US2019247318A1PendingUtilityA1

Proteinoid compounds, process of preparing same and uses thereof

Assignee: UNIV BAR ILANPriority: Aug 10, 2015Filed: Apr 22, 2019Published: Aug 15, 2019
Est. expiryAug 10, 2035(~9 yrs left)· nominal 20-yr term from priority
A61K 49/0056A61K 49/0093C08G 63/6852A61K 49/0034C08G 63/912A61K 49/0058A61K 49/0043A61K 9/5169A61K 49/0032A61K 38/00C08G 63/685
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Claims

Abstract

Proteinoid compounds characterized by a molecular weight (Mw) of at least 15,000 Da, processes of preparing such compounds and methods of use thereof, are provided. A method of monitoring the presence and metastases of cancer in a body of an individual is further disclosed.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A proteinoid compound comprising a polymeric backbone, wherein said polymeric backbone comprises monomeric units, each of said monomeric units being derived from an amino acid, and wherein said polymeric backbone is characterized by a molecular weight (Mw) of at least 15,000 Da. 
     
     
         2 . The proteinoid compound of  claim 1 , wherein said amino acid, in each instance, is selected from the group consisting of: Glu, Lys, Asp, Arg, Tyr, His, Ala, Phe, Cys, Ile, and p-amino benzoic acid. 
     
     
         3 . The proteinoid compound of  claim 1 , wherein said polymeric backbone further comprises polyester. 
     
     
         4 . The proteinoid compound of  claim 3 , wherein said polyester is selected from the group consisting of polylactide, polyglycolide, and polycaprolactone, polyhydroxyalkanoate. 
     
     
         5 . The proteinoid compound of  claim 1 , wherein said polymeric backbone is represented by the following formula [Phe] n [Arg] x [His] y [Lys] z [A 4 ]
 wherein:   A 4  represents a polyester or is absent;   n, x, y, and z are integers, independently, representing the total numbers of Phe, Arg, His, and Lys, respectively, in the polymeric backbone, such that n+x+y+z has a value of at least 100.   
     
     
         6 . The proteinoid compound of  claim 1 , wherein said polymeric backbone is represented by the following formula: [A 1 ] x [A 2 ] y [A 3 ] z [A 4 ]
 wherein:   a) A 1 , in each instance, is selected from Glu and Lys;   b) A 2 , and A 3  are each, independently, a monomeric unit derived from an amino acid or are each, independently, absent;   c) A 4  represents the polyester or is absent, and   d) x, y, and z are integers, independently, representing the total numbers of A 1 , A 2 , and A 3 , respectively, in said polymeric backbone, such that x+y+z has a value of at least 100.   
     
     
         7 . The proteinoid compound of  claim 6 , wherein said amino acid is selected from the group consisting of: Asp, Lys, Arg, and Phe. 
     
     
         8 . The proteinoid compound of  claim 6 , wherein said polyester is at least 1%, by weight, of the polymeric backbone. 
     
     
         9 . The proteinoid compound of  claim 6 , wherein A 1  is Glu, A 2  is Phe and A 3  is absent. 
     
     
         10 . The proteinoid compound of  claim 6 , wherein A 1  is Glu, A 2  is Asp, and A 3  is selected from the group consisting of Lys, Phe, or is absent. 
     
     
         11 . The proteinoid compound of  claim 6 , wherein A 1  is Glu, A 2  is Lys, and A 3  is Phe or is absent. 
     
     
         12 . The proteinoid compound of  claim 6 , wherein x, y, and z have a value such that at least one of: x/y, x/z, and y/z ranges from about 1:3 to about 3:1. 
     
     
         13 . The proteinoid compound of  claim 5 , wherein A 4  is absent. 
     
     
         14 . The proteinoid compound of  claim 5 , wherein A 4  is polylactide. 
     
     
         15 . The proteinoid compound of  claim 3 , wherein said polyester is at least 1%, by weight, of the polymeric backbone. 
     
     
         16 . A composition-of-matter comprising a plurality of the proteinoid compounds of  claim 1 . 
     
     
         17 . The composition-of-matter of  claim 16 , wherein at least 80% of said plurality of the proteinoid compound is characterized by a dispersity index (Ð) value of less than 1.1. 
     
     
         18 . The composition-of-matter of  claim 16 , further comprising one or more agents selected from: labeling compound, UV blocker, an antibacterial compound, a magnetite, an antioxidant, a filler, biologically active agent, said one or more agents being attached to and/or encapsulated within said hollowsphere. 
     
     
         19 . A method of monitoring the presence and metastases of cancer in a body of an individual, the method comprising administering to the individual the composition-of-matter of  claim 16 , and employing an imaging technique for monitoring a distribution of the composition-of-matter within the body or within a portion thereof. 
     
     
         20 . A process of synthesizing a proteinoid compound characterized by molecular weight (Mw) of at least 15,000 Da, the process comprising:
 a) heating one or more types of amino acid to a temperature that ranges from 100° C. to 200° C., under an inert gas, thereby forming a molten content or a mixture of said one or more amino acids;   b) stirring said molten content or a mixture at a temperature that ranges from 100° C. to 200° C., for at least 30 min, thereby polymerizing a plurality of monomeric units derived from said one or more amino acids in said content or mixture;   c) bringing the content or mixture to room temperature;   d) adding water to said content or a mixture, thereby obtaining a proteinoid compound solution; and   e) cleaning (e.g., dialyzing) said solution to thereby obtain the proteinoid compound.

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