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US 10,865,186 B2Granted
Opioid agonists and uses thereof
AssigneeNektar Therapeutics
InventorsFranco J. Duarte, Neel K. Anand, Pankaj Sharma, Devendrapratap Singh
Life of this patent
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Abstract
Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
Claims11
A compound selected from the formula:
- wherein:
- R2 is an substituted alkyl;
- (i) R1 and R3 are taken together with their intervening atoms to form a fused, substituted thiazole and R5 is hydrogen, where R1 and R3 are positions 4 and 5 of the thiazole, wherein the thiazole is substituted with —X-POLY at position 2 of the thiazole;
- or
- (ii) R3 and R5 are taken together with their intervening atoms to form a fused, substituted thiazole and R1 is hydrogen, where R1 and R3 are positions 4 and 5 of the thiazole, wherein the thiazole is substituted with —X-POLY at position 2 of the thiazole;
- is a double bond;
- G is ═O;
- X is a spacer moiety selected from a covalent bond, —C(O)—, —NHC(O)—, —NH—, —CH2CHOHCH2NH—, and —O—;
- POLY is a poly(alkylene oxide) oligomer;
- or pharmaceutically acceptable salts thereof.
7 more elements
A compound, selected from
- (6S,10R,12R)-2-(2,5,8,11,14-pentaoxahexadecan-16-ylamino)-7-(cyclopropylmethyl)-10,12-dimethyl-7,8,9,10-tetrahydro-6,10-methanothiazolo[4′,5′:4,5]benzo[1,2-d]azocin-5(6H)-one;
- and
- (7S,11R,12R)-2-(2,5,8,11,14-pentaoxahexadecan-16-ylamino)-8-(cyclopropylmethyl)-11,12-dimethyl-8,9,10,11-tetrahydro-7,11-methanothiazolo[5′,4′:3,4]benzo[1,2-d]azocin-6(7H)-one;
- or pharmaceutically acceptable salts thereof.
1 more element
Dependencies are inferred from the claim text.