公开(公告)号：EP1461014A2

公开(公告)日：2004-09-29

申请号：EP02788510.2

申请日：2002-12-04

申请人： Ben Gurion University Of The Negev Research And Development Authority

发明人： HELDMAN, Eliahu ,  LINDER, Charles ,  GRINBERG, Sarina ,  KOLOT, Victoria ,  SHAUBI, Eleonora

IPC分类号： A61K9/127 ,  C07D303/00 ,  C07C233/00

CPC分类号： C07D401/04 ,  A61K9/1272 ,  C07C219/06 ,  C07C233/36 ,  C07C235/28 ,  C07C237/10 ,  C07D303/46 ,  C07H7/00 ,  C07H15/10 ,  C07H15/26

摘要： An amphiphilic compound is provided capable of forming vesicles or liposomes, said amphiphilic compound having at least one headgroup containing a selectively cleavable group or moiety such as a residue of a choline or phenylalanine derivative, and at least one hydrogen-bonding group located either within said headgroup and/or in close proximity thereto. The cleavable group or moiety is cleaved under selective conditions including change of chemical, physical or biological environment and is preferably cleaved enzymatically in a biological environment such as the brain or the blood. Vesicles or liposomes made from said amphiphilic compounds are suitable for delivery of a therapeutic substance or a diagnostic agent specifically to a target organ or tissue, or for delivery of a nucleic acid for gene therapy.

公开(公告)号：EP1360168A2

公开(公告)日：2003-11-12

申请号：EP02716274.2

申请日：2002-01-16

申请人： Ben Gurion University Of The Negev Research And Development Authority

发明人： GRINBERG, Sarina ,  LINDER, Charles ,  WIESMAN, Zeev ,  HELDMAN, Eliahu ,  KOLOT, Victoria

IPC分类号： C07C69/76

CPC分类号： C07C247/12 ,  A61K8/14 ,  A61K8/41 ,  A61K8/416 ,  A61K8/42 ,  A61K8/46 ,  A61K8/4926 ,  A61K8/922 ,  A61K9/0014 ,  A61K9/1075 ,  A61K9/1272 ,  A61K47/18 ,  A61K47/24 ,  A61Q19/00 ,  C07C69/675 ,  C07C69/732 ,  C07C229/12 ,  C07C229/22 ,  C07C235/28 ,  C07C301/00 ,  C07D213/53 ,  C07D303/04 ,  C07D303/48 ,  C07D407/12 ,  C07F9/65505

摘要： Amphiphilic derivatives composed of at least one fatty acid chain are derived from natural vegetable oils such as vernonia oil, lesquerella oil and castor oil, in which the several reactive groups such as epoxy, hydroxy and double bonds can be modified to polar and ionic groups. The head group of the amphiphilic derivative may be in the main fatty acid chain or in a side chain. The amphiphiles are useful for the formation of vesicles and micelles and for use as complexants and surfactants.