US 2006/0235161 A1Published application

PEG-polyacetal and PEG-polyacetal-POE graft copolymers and pharmaceutical compositions

OwnerJorge Heller, Etienne Schacht +1inventors

InventorsJorge Heller, Etienne Schacht, Veska Toncheva

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Abstract

The present invention provides graft copolymer delivery vehicle which comprises a polyethyleneglycol (PEG)-polyacetal (PA) copolymer or a polyethyleneglycol (PEG)-polyacetal (PA)-polyorthoester (POE) copolymer. The polyethyleneglycol-polyacetal graft copolymers or the polyethyleneglycol-polyacetal-polyorthoester graft copolymers, in particular, the PA-g-PEG or the PA-POE-g-PEG suitable for the invention are represented by Formulae I and V:

Claims94

Dependent claims

A graft copolymer of Formula I or Formula V:

wherein:
L is a linker comprising a backbone chain of 2-10 atoms comprising C, N, O, S, or P optionally interrupted with one or more —C(O)O—, —OC(O)—, —COS—, —SC(O)—, —C(S)O—, —CON—, —CONH—, —CONR′—, —NCO—, —NHCO—, —R′NCO—, —OCO2—, —OCON—, —OCONH—, —NCO2—, —NHCO2—, —OCONR′—, —R′NCO2—, —NCONH—, —NHCON—, —NHCONH—, —NR′CONH, —NR′CON—, —NHCONR′—, —NCONR′—, —NR′CONR′—, —CO—, —Ro—CO—Ro—, —Ro—, —Ro—CR2(NR—)—Ro—, —Ro—CR2(CONH—)—Ro—, —Ro—CR2(NHCO—)—Ro—, optionally substituted C2-C4 alkenes, or substituted C2-C4 alkynes, where each R′ is independently alkyl, substituted alkyl, aryl or substituted aryl groups;
m and n are independently integers from 2 to 500;
p and q are independently an integer from 5 to 100;
each Ro is independently C1-C4 alkylene;
R1 is C1-C4 alkyl;
R, R2 and R3 are each independently H or C1-C4 alkyl;
and
A, D and D′ are each independently selected from R4, R5, R6, and R7;
where:
R4 is
in which:
x is an integer from 0 to 10;
R8 is H or C1-C6 alkyl;
and
R9 is selected from
where m′ is an integer from 1 to 6,
s is an integer from 0 to 30,
t is an integer from 1 to 200, and
R10 and R11 are independently H or C1-C4 alkyl;
R5 is selected from:
where m′ is an integer from 1 to 6;
R6 is selected from:
where:
x is an integer from 0 to 30;
y is an integer from 1 to 200;
R10 R11 are independently H or C1-C4 alkyl;
R12 and R13 are independently C1-C12 alkylene;
R14 is H or C1-C6 alkyl;
and R15 is C1-C6 alkyl;
or R14 and R15 together are C3-C10 alkylene;
R16 is C1-C4 alkyl;
and
R7 is (i) the residue of a diol containing at least one amine functionality incorporated therein, or
(ii) the residue of a diol containing at least one functional group independently selected from amide, imide, urea, and urethane groups.

32 more elements

Dependencies are inferred from the claim text.

Facts

Application: 11/392,232Filed 28 Mar 2006
Priority: 31 Mar 2005
Published: 19 Oct 2006
Term ends: Not estimatedThe source records don’t support an estimate.

Classification16 codes

A61K 9/0048
Galenical forms characterised by the site of application: eye, e.g. artificial tears
A61K 9/0024
Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in…
A61K 47/34
Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates: macromolecular compounds obtained otherwise than by reactions only…
A61K 47/59
The modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule: obtained otherwise than by…

Family

Application60/667,710Us provisional application · filed 31 Mar 2005
US 2006/0235161 A1This patent

From the US filing history. Foreign family members aren’t listed.

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Abstract

A graft copolymer of Formula I or Formula V:

wherein:
L is a linker comprising a backbone chain of 2-10 atoms comprising C, N, O, S, or P optionally interrupted with one or more —C(O)O—, —OC(O)—, —COS—, —SC(O)—, —C(S)O—, —CON—, —CONH—, —CONR′—, —NCO—, —NHCO—, —R′NCO—, —OCO2—, —OCON—, —OCONH—, —NCO2—, —NHCO2—, —OCONR′—, —R′NCO2—, —NCONH—, —NHCON—, —NHCONH—, —NR′CONH, —NR′CON—, —NHCONR′—, —NCONR′—, —NR′CONR′—, —CO—, —Ro—CO—Ro—, —Ro—, —Ro—CR2(NR—)—Ro—, —Ro—CR2(CONH—)—Ro—, —Ro—CR2(NHCO—)—Ro—, optionally substituted C2-C4 alkenes, or substituted C2-C4 alkynes, where each R′ is independently alkyl, substituted alkyl, aryl or substituted aryl groups;
m and n are independently integers from 2 to 500;
p and q are independently an integer from 5 to 100;
each Ro is independently C1-C4 alkylene;
R1 is C1-C4 alkyl;
R, R2 and R3 are each independently H or C1-C4 alkyl;
and
A, D and D′ are each independently selected from R4, R5, R6, and R7;
where:
R4 is
in which:
x is an integer from 0 to 10;
R8 is H or C1-C6 alkyl;
and
R9 is selected from
where m′ is an integer from 1 to 6,
s is an integer from 0 to 30,
t is an integer from 1 to 200, and
R10 and R11 are independently H or C1-C4 alkyl;
R5 is selected from:
where m′ is an integer from 1 to 6;
R6 is selected from:
where:
x is an integer from 0 to 30;
y is an integer from 1 to 200;
R10 R11 are independently H or C1-C4 alkyl;
R12 and R13 are independently C1-C12 alkylene;
R14 is H or C1-C6 alkyl;
and R15 is C1-C6 alkyl;
or R14 and R15 together are C3-C10 alkylene;
R16 is C1-C4 alkyl;
and
R7 is (i) the residue of a diol containing at least one amine functionality incorporated therein, or
(ii) the residue of a diol containing at least one functional group independently selected from amide, imide, urea, and urethane groups.

32 more elements

Facts

Application

11/392,232Filed 28 Mar 2006

Priority

31 Mar 2005

Published

19 Oct 2006

Term ends

Not estimatedThe source records don’t support an estimate.

Classification16 codes

A61K 9/0048
Galenical forms characterised by the site of application: eye, e.g. artificial tears
A61K 9/0024
Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in…
A61K 47/34
Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates: macromolecular compounds obtained otherwise than by reactions only…
A61K 47/59
The modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule: obtained otherwise than by…