 Non-antigenic amine derived polymers and polymer conjugates |
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| Biodegradable high molecular weight polymeric linkers and their conjugates |
| The present invention includes compounds of the formula: (D).sub.n --M--(R.sub.1).sub.m (I) wherein ... |
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| Modified polypeptides with high activity and reduced allergenicity |
| OF THE INVENTION The modified polypeptide of the present invention is represented by the formula: A... |
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| Poly(ethylene glycol) derivatives with proximal reactive groups |
| OF THE INVENTION The terms "group," "functional group," "moiety," "active moiety," "reactive site,"... |
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| Devices for cloaking transplanted cells |
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| Terminally-branched polymeric linkers and polymeric conjugates containing the same |
| In one aspect of the invention, compounds of Formula (I) are provided: ##STR6## wherein: J is ##STR7... |
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| Rectally absorbable form of L-dopa |
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| Rectally absorbable form of L-dopa |
| What is claimed is: 1. A method of enhancing the rate of absorption of a rectally administered ... |
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| Rectally absorbable form of L-dopa |
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| Method to treat Parkinsons disease |
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Poly(ethylene glycol) and related polymers monosubstituted with propionic or butanoic acids and functional derivatives thereof for biotechnical applications
| Details |
Inventors: Harris, J. Milton; Kozlowski, Antoni;
Assignee: Shearwater Polymers, Inc. (Huntsville, AL)
Primary Examiner: Krass; Frederick
Assistant Examiner:
Attorney, Agent or Firm: Bell, Seltzer, Park & Gibson, P.A.
Active esters of PEG acids and related polymers are provided that have a single propionic or butanoic acid moiety and no other ester linkages. These polymer acids have a half life in water of from about 10 to 25 minutes. For example, alpha-methoxy, omega-propionic acid succinimidyl ester of PEG ("methoxy-PEG-SPA") has a nearly ideal reactivity with amino groups on proteins and other biologically active substances. The half life of methoxy-PEG-SPA is about 16.5 minutes in water. The invention also provides conjugates with proteins, enzymes, polypeptides, drugs, dyes, nucleosides, oligonucleotides, lipids, phospholipids, liposomes, and surfaces of solid materials that are compatible with living organisms, tissue, or fluid. |
|
DETAILED DESCRIPTION OF THE INVENTION The following examples are given to illustrate the invention, but should not be considered in limitation of the invention: Example 1--Synthesis of CH.
sub.
3 O--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 CO.
sub.
2 --NHS Example 2--Synthesis of CH.
sub.
3 O--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 --S--CH.
sub.
2 CH.
sub.
2 CO.
sub.
2 --NHS Example 3--Synthesis of CH.
sub.
3 O--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 CH.
sub.
2 CO.
sub.
2 --NHS Example 4--Rates of hydrolysis of PEG-NHS active esters Example 5--Synthesis of HO--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 --S--CH.
sub.
2 CH.
sub.
2 --CO.
sub.
2 H Example 6--Synthesis of HO--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 --S--CH.
sub.
2 CH.
sub.
2 --CO.
sub.
2 --NHS Example 7--Synthesis CH.
sub.
2 .
dbd.
CH--CO.
sub.
2 (CH.
sub.
2 CH.
sub.
2 O).
sub.
n CH.
sub.
2 CH.
sub.
2 --S--CH.
sub.
2 CH.
sub.
2 CO.
sub.
2 --NHS Example 8--Synthesis CH.
sub.
2 .
dbd.
CHCH.
sub.
2 O--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n CH.
sub.
2 CH.
sub.
2 S --CH.
sub.
2 CH.
sub.
2 CO.
sub.
2 NHS Example 9--Synthesis of HO--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 O).
sub.
n --NHCOCH.
sub.
2 CH.
sub.
2 CO.
sub.
2 C (CH.
sub.
3).
sub.
3 Example 10--Synthesis of H.
sub.
2 N--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n CH.
sub.
2 CH.
sub.
2 --S--CH.
sub.
2 CH.
sub.
2 CO.
sub.
2 H Example 11--Synthesis of HO--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 CO.
sub.
2 H Example 12--Synthesis of H.
sub.
2 N--CH.
sub.
2 CH.
sub.
2 O(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 CO.
sub.
2 H Example 13--Synthesis of (CH.
sub.
3).
sub.
3 C--O--CONH--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --S --CH.
sub.
2 CH.
sub.
2 COOH Example 14--Synthesis of (CH.
sub.
3).
sub.
3 C--O--CONH--(CH.
sub.
2 CH.
sub.
2 O).
sub.
n --CH.
sub.
2 CH.
sub.
2 COOH Example 15--.
alpha.
-methoxy-.
omega.
-dipalmitoylphosphatidylethanolamide of propionic acid of PEG (a "PEG-phospholipid") Example 16--.
alpha.
-methoxy-.
omega.
-distearoylphosphatidylethanolamide of propionic acid of PEG (a "PEG"-phospholipid) Example 17--Synthesis of HS--CH.
sub.
2 CH.
sub.
2 CONH--(CH.
sub.
2 CH.
sub.
2 O)
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