US2004253206A1PendingUtilityA1
Drug-oligomer conjugates
Priority: Sep 13, 1999Filed: Mar 29, 2004Published: Dec 16, 2004
Est. expirySep 13, 2019(expired)· nominal 20-yr term from priority
A61P 35/00A61P 43/00A61P 35/04A61P 35/02A61K 47/50A61K 47/60
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Claims
Abstract
Drug-oligomer conjugates and pharmaceutical compositions prepared therefrom. Methods of making and using the drug-oligomer conjugates and pharmaceutical compositions.
Claims
exact text as granted — not AI-modifiedWe claim:
1 . A conjugate comprising:
(a) at least one therapeutic compound; and (b) one or more PEG polymers and/or oligomers, each joined to a bonding site on the therapeutic compound by a hydrolyzable bond, said PEG polymers and/or oligomers each:
(i) comprising a straight or branched PEG segment consisting of 1 to 25 polyethylene glycol units; and
(ii) comprising a salt-forming moiety.
2 . The conjugate of claim 1 , wherein the conjugate is a prodrug.
3 . The conjugate of claim 1 , wherein the straight or branched PEG segment consists of from 2 to 20 polyethylene glycol units.
4 . The conjugate of claim 1 , wherein the polyethylene glycol oligomer has a number of polyethylene glycol units selected from the group consisting of 1, 2, 3, 4, 5, 6, 7, 8, and 9.
5 . The conjugate of claim 1 , wherein the salt-forming moiety is selected from the group consisting of: ammonium, carboxylate, phosphate, sulfate and mesylate.
6 . The conjugate of claim 1 , wherein the therapeutic compound is derivatized by from 1 up to the maximum number of sites of attachment for the polyethylene glycol oligomer(s).
7 . The conjugate of claim 1 , which, when delivered via the oral route of administration to treat a mammalian subject having a disease condition responsive to the therapeutic compound, provides a therapeutically effective dose of the therapeutic compound to the blood.
8 . The conjugate of claim 1 , wherein the therapeutic compound is a peptide.
9 . The conjugate of claim 1 , wherein the therapeutic compound is a protein.
10 . A pharmaceutical composition comprising:
(a) a conjugate of claim 1; and (b) a pharmaceutically acceptable carrier.
11 . The pharmaceutical composition of claim 10 , wherein the conjugate is a prodrug.
12 . The pharmaceutical composition of claim 10 in a form suitable for oral administration.
13 . A conjugate comprising a therapeutic compound joined by hydrolysable bond(s) to one or more PEG oligomer(s) selected from the group consisting of:
wherein n is from 1 to 7, m is from 2 to 25, and R is hydrogen or lower alkyl;
wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, and R is hydrogen or lower alkyl;
wherein n is from 1 to 6, m and r are each independently from 2 to 25, and R is hydrogen or lower alkyl;
wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25 and R is hydrogen or lower alkyl;
wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, R is hydrogen or lower alkyl, and X − is a negative ion;
wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, and R 1 and R 2 are each independently hydrogen or lower alkyl;
wherein n is from 1 to 6, p is from 2 to 8 and m is from 2 to 25;
wherein n and p are each independently from 1 to 6, m is from 2 to 25 and X 30 is a positive ion;
wherein n is from 1 to 5, m is from 2 to 25, X − is a negative ion, and wherein R 1 and R 2 are each independently hydrogen or lower alkyl;
wherein n is from 1 to 6, m is from 2 to 25 and X − is a negative ion; and
wherein n is from 1 to 12, m is from 2 to 25, p is from 2 to 12, X 30 is a positive ion and Z − is a negative ion.
14 . The conjugate of claim 13 , wherein the conjugate is a prodrug.
15 . The conjugate of claim 13 , wherein the therapeutic compound is derivatized by from 1 up to the maximum number of sites of attachment for the polyethylene glycol oligomer(s).
16 . The conjugate of claim 13 , wherein the therapeutic compound is a peptide.
17 . The conjugate of claim 13 , wherein the therapeutic compound is a protein.
18 . A pharmaceutical composition comprising:
(a) a conjugate of claim 13; and (b) a pharmaceutically acceptable carrier.
19 . The pharmaceutical composition of claim 18 , wherein the conjugate is a prodrug.
20 . The pharmaceutical composition of claim 18 in a form suitable for oral administration.
21 . A method of treating a mammalian subject having a disease condition responsive to a therapeutic compound, said method comprising administering to the subject of an effective disease treating amount of a conjugate comprising:
(a) at least one therapeutic compound; and (b) one or more PEG polymers and/or oligomers, each joined to a bonding site on the therapeutic compound by a hydrolyzable bond, said PEG polymers and/or oligomers each:
(i) comprising a straight or branched PEG segment consisting of 1 to 25 polyethylene glycol units; and
(ii) comprising a salt-forming moiety.
22 . The method of claim 21 , wherein the conjugate is a prodrug.
23 . The conjugate of claim 21 , wherein the therapeutic compound is a peptide.
24 . The conjugate of claim 21 , wherein the therapeutic compound is a protein.
25 . A method of treating a mammalian subject having a disease condition responsive to a therapeutic compound, said method comprising administering to the subject of an effective disease treating amount of a conjugate comprising the therapeutic compound joined by hydrolyzable bond(s) to one or more PEG oligomer(s) selected from the group consisting of:
wherein n is from 1 to 7, m is from 2 to 25, and R is hydrogen or lower alkyl;
wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, and R is hydrogen or lower alkyl;
wherein n is from 1 to 6, m and r are each independently from 2 to 25, and R is hydrogen or lower alkyl;
wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25 and R is hydrogen or lower alkyl;
wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, R is hydrogen or lower alkyl, and X − is a negative ion;
wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, and R 1 and R 2 are each independently hydrogen or lower alkyl;
wherein n is from 1 to 6, p is from 2 to 8 and m is from 2 to 25;
wherein n and p are each independently from 1 to 6, m is from 2 to 25 and X 30 is a positive ion;
wherein n is from 1 to 5, m is from 2 to 25, X − is a negative ion, and wherein R 1 and R 2 are each independently hydrogen or lower alkyl;
wherein n is from 1 to 6, m is from 2 to 25 and X − is a negative ion; and
wherein n is from 1 to 12, m is from 2 to 25, p is from 2 to 12, X 30 is a positive ion and Z − is a negative ion.
26 . The method of claim 25 , wherein the conjugate is a prodrug.
27 . The conjugate of claim 25 , wherein the therapeutic compound is a peptide.
28 . The conjugate of claim 25 , wherein the therapeutic compound is a protein.Join the waitlist — get patent alerts
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