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US 2019/0161490 A1Published application
Novel aryl ethene derivative and pharmaceutical composition containing same as active ingredient
AssigneeSung Yeoun Hwang
InventorsSung Yeoun HWANG, Sung Jin CHO, Jina KIM, Jungwook CHIN, Hayoung HWANG, In-Kyu LEE, Yong-Hyun JEON, Jaetae LEE, Jae-Han JEON, Sang Wook KIM
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Abstract
The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.
Claims10
An arylethene derivative represented by the following Chemical Formula 1, or a prodrug, solvate, stereoisomer, or pharmaceutically acceptable salt thereof:
- wherein
- L is (C6-C20)arylene, (C3-C20)heteroarylene, or (C3-C20) fused heterocycle;
- R1 is (C3-C20)heterocycloalkyl, (C3-C20)heteroaryl, —O—(CH2)m—R11, —(CH2)m—R12, —NH—(CH2)m—R13, —NHCO—(CH2)n—R14, or —SiR16R17—(CH2)m—R15;
- R11 to R15 are independently of one another (C3-C20)heterocycloalkyl;
- R16 and R17 are independently of each other (C1-C20)alkyl;
- m is an integer of 1 to 3;
- and
- n is an integer of 0 or 1;
- Ar is (C6-C20)aryl or (C3-C20)heteroaryl, in which the aryl or heteroaryl of Ar may be further substituted by one or more selected from the group consisting of hydroxy, halogen, (C1-C20)alkyl, halo(C1-C20)alkyl, (C1-C20)alkoxy, nitro, cyano, —NR21R22, (C1-C20)alkylcarbonyloxy, (C1-C20)alkylcarbonylamino, guanidino, —SO2—R23, and —OSO2—R24;
- R21 and R22 are independently of each other hydrogen, (C1-C20)alkylsulfonyl, or (C3-C20)cycloalkylsulfonyl;
- R23 and R24 are independently of each other (C1-C20)alkyl, halo(C1-C20)alkyl, or (C3-C20)cycloalkyl;
- R2 is hydroxy, halogen, (C1-C20)alkylcarbonyloxy, or (C1-C20)alkylsulfonyloxy;
- the heterocycloalkyl or heteroaryl of R1 and the heterocycloalkyl of R11 to R15 may be further substituted by one or more selected from the group consisting of (C1-C20)alkyl, (C3-C20)cycloalkyl, (C2-C20)alkenyl, amidino, (C1-C20)alkoxycarbonyl, hydroxy, hydroxy(C1-C20)alkyl, and di(C1-C20)alkylamino(C1-C20)alkyl;
- and
- the heterocycloalkyl and heteroaryl contains one or more heteroatoms selected from the group consisting of N, O and S, and the heterocycloalkyl is a saturated or unsaturated mono-, bi-, or spirocycle having a carbon atom or nitrogen atom in a ring as a binding site.
12 more elements
Dependencies are inferred from the claim text.