel Paul Canterbury, Ye Che, Wenhua Jiao, Roger Hochoon Pak, Mark Edward Schnute
Life of this patent
Estimating the term…
Abstract
Compounds are provided having the following structure: (I) or a pharmaceutically acceptable salt, N-oxide, tautomer or stereoisomer thereof, wherein R1, G1, W and m, n, o and p are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a nucleic acid, compositions comprising the compounds and methods for their use and preparation are also provided.
Claims22
A compound of Formula (I)
- or a pharmaceutically acceptable salt, N-oxide, tautomer, or stereoisomer thereof, wherein
- m, n, o, and p are each independently 1-3;
- G1 is C1-12alkylene or C2-12alkenylene;
- R1 is —N(R2)R3, —OR4, CN, —N(R4)(heteroaryl), —O(CH2)qOH, —(OCH2CH2)rOH, —OC(═O)R5, —N(R4)C(═O)R5, —N(R4)S(O)2R5, —N(R4)C(═O)N(R2)R3, —OC(═O)N(R2)R3, —N(R4)C(═O)OR5, —N(R4)C(═S)N(R2)R3, —N(R4)C(═NR6)N(R2)R3, or
- R2 and R3 are each independently H, C1-6alkyl, C3-8cycloalkyl, or aryl;
- or R2 and R3 together with the nitrogen atom to which they are attached form a heterocyclic ring;
- R4 is H, C1-6alkyl or C3-8cycloalkyl;
- R5 is C1-6alkyl or C3-8cycloalkyl optionally substituted by C1-6alkyl;
- R6 is H, CN, NO2, C1-6alkyl, OR5, S(O)2R5, or S O)2N(R2)R3;
- q is 2-6;
- r is 1-6;
- W is
- X is N or CH;
- G2 and G3 are each independently C1-12alkylene or C2-12alkenylene;
- L1 and L2 are each independently —C(═O)OR7, —OC(═O)R7, —OC(═O)(CH2)rC(═O)OR7, —OC(═O)(CH2)rOC(═O)R7, —OC(═O)N(R4)R7, —N(R4)C(═O)OR7, —N(R4)C(═O)N(R4)R7, —OC(═O)OR7, or —S—SR7;
- and
- R7 is C6-24alkyl, C6-24alkenyl, or C6-24alkynyl where each is optionally substituted by F, C1-6alkoxy, C3-8cycloalkyl, or C3-8cycloalkenyl, wherein the R7 of L1 and L2 may be the same or different.
14 more elements
2-4. (canceled)
13-40. (canceled)
(canceled)
51-53. (canceled)
Dependencies are inferred from the claim text.