公开(公告)号：US09580711B2

公开(公告)日：2017-02-28

申请号：US15146783

申请日：2016-05-04

Applicant: Arcturus Therapeutics, Inc.

Inventor： Joseph E. Payne ,  Padmanabh Chivukula ,  David Webb

IPC: C07J41/00 ,  C07C333/04 ,  C07C271/22 ,  C07C235/12 ,  C07C237/12 ,  A61K9/107 ,  C12N15/113 ,  C12N15/11 ,  A23D9/013 ,  A61K9/127

CPC classification number: C07C333/04 ,  A23D9/013 ,  A61K9/1075 ,  A61K9/1272 ,  A61K31/713 ,  C07C235/12 ,  C07C237/12 ,  C07C271/22 ,  C07J41/0055 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/14 ,  C12N2320/32

Abstract: What is described is a lipid particle comprising the compound of formula I wherein R1 consists of alkyl, alkenyl, alkynyl, or cholesteryl; R2 consists of alkyl or alkenyl; L1 consists of alkyl, alkylene or alkenyl; X1 consists of —O—(CO)— or —(CO)—O—; X2 consists of S or O; L2 consists of a bond or alkylene; R3 consists of alkylene; and R4 and R5 are the same or different, each consisting of alkyl; or a pharmaceutical preparation thereof.

Abstract translation: 描述的是式I的化合物，其中R 1由1-18个碳组成的直链或支链烷基，由2至12个碳组成的烯基或炔基或胆固醇基; R2由直链或支链烷基或由1至18个碳组成的烯基组成; L1由5至9个碳原子的直链烷基组成，或当R1由胆甾醇基组成时，则L1由直链亚烷基或由3至4个碳组成的烯基组成; X1由-O-（CO） - 或 - （CO）-O-组成; X2由S或O组成; L2由1至6个碳原子的键或直链亚烷基组成; R3由具有1至6个碳的直链或支链亚烷基组成; 并且R 4和R 5相同或不同，各自由1至6个碳的直链或支链烷基组成; 或其药学上可接受的盐。

公开(公告)号：US09365610B2

公开(公告)日：2016-06-14

申请号：US14707876

申请日：2015-05-08

Applicant: Arcturus Therapeutics, Inc.

Inventor： Joseph E. Payne ,  Padmanabh Chivukula ,  David Webb

IPC: C07J41/00 ,  C07C333/04 ,  C07C271/22 ,  C07C235/12 ,  C07C237/12 ,  C12N15/11 ,  A23D9/013 ,  A61K9/127 ,  A61K9/107

CPC classification number: C07C333/04 ,  A23D9/013 ,  A61K9/1075 ,  A61K9/1272 ,  A61K31/713 ,  C07C235/12 ,  C07C237/12 ,  C07C271/22 ,  C07J41/0055 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/14 ,  C12N2320/32

Abstract: What is described is a compound of formula I wherein R1 consists of a linear or branched alkyl consisting of 1-18 carbons, an alkenyl or alkynyl consisting of 2 to 12 carbons, or a cholesteryl; R2 consists of a linear or branched alkyl or an alkenyl consisting of 1 to 18 carbons; L1 consists of a linear alkyl consisting of 5 to 9 carbons or, when R1 consists of a cholesteryl then L1 consists of a linear alkylene or alkenyl consisting of 3 to 4 carbons; X1 consists of —O—(CO)— or —(CO)—O—; X2 consists of S or O; L2 consists of a bond or a linear alkylene of 1 to 6 carbons; R3 consists of a linear or branched alkylene with 1 to 6 carbons; and R4 and R5 are the same or different, each consisting of a linear or branched alkyl of 1 to 6 carbons; or a pharmaceutically acceptable salt thereof.

Abstract translation: 描述的是式I的化合物，其中R 1由1-18个碳组成的直链或支链烷基，由2至12个碳组成的烯基或炔基或胆固醇基; R2由直链或支链烷基或由1至18个碳组成的烯基组成; L1由5至9个碳原子的直链烷基组成，或当R1由胆甾醇基组成时，则L1由直链亚烷基或由3至4个碳组成的烯基组成; X1由-O-（CO） - 或 - （CO）-O-组成; X2由S或O组成; L2由1至6个碳原子的键或直链亚烷基组成; R3由具有1至6个碳的直链或支链亚烷基组成; 并且R 4和R 5相同或不同，各自由1至6个碳的直链或支链烷基组成; 或其药学上可接受的盐。

公开(公告)号：US20160244761A1

公开(公告)日：2016-08-25

申请号：US15146783

申请日：2016-05-04

Applicant: Arcturus Therapeutics, Inc.

Inventor： Joseph E. Payne ,  Padmanabh Chivukula ,  David Webb

IPC: C12N15/113

CPC classification number: C07C333/04 ,  A23D9/013 ,  A61K9/1075 ,  A61K9/1272 ,  A61K31/713 ,  C07C235/12 ,  C07C237/12 ,  C07C271/22 ,  C07J41/0055 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/14 ,  C12N2320/32

Abstract: What is described is a lipid particle comprising the compound of formula I wherein R1 consists of alkyl, alkenyl, alkynyl, or cholesteryl; R2 consists of alkyl or alkenyl; L1 consists of alkyl, alkylene or alkenyl; X1 consists of —O—(CO)— or —(CO)—O—; X2 consists of S or O; L2 consists of a bond or alkylene; R3 consists of alkylene; and R4 and R5 are the same or different, each consisting of alkyl; or a pharmaceutical preparation thereof.

Abstract translation: 描述的是包含式I化合物的脂质颗粒，其中R 1由烷基，烯基，炔基或胆固醇基组成; R2由烷基或烯基组成; L1由烷基，亚烷基或烯基组成; X1由-O-（CO） - 或 - （CO）-O-组成; X2由S或O组成; L2由键或亚烷基组成; R3由亚烷基组成; 并且R 4和R 5相同或不同，各自由烷基组成; 或其药物制剂。