阅读说明：本技术 用于治疗三阴性乳腺癌的喹啉衍生物 (Quinoline derivatives for the treatment of triple negative breast cancer ) 是由 田心 吕鹏 杨玲 王祥建 张喜全 王善春 王训强 江海 于 2019-03-13 设计创作，主要内容包括：本发明提供了一种用于治疗三阴性乳腺癌的喹啉衍生物,及其在制备用于肿瘤治疗的药物组合物的用途。具体而言,本发明涉及喹啉衍生物1-[[[4-(4-氟-2-甲基-1H-吲哚-5-基)氧基-6-甲氧基喹啉-7-基]氧基]甲基]环丙胺在治疗三阴性乳腺癌中的用途,(I)。<Image he="328" wi="366" file="734280DEST_PATH_IMAGE001.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"></Image>(The invention provides a quinoline derivative for treating triple negative breast cancer and application thereof in preparing a pharmaceutical composition for treating tumors. In particular, the invention relates to quinoline derivatives 1- [ [ [4- (4-fluoro-2-methyl-1H-indol-5-yl) oxy-6-methoxyquinolin-7-yl]Oxy radical]Methyl radical]Use of cyclopropylamine in the treatment of triple negative breast cancer, (I).)

Use of compound I or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for the treatment of triple negative breast cancer,

the use of claim 1, wherein the triple negative breast cancer is advanced or metastatic triple negative breast cancer.

The use of any one of claims 1-2, wherein the triple negative breast cancer is a triple negative breast cancer with failed prior therapy; preferably, the triple negative breast cancer is the triple negative breast cancer which fails to be treated by radiotherapy and/or chemotherapy medicaments.

Use according to any one of claims 1 to 3, characterized in that the pharmaceutically acceptable salt thereof is a salt of compound I with any of the following acids: hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, acetic acid, trifluoroacetic acid, propionic acid, hexanoic acid, heptanoic acid, cyclopentanepropionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, succinic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1, 2-ethanedisulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, p-chlorobenzenesulfonic acid, p-toluenesulfonic acid, 3-phenylpropionic acid, trimethylacetic acid, tert-butylacetic acid, dodecylsulfuric acid, gluconic acid, glutamic acid, hydroxynaphthoic acid, salicylic acid, stearic acid; preferably in the form of the hydrochloride or maleate salt, more preferably the dihydrochloride salt.

The use according to any one of claims 1 to 4, wherein the medicament is a formulation suitable for any one of oral, parenteral, intraperitoneal, intravenous, intraarterial, transdermal, sublingual, intramuscular, rectal, transbuccal, intranasal, inhalation, vaginal, intraocular, topical, subcutaneous, intralipid, intraarticular, intraperitoneal or intrathecal administration; preferably a formulation suitable for oral administration; further preferably a tablet, capsule, powder, granule, dripping pill, paste or powder, more preferably a tablet or capsule.

The use according to any one of claims 1 to 5, wherein the compound I or the pharmaceutically acceptable salt thereof is administered in a daily dose of 3 mg to 30 mg, preferably 5 mg to 20 mg, more preferably 8mg to 16 mg, even more preferably 8mg to 14 mg, most preferably 8mg, 10mg or 12 mg.

The use according to any one of claims 1 to 6, wherein the Compound I or the pharmaceutically acceptable salt thereof is administered at intervals between a dosing period and a rest period; the ratio of the administration period to the withdrawal period in days is preferably 2: 0.5-5, more preferably 2: 0.5-3, even more preferably 2: 0.5-2, and still more preferably 2: 0.5-1; as a further preferred mode of administration at intervals, one of the following modes is used: stopping the drug for 2 weeks after 2 weeks of continuous administration, for 1 week after 2 weeks of continuous administration, or for 2 days after 5 days of continuous administration; the intermittent administration mode may be repeated a plurality of times.

A method of treating triple negative breast cancer, comprising administering to a patient in need thereof a therapeutically effective amount of Compound I, or a pharmaceutically acceptable salt thereof,