US2019247388A1PendingUtilityA1
Oligomer-opioid agonist conjugates
Est. expiryMar 12, 2027(~0.6 yrs left)· nominal 20-yr term from priority
A61P 25/00A61K 31/439A61K 31/402A61K 31/4468A61K 31/485C07D 489/02A61K 47/60A61K 47/10A61K 31/4025
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Claims
Abstract
The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound comprising a residue of an opioid agonist covalently attached to a water-soluble, non-peptidic oligomer.
2 . The compound of claim 1 , wherein the opioid agonist is a kappa opioid agonist.
3 . The compound of claim 1 , wherein the opioid agonist is a mu opioid agonist.
4 . The compound of claim 1 , having the following structure:
wherein:
R 2 is H or OH;
R 3 is H or an organic radical;
R 4 is H or an organic radical;
the dotted line (“---”) represents an optional double bond;
Y 1 is O or S;
R 5 is selected from the group consisting of
wherein R 6 is an organic radical;
X is a spacer moiety;
POLY is a water-soluble, non-peptidic oligomer.
5 . The compound of claim 1 , having the following structure:
wherein:
R 1 is H or an organic radical;
R 2 is H or OH;
R 3 is H or an organic radical;
R 4 is H or an organic radical;
the dotted line (“---”) represents an optional double bond;
Y 1 is O or S;
X is a spacer moiety; and
POLY is a water-soluble, non-peptidic oligomer.
6 . The compound of claim 1 , having the following structure:
wherein:
R 1 is H or an organic radical;
R 2 is H or OH;
R 3 is H or an organic radical;
R 4 is H or an organic radical;
Y 1 is O or S; and
R 5 is selected from the group consisting of
wherein R 6 is an organic radical;
X is a spacer moiety; and
POLY is a water-soluble, non-peptidic oligomer.
7 . The compound of claim 1 , having the following structure:
wherein:
R 1 is H or an organic radical;
R 2 is H or OH;
R 3 is H or an organic radical;
R 4 is H or an organic radical;
the dotted line (“---”) represents an optional double bond;
Y 1 is O or S;
R 5 is selected from the group consisting of
wherein R 6 is an organic radical;
X is a spacer moiety; and
POLY is a water-soluble, non-peptidic oligomer.
8 . The compound of claim 1 , having the following structure:
wherein:
R 1 is H or an organic radical;
R 3 is H or an organic radical;
R 4 is H or an organic radical;
the dotted line (“---”) represents an optional double bond;
Y 1 is O or S; and
R 5 is selected from the group consisting of
wherein R 6 is an organic radical;
X is a spacer moiety; and
POLY is a water-soluble, non-peptidic oligomer.
9 . The compound of claim 1 , wherein the opioid agonist is selected from the group consisting of asimadoline, bremazocine, enadoline, ethylketocyclazocine, GR89,696, ICI204448, ICI197067, PD117,302, nalbuphine, pentazocine, quadazocine (WIN 44,441-3), salvinorin A, spiradoline, TRK-820, U50488, and U69593.
10 . A compound corresponding to a structure selected from the group consisting of Formula I-Cb, Formula I-Cc, Formula I-Cd, and Formula I-Ce, wherein
R 1 is H R 2 is H or OH; R 3 is H or an organic radical; R 4 is H or an organic radical; R 5 is selected from the group consisting of
wherein R 6 is an organic radical;
the dotted line (“---”) represents an optional double bond;
Y 1 is O or S;
X is a spacer moiety; and
POLY is a water-soluble, non-peptidic oligomer.
11 . A compound of claim 10 , wherein Y is O.
12 . A compound of claim 10 , wherein R 2 is OH.
13 . A compound of claim 10 , wherein R 2 is H.
14 . A compound of claim 10 , wherein R 3 is selected from the group consisting of H, unsubstituted alkyl, cycloalkyl-substituted alkyl, and allyl.
15 . A compound of claim 10 , wherein R 4 is H.
16 . A compound of claim 10 , wherein R 5 is selected from the group consisting of
17 . A compound of claim 10 , wherein the optional double bond is present.
18 . A compound of claim 10 , wherein the optional double bond is not present.
19 . The compound of claim 1 , wherein the water-soluble, non-peptidic oligomer is a poly(alkylene oxide).
20 . The compound of claim 19 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).
21 . The compound of claim 1 , wherein the water-soluble, non-peptidic oligomer is made of between 1 and 30 monomers.
22 . The compound of claim 21 , wherein the water-soluble, non-peptidic oligomer is made of between 1 and 10 monomers.
23 . The compound of claim 19 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.
24 . The compound of claim 1 , wherein a single water-soluble, non-peptidic oligomer is attached to the residue of the opioid agonist.
25 . The compound of claim 1 , wherein the residue of the opioid agonist is covalently attached via a stable linkage.
26 . The compound of claim 1 , wherein the residue of the opioid agonist is covalently attached via a degradable linkage.
27 . The compound of claim 1 , wherein the linkage is an ether linkage.
28 . A composition comprising a compound comprising a residue of an opioid agonist covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer, and optionally, a pharmaceutically acceptable excipient.
29 . A composition of matter comprising a compound comprising a residue of an opioid agonist covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer, wherein the compound is present in a dosage form.
30 . A method comprising covalently attaching a water-soluble, non-peptidic oligomer to an opioid agonist.
31 . A method comprising administering a compound comprising a residue of an opioid agonist covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer.
32 . A method comprising binding mu opioid receptors, wherein said binding is achieved by administering a compound comprising a residue of an opioid agonist covalently attached to a water-soluble, non-peptidic oligomer.
33 . A method comprising binding kappa opioid receptors, wherein said binding is achieved by administering a compound comprising a residue of an opioid agonist covalently attached to a water-soluble, non-peptidic oligomer.Join the waitlist — get patent alerts
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