CN105622562A - 一种治疗心脑血管疾病的药物组合物 - Google Patents

一种治疗心脑血管疾病的药物组合物 Download PDF

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CN105622562A
CN105622562A CN201610114417.XA CN201610114417A CN105622562A CN 105622562 A CN105622562 A CN 105622562A CN 201610114417 A CN201610114417 A CN 201610114417A CN 105622562 A CN105622562 A CN 105622562A
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cerebrovascular diseases
cardiovascular
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pharmaceutical composition
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CN105622562B (zh
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张宏业
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Dongguan Asia Pharmaceutical Technology Co ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • C07D311/26—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3
    • C07D311/28—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only
    • C07D311/30—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 

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Abstract

本发明涉及一种治疗心脑血管疾病的药物组合物，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：

Description

一种治疗心脑血管疾病的药物组合物
技术领域
本发明涉及医药领域，具体的说，本发明涉及一种治疗心脑血管疾病的药物组合物。
背景技术
心脑血管意外是一种严重威胁人类，特别是50岁以上中老年人健康的常见病，即使应用最先进、完善的治疗手段，仍可有50％以上的脑血管意外幸存者生活不能完全自理。全世界每年死于心脑血管疾病的人数高达1500万人，居各种死因首位。心脑血管疾病己成为人类死亡病因最高的头号杀手，也是人们健康的“无声凶煞”。心脑血管疾病主要原因就是血管壁平滑肌细胞非正常代谢造成的，血管组织和人体的其他组织在一定周期内完成新陈代谢的过程，但是由于新的细胞组织不能正常的形成，使血管壁本身存在“缺陷”因此就容易产生炎症血管收缩不畅，就像是一条破烂不堪的旧管道，随时都有阻塞或破裂的可能。
发明内容
本发明的目的在于提供一种治疗心脑血管疾病的药物组合物。
为了实现本发明的目的，本发明提供一种治疗心脑血管疾病的化合物，该化合物具有下列结构：
本发明还提供一种治疗心脑血管疾病的药物组合物，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
优选地，所述药学上可接受的载体为稀释剂、崩解剂、粘合剂、润滑剂、稳定剂或矫正剂。
优选地，所述稀释剂为糖衍生物、淀粉衍生物或纤维素衍生物。
优选地，所述稀释剂为乳糖。
优选地，所述药物组合物为散剂、微粒剂、颗粒剂、胶囊剂或片剂。
本发明还提供化合物在制备治疗心脑血管疾病的药物中的用途，该化合物具有下列结构：
本发明的化合物对于心脑血管疾病的效果显著，可以开发成临床上有效的新的药物组合物。
具体实施方式
以下通过具体实施方式的描述对本发明作进一步说明，但这并非是对本发明的限制，本领域技术人员根据本发明的基本思想，可以做出各种修改或改进，但是只要不脱离本发明的基本思想，均在本发明的范围之内。
目标化合物：
实验例
选取清洁级SD大鼠120只，体重180-220g，雌雄各半，将大鼠适应性喂养7天后，尾静脉取血，检测血脂水平，排除非健康实验动物对实验结果的影响，并根据体重、性别将大鼠随机分为4组后分笼饲养，分别为正常组、模型组、阳性药组、目标化合物组，每组30只。除了正常组给予普通饲料喂养外，其余各组大鼠首先给予维生素D370万IU/kg，3天内灌胃(正常组给予同等体积的生理盐水)，然后饲以高脂饲料(重量％)：胆固醇1％、丙基硫氧嘧啶0.61％，牛胆酸钠0.35％，猪油5％，基础饲料93.04％，饲养8周，以造成血脂异常动物模型。
造模后第3天开始给药，各组给药量如下：阳性药组，阿托伐他汀溶液0.09mg/ml，给予灌胃1mL/100g体重；目标化合物组，0.02g的目标化合物加1000mL生理盐水配制成混悬液，给予灌胃1mL/100g体重。1次/日，连续给药20d。
各组的大鼠用25％乌拉坦3ml/kg腹腔注射麻醉，30分钟后，将各组大鼠分别背部固定，剖开腹腔，腹主动脉取血5m1做血脂指标。腹主动脉取血5m1，离心机5000转/min离心10min，制备血清。采用天冬氨酸转氨酶(AST)活性检测试剂盒(Sigma-Aldrich)检测AST。
结果见下表。
组别 AST(U/L)
正常组 81.36±6.52
模型组 253.51±12.51
阳性药组 193.72±9.69
目标化合物组 216.52±11.06
与正常组比较，模型组及各治疗组AST含量均显著升高；与模型组比较，治疗后AST含量明显下降，说明均具有治疗效果。

Claims (7)

1.一种治疗心脑血管疾病的化合物，其特征在于，该化合物具有下列结构：
2.一种治疗心脑血管疾病的药物组合物，其特征在于，所述药物组合物包含有效量的化合物和药学上可接受的载体，所述化合物具有下列结构：
3.根据权利要求2所述的治疗心脑血管疾病的药物组合物，其特征在于，所述药学上可接受的载体为稀释剂、崩解剂、粘合剂、润滑剂、稳定剂或矫正剂。
4.根据权利要求3所述的治疗心脑血管疾病的药物组合物，其特征在于，所述稀释剂为糖衍生物、淀粉衍生物或纤维素衍生物。
5.根据权利要求4所述的治疗心脑血管疾病的药物组合物，其特征在于，所述稀释剂为乳糖。
6.根据权利要求3所述的治疗心脑血管疾病的药物组合物，其特征在于，所述药物组合物为散剂、微粒剂、颗粒剂、胶囊剂或片剂。
7.化合物在制备治疗心脑血管疾病的药物中的用途，其特征在于，该化合物具有下列结构：
CN201610114417.XA 2016-03-01 2016-03-01 一种治疗心脑血管疾病的药物组合物 Active CN105622562B (zh)

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101475552A (zh) * 2009-02-09 2009-07-08 沈阳药科大学 羟基黄酮衍生物及其抗血小板聚集的用途
CN102285951A (zh) * 2011-09-13 2011-12-21 辽宁亿灵科创生物医药科技有限公司 木犀草素衍生物及其预防和治疗心血管疾病的用途
CN103408525A (zh) * 2013-08-13 2013-11-27 商洛学院 一种黄酮类化合物的合成方法及其应用

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101475552A (zh) * 2009-02-09 2009-07-08 沈阳药科大学 羟基黄酮衍生物及其抗血小板聚集的用途
CN102285951A (zh) * 2011-09-13 2011-12-21 辽宁亿灵科创生物医药科技有限公司 木犀草素衍生物及其预防和治疗心血管疾病的用途
CN103408525A (zh) * 2013-08-13 2013-11-27 商洛学院 一种黄酮类化合物的合成方法及其应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WEN LUO 等: "Design, synthesis and evaluation of novel 7-aminoalkyl-substituted flavonoid derivatives with improved cholinesterase inhibitory activities", 《BIOORGANIC & MEDICINAL CHEMISTRY》 *

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