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| OF THE INVENTION A. THE PRODRUGS In most aspects of the invention, the prodrug compositions of the ... |
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| Non-antigenic amine derived polymers and polymer conjugates |
| In one aspect of the invention, there are provided amine-based polymer intermediates having the ... |
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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 |
| 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 |
| 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 |
| What is claimed is: 1. A pharmaceutical composition for enhancing rectal absorption of L-dopa by ... |
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Electrophilic polyethylene oxides for the modification of polysaccharides, polypeptides (proteins) and surfaces
| Details |
Inventors: Dolence, Eric Kurt; Hu, Chen-Ze; Tsang, Ray; Sanders, Clifton G.; Osaki, Shigemasa;
Assignee: Surface Engineering Technologies, Division of InnerDyne, Inc. (Salt Lake City, UT)
Primary Examiner: Krass; Frederick
Assistant Examiner:
Attorney, Agent or Firm: Lyon & Lyon LLP
Several poly(ethylene glycol) mixed carbonates and their preparation are closed. These carbonates are synthesized by conversion of polyethylene glycol first to the chloroformate then by reaction with the hydroxyl group of N-hydroxybenzotriazole or 2-hydroxypyrimidine or N-hydroxy-2-pyrrolidinone. These mixed carbonate analogs smoothly react with amino groups in aminoglycans and protein and amino containing surfaces to form stable, hydrolysis resistant carbamate linkages. |
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DETAILED DESCRIPTION The present invention provides for compounds having the formula: ##STR1## wherein R.
sub.
1 is selected from the group consisting of an N-benzotriazole group, an N-2-pyrrolidinone group, and an 2-oxypyrimidine group; R.
sub.
2, R.
sub.
3 and R.
sub.
4 are independently selected lower alkylene groups, preferably of about 2 to about 3 carbon atoms, and may be the same or different; R.
sub.
5 is selected from the group consisting of hydrogen, methyl, a carbonyloxy-N-benzotriazole group, a carbonyl-oxy-N-2-pyrrolidinone group, and a carbonyl-2-oxypyrimidine; a is an integer from 1 to 1000 and each of b and c is an integer from 0 to 1000, and a, b and c are selected so that the sum of a, b, and c is an integer between 3 and 1000.
Preferred are compounds of formula (I) wherein each of R.
sub.
2, R.
sub.
3 and R.
sub.
4 is independently --CH.
sub.
2 CH.
sub.
2 -- or --CH.
sub.
2 CH(CH.
sub.
3)-- or a combination thereof.
These compounds may be homobifunctional or hetereobifunctional and are suitable for modifying a variety of bioactive compounds as well as acting as a tether to link a bioactive compound to a membrane or polymeric surface.
According to a preferred aspect, the present invention further provides for the production of a modified bioactive compound such as a polysaccharide or polypeptide or other pharmaceutical that has conjugated to it via an urethane bond at least one molecule of polyoxyethylene having the structure: ##STR2## where R.
sub.
5 is selected from the group consisting of hydrogen, methyl, a carbonyloxy-N-benzotriazole group, a carbonyloxy-N-2-pyrrolidinone group, or a carbonyl-2-oxypyrimidine group, R.
sub.
2, R.
sub.
3 and R.
sub.
4 are ethylene, R.
sub.
6 is a bioactive compound selected from an aminoglycan polysaccharide, a polypeptide, a protein or other reactive pharmaceutical compound, and a, b, and c are as defied in connection with formula (I).
These modified bioactive compounds having covalently attached polyoxyalkylene groups have a variety of uses in vivo, since such substances may exhibit a reduced rate of kidney clearance and/or enhanced association with cells, and in certain instances decreased immunogenicity
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