公开(公告)号：US20170246197A1

公开(公告)日：2017-08-31

申请号：US15430715

申请日：2017-02-13

申请人： Vascular Biogenics Ltd.

发明人： Gideon HALPERIN ,  Eti KOVALEVSKI-ISHAI

IPC分类号： A61K31/685 ,  A61K9/48 ,  A61K9/00

CPC分类号： A61K31/685 ,  A61K9/0053 ,  A61K9/48 ,  A61K31/661 ,  C07F9/106 ,  C07F9/1411

摘要： Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids, are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorus-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby. Further disclosed is substantially pure 1-hexadecyl-2-(4′-carboxy)butyl-sn-glycero-3-phosphocholine (CI-201).

公开(公告)号：US20130190523A1

公开(公告)日：2013-07-25

申请号：US13796654

申请日：2013-03-12

申请人： Vascular Biogenics Ltd.

发明人： Gideon HALPERIN ,  Eti KOVALEVSKI-ISHAI

IPC分类号： C07B41/00 ,  C07C67/39 ,  C07C51/16 ,  C07F9/09 ,  C07C29/48 ,  C07C45/27

CPC分类号： C07B41/00 ,  C07C29/48 ,  C07C41/26 ,  C07C45/27 ,  C07C45/29 ,  C07C51/16 ,  C07C51/29 ,  C07C67/08 ,  C07C67/28 ,  C07C67/39 ,  C07F9/091 ,  C07F9/10 ,  C07F9/106 ,  Y02P20/55

摘要： Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorous-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates firmed thereby.

摘要翻译： 公开了高度适用于治疗有益的氧化磷脂的工业制备的新型合成路线。 特别地，公开了用于有效制备具有连接到甘油主链上的甘油主链和一个或多个氧化部分的化合物的新方法，其没有进行柱层析。 进一步公开的是将含有磷的部分例如磷酸酯部分引入具有甘油主链的化合物和由此确认的中间体的新方法。

公开(公告)号：US20130158283A1

公开(公告)日：2013-06-20

申请号：US13709198

申请日：2012-12-10

申请人： Vascular Biogenics Ltd.

发明人： Gideon HALPERIN ,  Eti Kovalevski-Ishai

IPC分类号： C07F9/10 ,  C07C41/26 ,  C07C51/29 ,  C07C67/28 ,  C07C67/08 ,  C07C45/29

CPC分类号： C07B41/00 ,  C07C29/48 ,  C07C41/26 ,  C07C45/27 ,  C07C45/29 ,  C07C51/16 ,  C07C51/29 ,  C07C67/08 ,  C07C67/28 ,  C07C67/39 ,  C07F9/091 ,  C07F9/10 ,  C07F9/106 ,  Y02P20/55

摘要： Novel synthetic routes, which are highly applicable for industrial preparation of therapeutically beneficial oxidized phospholipids are disclosed. Particularly, novel methods for efficiently preparing compounds having a glycerolic backbone and one or more oxidized moieties attached to the glycerolic backbone, which are devoid of column chromatography are disclosed. Further disclosed are novel methods of introducing phosphorous-containing moieties such as phosphate moieties to compounds having glycerolic backbone and intermediates formed thereby.

摘要翻译： 公开了高度适用于治疗有益的氧化磷脂的工业制备的新型合成路线。 特别地，公开了用于有效制备具有连接到甘油主链上的甘油主链和一个或多个氧化部分的化合物的新方法，其没有进行柱层析。 进一步公开的是将含有磷的部分例如磷酸酯部分引入具有甘油主链的化合物和由其形成的中间体的新方法。