US4228152A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Polymers containing prostaglandin radicals, process for their preparation and use thereof
Assignee: Individual
•
Filing: 1978-11-14
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Granted: 1980-10-14
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Expires: 1998-11-14
Abstract
Abstract There are disclosed non-toxic polymers having a molecular weight between 1,000 and 1,500,000 and containing prostaglandin radicals directly connected or connected through an oxyalkylenic, aminoalkylenic, or oxyaminoalkylenic chain to a polyacrylic or polymethacrylic backbone. Upon entry of the polymer into the body, the prostaglandin radicals are hydrolyzed causing free prostaglandins to be released in the body. Methods for making the non-toxic polymers and therapeutic compositions containing the non-toxic polymers are also disclosed.
Inventors
- 👤 Paolo Ferruti
- 👤 Rodolfo Paoletti
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 22:02
CPC Classifications
C; C08; C08F; C08F8/00; C08F8/14; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; C08F8/10; C08F8/30; C08G; C08G81/00; C08G81/02
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
110 words
A non-toxic polymer having a molecular weight between 1,000 and 1,500,000 containing prostaglandin radicals bound to a polyacrylic or polymethacrylic backbone either directly or through oxyalkylenic, aminoalkylenic or oxyaminoalkylenic chains, said polymer containing units of the formula ##STR5## wherein R represents H or CH 3 , A represents an alkylene radical terminated at both ends with an --NH-- or --O-- group, n represents 0 or 1 in both occurences, B represents --OPg or --CO--Pg wherein Pg represents a prostaglandin residue, and D represents a divalent radical supplied by a comonomer selected from the group consisting of 1-acryloyl-4-methyl piperazine, N-acryloyl morpholine, N-vinyl pyrrolidone, divinylbenzene, methylene bisacrylamide, N,N'-bisacryloyl piperazine, N,N'-bisacryloyl N,N'-dimethylethylene diamine.
Claim 2
Dependent Claim
110 words
A non-toxic polymer having a molecular weight between 1,000 and 1,500,000 containing prostaglandin radicals bound to a polyacrylic or polymethacrylic backbone either directly or through oxyalkylenic, aminoalkylenic or oxyaminoalkylenic chains, said polymer containing units of the formula ##STR5## wherein R represents H or CH 3 , A represents an alkylene radical terminated at both ends with an --NH-- or --O-- group, n represents 0 or 1 in both occurences, B represents --OPg or --CO--Pg wherein Pg represents a prostaglandin residue, and D represents a divalent radical supplied by a comonomer selected from the group consisting of 1-acryloyl-4-methyl piperazine, N-acryloyl morpholine, N-vinyl pyrrolidone, divinylbenzene, methylene bisacrylamide, N,N'-bisacryloyl piperazine, N,N'-bisacryloyl N,N'-dimethylethylene diamine.
Claim 3
Dependent Claim
27 words
The non-toxic polymer of claim 1 wherein the radical A is derived from compounds selected from the group consisting of N,N-dihydroxy ethyl-1,3-propanediamine, ethanolamine, ethylene diamine and ethyleneglycol.
Claim 4
Dependent Claim
10 words
The process of claim 1 wherein said monomer is homopolymerized.
Claim 5
Dependent Claim
26 words
The process of claim 1 wherein said monomer is copolymerized with monomers selected from the group consisting of 1-acryloyl-4-methyl piperazine, N-acryloyl-morpholine, N-vinylpyrrolidone, divinylbenzene, methylenebisacrylamide, N,N'-bisacryloylpiperazine, N,N'-bisacryloyl-N,N'-dimethylethylenediamine.
Claim 6
Dependent Claim
44 words
A process for the preparation of the non-toxic polymer of claim 1 comprising polymerizing acrylic acid or methacrylic acid, reacting the resulting polymer with carbonyldiimidazole to introduce reactive imidazolic groups into the chain of the resulting polymer, and reacting the treated polymer with prostaglandins.
Claim 7
Dependent Claim
13 words
The process of claim 5 wherein acrylic acid or methacrylic acid is homopolymerized.
Claim 8
Dependent Claim
29 words
The process of claim 5 wherein acrylic acid or methacrylic acid are copolymerized with monomers selected from the group consisting of 1-acryloyl-4-methylpiperazine, N-acryloyl morpholine, N-vinylpyrrolidone, divinylbenzene, methylenebisacrylamido, N,N'-bisacryloylpiperazine, N,N'-bisacryloyl-N,N'-dimethylethylenediamine.
Claim 9
Dependent Claim
84 words
A process for the preparation of the non-toxic polymer of claim 1 containing prostaglandin radicals bound through oxyalkenic, aminoalkylenic or oxyaminoalkylenic chains to a macromolecular polyacrylic or polymethacrylic backbone comprising polymerizing a monomer selected from the group consisting of 1-acryloyl benzotriazole, 1-acryloyl methoxy benzotriazole, 1-acryloyl methylbenzotriazole, 1-acryloyl imidazole, N-acryloyl succinimide, and N-2,4,5-trichlorophenylacrylamide to form a macromolecular polymer backbone, reacting said backbone with a compound selected from the group consisting of an alkylenediamine, an hydroxyalkylamine, and a glycol, and reacting the resulting polymer with prostaglandin.
Claim 10
Dependent Claim
10 words
The process of claim 8 wherein said monomer is homopolymerized.
Claim 11
Dependent Claim
25 words
The process of claim 8 wherein said monomer is copolymerized with monomers selected from the group consisting of 1-acryloyl-4-methylpiperazine, N-acryloylmorpholine, N-vinylpyrrolidone, divinylbenzene, methylenebisacrylamide, N,N'-bisacryloylpiperazine, N,N'-bisacryloyl-N,N'-dimethylethylenediamine.
Claim 12
Dependent Claim
21 words
The process of claim 8 wherein said compound is selected from the group consisting of N,N-dihydroxy ethyl-1,3-propanediamine, ethanolamine, ethylenediamine and ethyleneglycol.
Claim 13
Dependent Claim
19 words
A therapeutic composition containing a therapeutically effective dose of the polymer of claim 1 and a pharamceutically acceptable carrier.
Claim 14
Dependent Claim
62 words
A process for the preparation of the non-toxic polymer of claim 1 comprising: polymerizing a monomer selected from the group consisting of 1-acryloyl benzotriazole, 1-acryloly methoxy benzotriazole, 1-acryloly methylbenzotriazole, and 1-acryloly imidazole, and reacting the resulting polymer with prostaglandins, with the proviso that when the resulting polymer is a polyacrylolybenzotriazole, the reaction with prostaglandins is carried out in the presence of triethylamine.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-10-14 | 1984-04-14 | 1984-10-14 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-10-14 | 1988-04-14 | 1988-10-14 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-10-14 | 1992-04-14 | 1992-10-14 | $7700.00 | Window Closed / Lapsed |