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US 11,111,214 B2Granted
Kappa opioid agonists and uses thereof
AssigneeNektar Therapeutics
InventorsNeel K. Anand, Franco J. Duarte, Wen Zhang, Zhongxu Ren
Life of this patent
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Abstract
Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof: The compounds of Formula I described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
Claims14
A compound according to Formula I:
- wherein:
- R1 is an optionally substituted phenyl;
- R2 is hydrogen;
- R3 is selected from hydrogen and an optionally substituted alkyl;
- R4 is an optionally substituted phenyl;
- R5 and R6 taken together with the nitrogen to which they are attached form a pyrrolidinyl or azetidinyl ring substituted with —X-POLY;
- X is an optional linker selected from a covalent bond;
- —C(O)NH—;
- —C(O)NHCH2—;
- —C(O)NHCH2CH2—;
- —OC(O)NH—;
- —C(O)NH—;
- —O—;
- —NHC(O)—;
- —NHC(O)CH2—;
- —NHC(O)CH2(O)—;
- —NHC(O)CH2CH2—;
- or —NHS(O)2—;
- and
- POLY is a poly(alkylene oxide) oligomer comprising 2 to 10 alkylene oxide monomers;
- or pharmaceutically acceptable salts and solvates thereof.
18 more elements
A compound having the structure:
- wherein R10 is selected from the group consisting of ˜H, ˜OCH2CH2OH, ˜OCH2CH2OCH3, ˜NHCH2CH2OH, and ˜NHCH2CH2OCH3,
- X is an optional linker selected from a covalent bond;
- —C(O)NH—;
- —C(O)NHCH2—;
- —C(O)NHCH2CH2—;
- —OC(O)NH—;
- —C(O)NH—;
- —O—;
- —NHC(O)—;
- and —NHC(O)CH2—;
- POLY is a poly(alkylene oxide) oligomer comprising 2 to 10 alkylene oxide monomers, or pharmaceutically acceptable salts and solvates thereof.
8 more elements
A compound having the following structure:
- wherein:
- n is an integer of from 1 to 30;
- R10 is selected from the group consisting of ˜H, ˜OCH2CH2OH, ˜OCH2CH2OCH3, ˜NHCH2CH2OH, and ˜NHCH2CH2OCH3;
- R11 is selected from the group consisting of ˜H, ˜CH3, and ˜CF3, and pharmaceutically acceptable salts and solvates thereof.
1 more element
Dependencies are inferred from the claim text.