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US 2021/0261579 A1Published application
Prodrugs of naltrexone, nalmefene and derivatives thereof
AssigneeTaiwanj Pharmaceuticals Co., Ltd.
InventorsSyaulan S. YANG, Kuang Yuan LEE, Yan-Feng JIANG
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Abstract
A novel structure of an opioid antagonist is provided. One of the exemplary compounds of the present disclosure has the structure of Formula (II). The present disclosure overcomes the discomfort of conventional opioid antagonist due to rapid absorption and improves the patient compliance thereof.
Claims16
A compound according to formula (II), or a pharmaceutically acceptable salt, prodrug or solvate thereof:
- wherein:
- A has the following structure:
- X is CH2 or oxygen;
- R1, R2 or R3 is independently selected from the group consisting of H, C1-C20 alkyl, C2-C20 alkenyl, C2-C20 alkynyl, C3-C20 carbocyclyl, C6-C20 aryl, C1-C20 heterocyclyl and C1-C20 heteroaryl;
- R1, R2 or R3 is, independently, optionally substituted with one or more halogen, hydroxy, alkoxyl, CN, N3, N(Ra)(Rb), C(O)N(Ra)(Rb), N(Ra)C(O)N(Rb)(Rc), N(Ra)C(O)ORb, OC(O)N(Ra)(Rb), C(O)ORa, OC(O)ORa, C(O)Ra, OC(O)Ra, S(O)nRa, S(O)2N(Ra)(Rb) or N(Ra)S(O)2N(Rb)(Rc);
- Ra, Rb or Rc is independently selected from the group consisting of H, oxygen, C1-C10 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C8 carbocyclyl, C6-C20 aryl, C1-C20 heterocyclyl and C1-C20 heteroaryl;
- n=1, 2, or 3;
- R4 is H, methyl, allyl, or cyclopropyl methyl;
- and
- R5 is H or OH.
7 more elements
A compound according to formula (I), or a geometric isomer, enantiomer, diastereomer, racemate, atropisomer, pharmaceutically acceptable salt, prodrug or solvate thereof:
- wherein:
- X is CH2 or oxygen;
- R1, R2 or R3 is independently selected from the group consisting of H, C1-C20 alkyl, C2-C20 alkenyl, C2-C20 alkynyl, C3-C20 carbocyclyl, C6-C20 aryl, C1-C20 heterocyclyl and C1-C20 heteroaryl;
- R1, R2 or R3 is, independently, optionally substituted with one or more halogen, hydroxy, alkoxyl, CN, N3, N(Ra)(Rb), C(O)N(Ra)(Rb), N(Ra)C(O)N(Rb)(Rc), N(Ra)C(O)ORb, OC(O)N(Ra)(Rb), C(O)ORa, OC(O)ORa, C(O)Ra, OC(O)Ra, S(O)nRa, S(O)2N(Ra)(Rb) or N(Ra)S(O)2N(Rb)(Rc);
- Ra, Rb or Rc is independently selected from the group consisting of H, oxygen, C1-C10 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C8 carbocyclyl, C6-C20 aryl, C1-C20 heterocyclyl and C1-C20 heteroaryl;
- and
- n=1, 2, or 3.
4 more elements
Dependencies are inferred from the claim text.