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US 2024/0199632 A1Published application
Briarane compounds and use their use
AssigneesNational Health Research Institutes, National Sun Yat-Sen University, National Museum of Marine Biology & Aquarium
InventorsLun Kelvin Tsou, Guang-Hao Niu, Hsing-Pang Hsieh, Mingzi Zhang, Zhi-Hong Wen, Ping-Jyun Sung
Life of this patent
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Abstract
Disclosed are compounds compound of Formula (I): Each variable is defined herein. Also included are pharmaceutical compositions containing such a compound and a method of treating an inflammatory condition.
Claims21
A compound of Formula (I):
- in which
- R1 is C1-C6 alkyl;
- R2 is C1-C6 alkyl, formyl, carboxyl, —CH═N—ORa, —CH═NRa, or —C(O)NH—O—Ra, in which Ra is H, C1-C6 alkyl, C2-C6 alkynyl, or C1-C6 heterocycloalkyl;
- R3 is H, hydroxy, or combined with R4, and R4 is H or C1-C6 alkyl;
- when R3 and R4 are combined, they together with the two carbon atoms attached thereto form an epoxide ring;
- R5 is N3, methyl, or combined with X2, and when R5 and X2 are combined, they are N and, together with the carbon atoms attached thereto, form a heterocycloalkyl ring;
- R6 is H, halo, oxo, hydroxyl, ═NRb, ═N—NH—C(O)Rc, —OC(O)Rd, or —O—S(O)2Re, in which Rb is hydroxyl, C1-C6 alkoxy, or C1-C10 heterocycloalkyl, Rc is C1-C6 alkyl, C3-C6 cycloalkyl, 5 or 6-membered heterocycloalkyl, phenyl, or 5- or 6-membered heteroaryl, Rd is C3-C6 cycloalkyl, C2-C10 alkenyl, C1-C10 aminoalkyl, C3-C10 alkynylalkyl, C1-C10 heterocyclylalkyl, or phenyl, and Re is amino or C1-C6 alkyl;
- R7 is H or acetyloxy;
- X1 is hydroxyl or oxo;
- X2 is O or N, when X2 is N, it is combined with R5;
- each of is a single bond or a double bond;
- alkyl is unsubstituted or substituted with one or more groups selected from hydroxyl, amino, CN, aryl, heteroaryl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 carboxylate, and C1-C6 heterocycloalkyl;
- each of amino, aminoalkyl, alkenyl, alkoxy, cycloalkyl, alkynylalkyl, heterocyclylalkyl, heterocycloalkyl, heteroaryl, and phenyl, is unsubstituted or substituted with one or more groups selected from hydroxyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 carboxylate, C1-C6 heterocycloalkyl, aryl, heteroaryl, and aryl-amino-alkyl-aminocarbonyl.
10 more elements
Dependencies are inferred from the claim text.