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US 2026/0049060 A1Published application
Tetrahydroisoquinolinylmethylbenzamide compounds
AssigneeNational Health Research Institutes
InventorsShau-Hua Ueng, Shiu-Hwa Yeh, Chuan Shih
Life of this patent
Estimating the term…
Abstract
Disclosed are tetrahydroisoquinoline compounds useful for treating an opioid receptor-associated condition including pain, immune disease, esophageal reflux, diarrhea, anxiety, or heroin addiction. Also provided are pharmaceutical compositions and treatment methods.
Claims20
A compound of Formula (II):
- in which
- each of R1 to R4, independently, is H, halo, cyano, amino, nitro, thio, C1-6 alkyl, or C1-6 alkoxy;
- R5 is C1-6 alkyl, C3-8 cycloalkyl, or C1-6 alkenyl;
- R6 is C1-6 alkyl, C3-8 cycloalkyl, C2-8 heterocycloalkyl, C6-14 aryl, C6-14 cycloalkylaryl, C6-14 aralkyl, C2-13 heteroaryl, or 6 to 16-membered heterocycloalkylaryl;
- each of R11 to R16, independently, is H, halo, hydroxyl, cyano, amino, nitro, thio, carboxyl, C1-6 alkyl, or C1-6 alkoxy;
- R17 is H, C1-6 alkyl, C3-8 cycloalkyl, or C1-6 alkenyl;
- X is absent, H, or CR18R19R20, or X and R6, together with the carbon atoms they bond to, form a five or six-membered cycloalkyl- or heterocycloalkyl-fused phenyl, or X and R24, together with the carbon atoms they bond to, form cyclopropylene;
- each of R18 to R20, independently, is H, halo, hydroxyl, thio, cyano, amino, nitro, carboxyl, C1-6 alkyl, or C1-6 alkoxy;
- R24 is absent, H, halo, hydroxyl, cyano, amino, nitro, thio, carboxyl, C1-6 alkyl, C3-8 cycloalkyl, or C1-6 alkoxy;
- each of amino, thio, alkyl, alkoxy, and alkenyl is unsubstituted or substituted with one or more of halo, hydroxyl, thio, cyano, amino, nitro, carboxyl, and aryl;
- each of cycloalkyl, heterocycloalkyl, cycloalkylaryl, aralkyl, heteroaryl, heterocycloalkylaryl, and cyclopropylene is unsubstituted or substituted with one or more of halo, hydroxyl, thio, cyano, amino, nitro, carboxyl, alkyl, alkoxy, and aryl;
- aryl is unsubstituted or substituted with one or more of halo, thio, cyano, amino, nitro, carboxyl, alkyl, and aryl;
- each of the five or six-membered cycloalkyl- or heterocycloalkyl-fused phenyl is unsubstituted or substituted with one or more of halo, hydroxyl, thio, cyano, amino, nitro, carboxyl, alkyl, alkoxy, and aryl;
- each of m and n, independently, is 0 or 1;
- and
- is a single bond or double bond.
13 more elements
A compound of Formula (IV):
- in which
- each of R1 to R4, R7 to R16, and R24, independently, is H, halo, hydroxyl, cyano, amino, nitro, thio, carboxyl, C1-6 alkyl, or C1-6 alkoxy;
- R5 is C1-6 alkyl, C3-8 cycloalkyl, or C1-6 alkenyl;
- R17 is H, C1-6 alkyl, C3-8 cycloalkyl, or C1-6 alkenyl;
- X is S, CR18R19, or NR18;
- Y is a bond or CR21R22;
- each of R18, R19, R21, and R22, independently, is H, halo, hydroxyl, thio, cyano, amino, nitro, carboxyl, C1-6 alkyl, or C1-6 alkoxy;
- each of amino, thio, alkyl, alkoxy, alkenyl, and cycloalkyl, independently, is unsubstituted or substituted with one or more of halo, hydroxyl, thio, cyano, amino, nitro, carboxyl, alkyl, alkoxy, and aryl, and
- is a single bond or double bond.
6 more elements
The method of 18, wherein the opioid receptor-associated condition is pain, immune disease, esophageal reflux, diarrhea, anxiety, or heroin addiction.
Dependencies are inferred from the claim text.