US5238940A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Compositions for photodynamic therapy
Assignee: Novelion Therapeutics Inc
•
Filing: 1991-09-30
•
Granted: 1993-08-24
•
Expires: 2011-09-30
Abstract
Abstract Methods to prepare intermediates for the conjugation of active ingredients to hydrophilic carriers are described. The polyhydroxylated carriers are first derivatized to convert the hydroxyls to leaving groups and then reacted with an alkylene diamine in the presence of a reducing agent. The resulting derivatized carrier can then be coupled to substituents containing carboxyl groups in the presence of dehydrating agents.
Inventors
- 👤 Daniel Liu
- 👤 Frank Jiang
- 👤 John Hobbs
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 03:53
CPC Classifications
A; A61; A61K; A61K41/00; A61K41/0057; A61K41/0071; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/61
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
113 words
A method to prepare a conjugate of a pharmaceutically active compound with a hydrophilic, water-soluble, multifunctional polymeric carrier, said carrier having a multiplicity of hydroxy substituents, which method comprises: contacting said carrier with a molar excess of an electrophile donor effective to convert said hydroxyl moieties to leaving groups; followed by treating said carrier having said converted hydroxyls with an alkylene diamine in the presence of a metal hydride reducing agent in approximately equimolar amount to the alkylene diamine to obtain an alkylene diamine-derivatized carrier; followed by coupling said alkylene diamine-derivatized carrier with a pharmaceutically active compound containing carboxyl substituents to obtain a pharmaceutically active conjugate of said carrier with said active compound.
Claim 2
Independent Claim
113 words
A method to prepare a conjugate of a pharmaceutically active compound with a hydrophilic, water-soluble, multifunctional polymeric carrier, said carrier having a multiplicity of hydroxy substituents, which method comprises: contacting said carrier with a molar excess of an electrophile donor effective to convert said hydroxyl moieties to leaving groups; followed by treating said carrier having said converted hydroxyls with an alkylene diamine in the presence of a metal hydride reducing agent in approximately equimolar amount to the alkylene diamine to obtain an alkylene diamine-derivatized carrier; followed by coupling said alkylene diamine-derivatized carrier with a pharmaceutically active compound containing carboxyl substituents to obtain a pharmaceutically active conjugate of said carrier with said active compound.
Claim 3
Dependent Claim
14 words
The method of claim 1 wherein said pharmaceutically active compound is a green porphyrin.
Claim 4
Dependent Claim
14 words
The method of claim 1 wherein said hydrophilic water-soluble multifunctional carrier is polyvinyl alcohol.
Claim 5
Dependent Claim
13 words
The method of claim 1 wherein said electrophile donor is 2-fluoro-1-methylpyridinium toluene-4-sulfonate (FMP).
Claim 6
Dependent Claim
12 words
The method of claim 1 wherein said reducing agent is sodium borohydride.
Claim 7
Dependent Claim
12 words
The method of claim 1 wherein said reducing agent is sodium borohydride.
Claim 8
Dependent Claim
29 words
The method of claim 1 wherein the hydrophilic, water-soluble, multifunctional carrier is polyvinyl alcohol; the electrophile donor is 2-fluoro-1-methylpyridiniumtoluene-4-sulfonate; and wherein said pharmaceutically active compound is a porphyrin-type photosensitizer.
Claim 9
Dependent Claim
13 words
The method of claim 7 wherein said porphyrin-type photosensitizer is a green porphyrin.
References Cited (Backward Citations)
US4268947A
Cited
US4500507A
Cited
EP0161606A2
Cited
US4577636A
Cited
US4512762A
Cited
US4748120A
Cited
US4727027A
Cited
US4485806A
Cited
US4675338A
Cited
US4753958A
Cited
EP0276121A2
Cited
US4883790A
Cited
US5095030A
Cited
US5093349A
Cited
WO1990002747A1
Cited
US5053423A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-08-23 | 1997-02-22 | 1997-08-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-08-23 | 2001-02-22 | 2001-08-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-08-23 | 2005-02-22 | 2005-08-24 | $7700.00 | Window Closed / Lapsed |