US2015038472A1PendingUtilityA1

Use of therapeutically effective lipids and method for producing organ-/tissue-specific therapeutically effective lipids

Assignee: PAT GMBHPriority: Sep 21, 2005Filed: Oct 21, 2014Published: Feb 5, 2015
Est. expirySep 21, 2025(expired)· nominal 20-yr term from priority
A61P 1/16A61K 49/0021A61K 31/685A61K 49/0052A61K 47/554A61K 31/683
52
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Claims

Abstract

The use of therapeutically active lipids for organ/tissue-specific enrichment for the treatment of inflammatory, ischemic or degenerative disorders and/or for stimulating a regeneration is arranged and developed such that the lipids are bound on application to carrier molecules for which cell-specific uptake systems in the cells of the organs and/or tissue exist. In addition, a method of producing organ/tissue-specific therapeutically active lipids for treatment of inflammatory, ischemic or degenerative disorders and/or stimulation of a regeneration, in particular for treating inflammatory liver disorders, is claimed, which is arranged and developed such that lysophosphatidylethanolamine (LysoPE) is coupled to the carboxyl group of ursodeoxycholate (UrsoDOCA) converted to an ester to give a LysoPE-DOCA compound.

Claims

exact text as granted — not AI-modified
That which is claimed is: 
     
         1 . Lysophospholipid which is covalently bonded to bile acids or asialoglycoptoteins. 
     
     
         2 . The lysophospholipid of  claim 1 , wherein said lysophospholipid is lyso-phosphatidylcholine or lysophosphatidlyethanolamine. 
     
     
         3 . The lysophospholipid of  claim 1 , wherein said bile acid is ursodeoxycholate or deoxycholate. 
     
     
         4 . The lysophospholipid of  claim 1 , wherein the lysophospholipid, which is covalently bonded to bile acids or asialoglycoptoteins comprises a hepatocytic-specifically recognized ligand and is absorbed by an absorption system of cells of a liver. 
     
     
         5 . The lysophospholipid of  claim 4 , wherein the absorption system is a Na+/taurocholate co-transporting polypeptide (NCTP-transporter protein). 
     
     
         6 . The Lysophospholipid of  claim 4 , wherein said lysophospholipid can be released from the ligand after being absorbed into the cells. 
     
     
         7 . A LysoPE-DOCA-compound obtainable by coupling lysophosphatidyl ethanolamine (LysoPE) to a carboxyl group of ursodeoxycholate (UrsoDOCA) converted into an ester to form a LysoPE-DOCA-compound. 
     
     
         8 . The LysoPE-DOCA-compound of  claim 7 , wherein the lysophospholipid is released from ursodeoxycholate after being absorbed into cells. 
     
     
         9 . The LysoPE-DOCA-compound of  claim 7  and a pharmaceutically acceptable carrier. 
     
     
         10 . A method of treating inflammatory, ischaemic or degenerative liver diseases and/or to stimulate regeneration of liver organ/tissue cells, said method comprising applying a lysophospholipid which is covalently bonded to bile acids or asialoglycoptoteins to a subject in need thereof. 
     
     
         11 . The method of  claim 10 , wherein said Lyso-phospholipid is Lyso-phosphatidylcholine or Lysophosphatidlyethanolamine. 
     
     
         12 . The method of  claim 10 , wherein said bile acid is ursodeoxycholate or deoxycholate. 
     
     
         13 . The method of  claim 10 , wherein the lysophospholipid which is covalently bonded to bile acids or asialoglycoptoteins comprises a hepatocytic-specifically recognized ligand and is absorbed by an absorption system of cells of a liver. 
     
     
         14 . The method of  claim 13 , wherein the absorption system is a Na+/taurocholate co-transporting polypeptide (NCTP-transporter protein). 
     
     
         15 . The method of  claim 13 , wherein said lysophospholipid can be released from the ligand after being absorbed into the cells. 
     
     
         16 . The method of  claim 11 , wherein applying the lysophospholipid occurs by at least one of direct, inhalation, drop-wise, oral, intravenous, or intraperitoneal application.

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