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US 10,577,346 B2Granted
Benzobicycloalkane derivatives, their preparation and pharmaceutical use thereof
AssigneesShanghai Haiyan Pharmaceutical Technology Co., Ltd., Yangtze River Pharmaceutical Group Co., Ltd.
InventorsFusheng Zhou, Shuchun Guo, Jinzhu Zhao, Hui Xu, Xia Shi, Yi Hu, Yufeng Li, Jiong Lan
Life of this patent
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Abstract
It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
Claims19
A compound of Formula (I), or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof:
- wherein,
- L is —CO— or —(C(R4R5)2)k—;
- k is 1, 2 or 3;
- X is —N(R1R2), —OR3 or —CH2O—((CH2)r—O)t—CH3;
- r is 2, 3 or 4;
- t is 1, 2, 3, 4, 5, 6, 7, 8 or 9;
- Ra and Rb are each independently hydrogen, methyl, —CHO, —C(O)OC1-10 alkyl or —C(O)C1-10 alkyl;
- R4 and R5 are each independently hydrogen or methyl;
- R1 and R2 are each independently hydrogen, C1-10 alkyl, C3-8 cycloalkyl, C6-10 aryl, 5 to 6 membered single heteroaryl ring, 4 to 6 membered saturated single heterocycle, spiro, spiroheterocycle, bridged ring, bridged heterocycle or —((CH2)n—O)m—CH3;
- wherein n is 2, 3 or 4;
- m is 1, 2, 3, 4, 5, 6, 7, 8 or 9;
- or R1 and R2, together with the nitrogen atom to which they are attached, form a 4 to 6 membered saturated single heterocycle;
- R3 is C1-10 alkyl, C3-8 cycloalkyl, —((CH2)p—O)q—CH3, —C(O)O—((CH2)p—O)q—CH3, —C(O)OC1-10 alkyl, —C(O)OC3-8 cycloalkyl, —C(O)C1-10 alkyl;
- wherein p is 2, 3 or 4;
- q is 1, 2, 3 or 4;
- and
- the alkyl, cycloalkyl, alkoxy, alkynyl, aryl, 4 to 6 membered saturated single heterocycle, 5 to 6 membered single heteroaryl ring, spiro, spiroheterocycle, bridged ring, and bridged heterocycle are unsubstituted or substituted with 1, 2 or 3 substituents selected from the group consisting of NRa0Rb0, halogen, acetyl, hydroxy, hydroxymethyl, hydroxyethyl, carboxyl, C1-8 alkyl, C1-8 alkoxy, halogenated C1-8 alkyl, C3-8 cycloalkyl, C3-8 cycloalkoxy, C2-10 alkenyl, C2-10 alkynyl, halogenated C1-8 alkoxy, C6-10 aryl, 4 to 6 membered saturated single heterocycle, —C(O)C1-10 alkyl, —C(O)OC1-10 alkyl, —OC(O)C1-10 alkyl, —CONRa0Rb0;
- and, Ra0 and Rb0 are each independently hydrogen, C1-8 alkyl, and C1-8 alkyl substituted with C1-8 alkoxy.
15 more elements
Dependencies are inferred from the claim text.