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Polymer derivatives having particular atom arrangements

A technology of atoms and atomic chains, applied in the field of new polymerization reagents, can solve problems such as short in vivo half-life conjugates and long in vivo half-life

Inactive Publication Date: 2011-01-19
NEKTAR THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thus, a relatively fast rate of hydrolysis can result in an unacceptably conjugate with too short a half-life in vivo, while a relatively slow hydrolysis can result in an unacceptably conjugate with a half-life in vivo that is too long

Method used

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  • Polymer derivatives having particular atom arrangements
  • Polymer derivatives having particular atom arrangements
  • Polymer derivatives having particular atom arrangements

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0306] Preparation of glycerol-based precursor molecules

[0307]

[0308] Glycerol-based precursor molecule (compound 8-02)

[0309] A solution of cis-1,3-O-benzylideneglycerol (7.2 g, 0.040 mole) (Sigma-Aldrich Corporation, St. Louis, MO) in toluene (100 mL) was azeotropically dried by distilling off the toluene. The dried compound was dissolved in anhydrous toluene (100ml), and a 1.0M solution of potassium tert-butoxide in tert-butanol (60ml, 0.060mol) and 1-(3-bromopropyl)-4-methyl- 2,6,7-Trioxabicyclo[2,2,2]octane (14.0 g, 0.0558 mol). The mixture was stirred overnight at 100°C in octane under argon atmosphere. The mixture was filtered, and the solvent was evaporated under reduced pressure to obtain 15.7 g of a solid product (Compound 5-02). NMR (d 6 -DMSO): 0.74ppm (s, 3H), 1.61ppm (m, 4H), 1.88ppm (m, 2H), 3.44ppm (t, 2H), 3.81ppm (s, 6H), 4.05ppm (m, 4H ), 5.55ppm (s, 1H), 7.37ppm (m, 5H).

[0310] The schematic representation of this reaction is as follows: ...

Embodiment 2

[0330] Preparation of "mPEG2 (40K) Butyric acid, N-hydroxysuccinimide ester"

[0331]

[0332] (where mPEG2 (20K) denotes PEG with a molecular weight of 20,000 Daltons)

[0333] "mPEG2 (40K) Butyric acid, N-hydroxysuccinimide ester"

[0334] Activation of hydroxyl groups in precursor molecules . Compound 8-02 (2.0 g, 0.0208 equivalents) was dissolved in anhydrous acetonitrile (50 ml), and anhydrous pyridine (2.2 ml, 0.272 moles) and N, N-disuccinimide carbonate (5.86 g , 0.0229 mol, DSC). The solution was stirred overnight at room temperature under an atmosphere of argon. Next, the mixture was filtered and the solvent was distilled off. The crude product was dissolved in CH 2 Cl 2 (50ml), and with 5% H 3 PO 4 Solution wash. The solution was then dried (MgSO 4 ), and the solvent was distilled off. The yield of the obtained product (compound 9-02) was 2.8 g. NMR (d 6 -DMSO): 1.76ppm (m, 2H), 2.35ppm (t, 2H), 2.82ppm (s, 8H), 3.56ppm (t, 2H), 3.58ppm (s...

Embodiment 3

[0351] Preparation of "mPEG2 (40K) - butyraldehyde"

[0352] Preparation of Tetra(Ethylene Glycol) Monobutyraldehyde, Diethyl Acetal

[0353] HO-(CH 2 CH 2 O) 4 CH 2 (CH 2 ) 2 -CH(OCH 2 CH 2 ) 2

[0354] A mixture of tetrakis(ethylene glycol) (97.1 g, 0.500 mol) and toluene (200 ml) was azeotropically dried by distilling off (rotary evaporator) toluene under reduced pressure. Dissolve the dried tetrakis(ethylene glycol) in anhydrous toluene (180ml), and add 1.0M potassium tert-butoxide in tert-butanol (120.0ml, 0.120mol) and 4-chlorobutyraldehyde diethyl acetal Aldehyde (18.1 g, 0.100 mole) (Alfa Aesar, Ward Hill, MA). The mixture was stirred overnight at 95-100°C under an atmosphere of argon. After cooling to room temperature, the mixture was filtered and the solvent was distilled off under reduced pressure. The crude product was dissolved in 1000 ml deionized water and the resulting solution was filtered through charcoal. Sodium chloride (100 g) was ad...

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Abstract

Polymeric reagents are provided comprising a moiety of atoms arranged in a specific order, wherein the moiety is positioned between a water-soluble polymer and a reactive group. The polymeric reagents are useful for, among other things, forming polymer-active agent conjugates. Related methods, compositions, preparations, and so forth are also provided.

Description

field of invention [0001] The present invention relates generally to novel polymeric reagents comprising specific internal structural orientations, and conjugates to these novel polymeric reagents. In addition, the present invention relates to methods of synthesizing polymeric reagents and methods of coupling polymeric reagents to active agents and other species. In addition, the invention relates to pharmaceutical formulations and methods of administering the conjugates to patients. Background of the invention [0002] Scientists and clinicians face many challenges in their attempts to develop active agents into forms suitable for delivery to patients. Active agents that are polypeptides, for example, are typically delivered by injection rather than the oral route. In this way, the polypeptide is introduced into the systemic circulation without exposure to the proteolytic environment of the stomach. However, injecting polypeptides has several disadvantages. For example,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48C08G65/333C08G65/329
CPCC08G65/329C08G65/33337C08G65/33344A61K47/48215A61K47/60A61P35/00A61K47/50C08G65/00C08G65/333
Inventor J·M·哈里斯A·科兹洛夫斯基S·P·麦克马纳斯M·D·本特利S·A·查尔斯
Owner NEKTAR THERAPEUTICS INC
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