公开(公告)号：US12121591B2

公开(公告)日：2024-10-22

申请号：US18392458

申请日：2023-12-21

申请人： NanoVation Therapeutics Inc.

发明人： Deaglan Arnold ,  Nagavenkata Durga Prasad Atmuri ,  Fariba Saadati ,  Huy Tran ,  Marco A. Ciufolini

IPC分类号： A61K47/69 ,  A61K9/51 ,  A61K47/20 ,  C07C323/12 ,  C07C323/25 ,  C07D205/04 ,  C07D317/28

CPC分类号： A61K47/6929 ,  A61K9/5123 ,  A61K47/20 ,  C07C323/12 ,  C07C323/25 ,  C07D205/04 ,  C07D317/28 ,  C07B2200/05

摘要： Provided herein is an ionizable, cationic amino lipid or a pharmaceutically acceptable salt thereof. The ionizable, cationic amino lipid has:



a protonatable amino head group;
two lipophilic chains, wherein the protonatable amino head group has a central carbon atom to which each of the two lipophilic chains are directly bonded;
at least one of the two lipophilic chains has a structure of Formula C:










wherein E is an ester in either orientation. The compounds may be formulated in a lipid nanoparticle for use in the delivery of charged cargo such as nucleic acid.

公开(公告)号：US20240294462A1

公开(公告)日：2024-09-05

申请号：US18442431

申请日：2024-02-15

申请人： NanoVation Therapeutics Inc.

发明人： Fariba Saadati ,  Huy Tran ,  Marco Ciufolini ,  N. D. Prasad Atmuri

IPC分类号： C07C227/16 ,  C07C213/00 ,  C07C213/02 ,  C07C319/02

CPC分类号： C07C227/16 ,  C07C213/00 ,  C07C213/02 ,  C07C319/02

摘要： Provided herein is a method for the preparation of ionizable, cationic amino lipids using a doubly alkylated nucleophilic intermediate to produce a ketone. The ketone, or a corresponding alcohol, is subjected to one or more synthesis steps to add an ionizable moiety thereto. The method can be advantageously employed for the synthesis of unsymmetrical analogues of the above lipids that would be considerably more difficult to make by alternative strategies. The method can also be used to prepare symmetrical ionizable, cationic amino lipids with fewer steps and/or with the use of fewer hazardous chemicals than known synthesis methods.

公开(公告)号：US20240261430A1

公开(公告)日：2024-08-08

申请号：US18392458

申请日：2023-12-21

申请人： NanoVation Therapeutics Inc.

发明人： Deaglan Arnold ,  Nagavenkata Durga Prasad Atmuri ,  Fariba Saadati ,  Huy Tran ,  Marco A. Ciufolini

IPC分类号： A61K47/69 ,  A61K9/51 ,  A61K47/20 ,  C07C323/12 ,  C07C323/25 ,  C07D205/04 ,  C07D317/28

CPC分类号： A61K47/6929 ,  A61K9/5123 ,  A61K47/20 ,  C07C323/12 ,  C07C323/25 ,  C07D205/04 ,  C07D317/28 ,  C07B2200/05

摘要： Provided herein is an ionizable, cationic amino lipid or a pharmaceutically acceptable salt thereof. The ionizable, cationic amino lipid has:



a protonatable amino head group;
two lipophilic chains, wherein the protonatable amino head group has a central carbon atom to which each of the two lipophilic chains are directly bonded;
at least one of the two lipophilic chains has a structure of Formula C:










wherein E is an ester in either orientation. The compounds may be formulated in a lipid nanoparticle for use in the delivery of charged cargo such as nucleic acid.