(CN109942595) Oxygen bridge bicyclo-[2.2.1]-heptene compound containing different functional side chain structures, as well as preparation and application thereof 机翻标题: 暂无翻译,请尝试点击翻译按钮。

源语言标题
(CN109942595) Oxygen bridge bicyclo-[2.2.1]-heptene compound containing different functional side chain structures, as well as preparation and application thereof
公开号/公开日
CN109942595CN109942595 / 2020-08-252019-06-28
申请号/申请日
CN201910080724 / 2019-01-28
发明人
ZHOU HAIBINGWU SHUWENLAN KELI YUANYUANZHANG SILONGDONG CHUNE;
申请人
WUHAN UNIVERSITY;
主分类号
IPC分类号
A61K-031/343 A61K-031/4025 A61K-031/4525 A61P-005/32 A61P-035/00 C07D-493/08
摘要
(CN109942595) The invention discloses an oxygen bridge bicyclo-[2.2.1]-heptene compound containing different functional side chain structures, as well as preparation and application thereof. The preparation comprises the following steps that furan derivatives which contain different functional side chain structures (2,3-glycol butyl, N,N-diethoxy ethylamino, 2-pyrrolidinyl ethyl, 2-piperidine ethyl and alkyl acid) and are synthesized from 3,4-bis(4-methyoxy-phenyl)furan reacts with vinyl sulfonamide derivatives at 90 DEG C for 12 hours in one step without solvent or catalyst to prepare the oxygen bridge bicyclo-[2.2.1]-heptene compound containing basic side chains and other functional side chain groups. In-vitro experiments indicate that, compared with an existing anti-breast cancer drug tamoxifen, thenovel sulfamide type oxygen bridge bicyclo-[2.2.1]-heptene compound has stronger inhibiting activity on MCF-7 cells, and has excellent protein degrading activity and equivalent degrading performance as that of existing drug fulvestrant.
机翻摘要
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地址
代理人
(CN109942595B) PENG JINGSONG ; WUHAN KEHAO INTELLECTUAL PROPERTY ATTORNEYS (SPECIAL GENERAL PARTNERSHIP) Reg. Nb: 42222
代理机构
;
优先权号
2019CN-0080724
主权利要求
(CN109942595) 1.一类含有不同功能性侧链结构的氧桥双环-[2.2.1]-庚烯类化合物及其药学上可接受的盐,其特征在于,具有以下通式I或II所示的结构:     其中,   R1为CH2CH3、CH2CF3、Me;   R2为H、4-OCH3、4-Cl、4-CH3;   SC为(n=6或10);   所述化合物具体为:   6-(4-(2,3-二羟基丙氧基)苯基)-5-(4-羟基苯基)-N-(4-甲氧基苯基)-N-(2,2,2-三氟乙基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17b);   N-(4-氯苯基)-6-(4-(2,3-二羟基丙氧基)苯基)-5-(4-羟基苯基)-N-(2,2,2-三氟乙基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17c);   6-(4-(2-(二甲基氨基)乙氧基)苯基)-5-(4-羟基苯基)-N-(4-甲氧基苯基)-N-(2,2,2-三氟乙基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17d);   5-(4-羟基苯基)-N-(4-甲氧基苯基)-6-(4-(2-(吡咯烷-1-基)乙氧基)苯基)-N-(2,2,2-三氟乙基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17e);   5-(4-羟基苯基)-6-(4-(2-(哌啶-1-基)乙氧基)苯基)-N-(对甲苯基)-N-(2,2,2-三氟乙基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17f);   5-(4-羟基苯基)-N-(4-甲氧基苯基)-6-(4-(2-(哌啶-1-基)乙氧基)苯基)-N-(2,2,2-三氟乙基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17g);   5-(4-羟基苯基)-N-甲基-N-苯基-6-(4-(2-(哌啶-1-基)乙氧基)苯基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17h);   N-乙基-5-(4-羟基苯基)-N-苯基-6-(4-(2-(哌啶-1-基)乙氧基)苯基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17i);   11-(4-(6-(N-乙基-N-苯基氨磺酰基)-3-(4-羟基苯基)-7-氧桥双环[2.2.1]-2-庚烯)苯氧基)十一烷酸(17l);   7-(4-(3-(4-羟基苯基)-6-(N-(4-甲氧基苯基)-N-(2,2,2-三氟乙基)氨磺酰基)-7-氧桥双环[2.2.1]-2-庚烯)苯氧基)庚酸(17m);   11-(4-(3-(4-羟基苯基)-6-(N-(4-甲氧基苯基)-N-(2,2,2-三氟乙基)氨磺酰基)-7-氧桥双环[2.2.1]-2-庚烯)苯氧基)十一烷酸(17o);   N-乙基-5,6-双(4-羟基苯基)-N-(4-(2-(哌啶-1-基)乙氧基)苯基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰胺(17q);   11-(4-(N-乙基-5,6-双(4-羟基苯基)-7-氧桥双环[2.2.1]-5-庚烯-2-磺酰氨基)苯氧基)十一烷酸(17t)。 2.权利要求1所述的含有不同功能性侧链结构的氧桥双环-[2.2.1]-庚烯类化合物及其药学上可接受的盐在制备抗乳腺癌药物中的应用。 3.权利要求1所述的含有不同功能性侧链结构的氧桥双环-[2.2.1]-庚烯类化合物及其药学上可接受的盐在在制备降解雌激素受体的药物中的应用。 4.一种抗乳腺癌药物组合物,其特征在于,包含权利要求1所述的含有不同功能性侧链结构的氧桥双环-[2.2.1]-庚烯类化合物及其药学上可接受的盐和一种或多种药学上可接受的助剂。 5.一种降解雌激素受体的药物组合物,包含权利要求1所述的含有不同功能性侧链结构的氧桥双环-[2.2.1]-庚烯类化合物及其药学上可接受的盐和一种或多种药学上可接受的助剂。
法律状态
GRANTED
专利类型码
BA
国别省市代码
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