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MetAP-2 inhibitor polymersomes for therapeutic administration
US9446140B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9446140-B2 |
| Application number | US-201414313020-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 24, 2014 |
| Priority date | Jun 26, 2007 |
| Publication date | Sep 20, 2016 |
| Grant date | Sep 20, 2016 |
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Abstract
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The present invention provides methods to treating inflammation related disease and disorders such as an autoimmune disease and autoimmune related uveitis by administering compositions and formulations comprising MetAP-2 inhibitors as disclosed herein. The composition comprises a formulation of a fumagillol derivative that retains anti-inflammation activity and is associated with a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety.
First claim
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The invention claimed is: 1. A method of treating an autoimmune disease in a subject in need thereof, the method comprising orally administering a formulation comprising micelles comprised of a fumagillol derivative having anti-inflammation activity, wherein the fumagillol derivative is covalently associated with a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety, wherein said hydrophilic moiety is a poly(ethylene glycol) (PEG) polymer and said hydrophobic polymer moiety of said block copolymer is poly(d,L-lactic acid) (PLA). 2. The method of claim 1 , wherein said fumagillol derivative comprises a derivative selected from the group consisting of 6-O—(N-chloroacetylcarbamoyl) fumagillol (TNP-470), 6-O-(4-methoxyaniline)acetyl fumagillol; 6-O-(3,4, 5-trimethexyaniline)acetyl fumagillol; 6-O-(4-(N,N-dimethylethoxy) aniline)acetyl fumagillol; 6-O-(cyclopropylamino) acetyl fumagillol; 6-O-(cyclobutylamino)acetyl fumagillol; 4-((cyclopropylamino)acetyl) oxy-2-(1,2-epoxy-1,5 20 dimethyl-4-hexenyl)-3-methoxy-1-chloromethyl-1 cyclohexanol; 4-((cyclobutylamino)acetyl) oxy-2-(1,2-epoxy-1,5 dimethyl-4-hexenyl)-3-methoxy-1-chloromethyl-1-cyclohexanol. 3. The method of claim 1 , wherein said fumagillol derivative is covalently linked to said hydrophobic polymer moiety of said block copolymer. 4. The method of claim 1 , wherein the autoimmune disease results in inflammation of the eye. 5. The method of claim 4 , wherein the inflammation is uveitis. 6. A method of treating autoimmune uveitis in a subject in need thereof, the method comprising orally administering a formulation comprising micelles comprised of a fumagillol derivative having anti-proliferation activity and anti-inflammation activity, wherein the fumagillol derivative is covalently associated with a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety, wherein said hydrophilic moiety is a poly(ethylene glycol) (PEG) polymer and said hydrophobic polymer moiety of said block copolymer is poly(d,L-lactic acid) (PLA). 7. The method of claim 6 , wherein said fumagillol derivative comprises a derivative selected from the group consisting of 6-O—(N-chloroacetylcarbamoyl) fumagillol (TNP-470), 6-O-(4-methoxyaniline)acetyl fumagillol; 6-O-(3,4, 5-trimethexyaniline)acetyl fumagillol; 6-O-(4-(N,N-dimethylethoxy) aniline)acetyl fumagillol; 6-O-(cyclopropylamino) acetyl fumagillol; 6-O-(cyclobutylamino)acetyl fumagillol; 4-((cyclopropylamino)acetyl) oxy-2-(1,2-epoxy-1,5 20 dimethyl-4-hexenyl)-3-methoxy-1-chloromethyl-1 cyclohexanol; 4-((cyclobutylamino)acetyl) oxy-2-(1,2-epoxy-1,5 dimethyl-4-hexenyl)-3-methoxy-1-chloromethyl-1-cyclohexanol. 8. The method of claim 6 , wherein said fumagillol derivative is covalently linked to said hydrophobic polymer moiety of said block copolymer.
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Classifications
Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title
Immunosuppressants, e.g. drugs for graft rejection · CPC title
Antioedematous agents; Diuretics · CPC title
Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers · CPC title
Anorexiants; Antiobesity agents · CPC title
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Frequently asked questions
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- What does patent US9446140B2 cover?
- The present invention provides methods to treating inflammation related disease and disorders such as an autoimmune disease and autoimmune related uveitis by administering compositions and formulations comprising MetAP-2 inhibitors as disclosed herein. The composition comprises a formulation of a fumagillol derivative that retains anti-inflammation activity and is associated with a block copoly…
- Who is the assignee on this patent?
- Children'S Medical Center Corp
- What technology area does this patent fall under?
- Primary CPC classification A61K47/60. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Sep 20 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).