CN105777657A - 一种治疗偏瘫的药物组合物 - Google Patents

一种治疗偏瘫的药物组合物 Download PDF

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CN105777657A
CN105777657A CN201610115213.8A CN201610115213A CN105777657A CN 105777657 A CN105777657 A CN 105777657A CN 201610115213 A CN201610115213 A CN 201610115213A CN 105777657 A CN105777657 A CN 105777657A
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hemiplegia
compound
pharmaceutical composition
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张宏业
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

本发明涉及一种治疗偏瘫的药物组合物，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

一种治疗偏瘫的药物组合物
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偏瘫的药物组合物。
背景技术
偏瘫又叫半身不遂，是指一侧上下肢、面肌和舌肌下部的运动障碍，是急性脑血管病的常见症状。轻度偏瘫病人虽然尚能活动，但走起路来，往往上肢屈曲，下肢伸直，瘫痪的下肢走一步划半个圈，这种特殊的走路姿势，叫做偏瘫步态。严重者常卧床不起，丧失生活能力。按照偏瘫的程度，可分为轻瘫、不完全性瘫痪和全瘫。轻瘫：表现为肌力减弱，肌力在4～5级，一般不影响日常生活，不完全性瘫较轻瘫重，范围较大，肌力2～4级，全瘫：肌力0～1级，瘫痪肢体完全不能活动。
发明内容
本发明的目的在于提供一种治疗偏瘫的药物组合物。
为了实现本发明的目的，本发明提供一种治疗偏瘫的化合物，该化合物具有下列结构：
本发明还提供一种治疗偏瘫的药物组合物，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偏瘫的药物中的用途，该化合物具有下列结构：
本发明的化合物对于偏瘫的效果显著，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。
实验例
目标化合物：
取SD大鼠(清洁级，体重180-220g，雄性)40只，于清洁级环境中适应性饲养。按ZeaLonga文献方法(LongaEZ,WeinsteinPR,CarlsonS,eta1.Reversiblemiddlecerebralarteryocclusionwithoutcraniotomyinrats[J].Stroke,1989,20(1):84-91)，选用大脑中动脉栓塞模型造模。
术前禁食12h，自由饮水。实验前腹注10％水合氯醛(0.35g/kg)麻醉，仰卧位固定，用烤灯维持肛温在36.5-37.0℃，分离右侧颈总动脉、颈外动脉和颈内动脉，结扎颈外动脉和颈总动脉。在颈总动脉靠近颈内动脉和颈外动脉分支处切口，将16-17mm长4-0尼龙线从切口处插入颈内动脉后结扎，完全插入即表示已插入大脑中动脉。空白对照组分离颈总动脉、颈内动脉和颈外动脉，结扎颈外动脉。动物手术清醒后有明显对侧Horner征及偏瘫体征显示造模成功。
手术后，动物保温28℃，单笼饲养。将造模大鼠随机均分为4组，每组10只，分别为正常对照组、模型对照组、阳性药(脑心通胶囊，陕西步长制药有限公司)组、目标化合物组。从造模前3d开始给药，1次/d，连续7d。各组给药量如下：正常组与模型组，给予生理盐水灌胃1mL/100g体重；阳性药组，脑心通胶囊内容物10g加1000mL生理盐水配制成混悬液，给予灌胃1mL/100g体重；目标化合物组，0.01g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。
检测项目
神经功能缺损评分：6组分别于术后1d、3d、7d进行神经功能缺损评分，按Longa5分评分标准评分(LongaEZ,WeinsteinPR,CarlsonS,eta1.Reversiblemiddlecerebralarteryocclusionwithoutcraniotomyinrats[J].Stroke,1989,20(1):84-91)。0分：无神经损伤症状；1分：不能完全伸展对侧前爪；2分：向外侧转圈；3分：向对侧倾斜；4分：不能自发行走，意识丧失。结果见下表。
组别 N 1d 3d 7d
正常组 10 0 0 0
模型组 10 2.52±0.28* 2.30±0.22* 1.76±0.15*
阳性药组 10 2.41±0.25*Δ 1.81±0.13*Δ 1.22±0.11*Δ
目标化合物组 10 2.10±0.16*Δ 1.20±0.11*Δ 1.01±0.10*Δ
和正常组比较，*P<0.05；和模型组比较，ΔP<0.05
与正常组比较，模型组及各治疗组神经功能缺损评分均显著升高；与模型组比较，治疗后神经功能缺损评分明显下降，说明均具有治疗效果。

Claims (7)

1.一种治疗偏瘫的化合物，其特征在于，该化合物具有下列结构：
2.一种治疗偏瘫的药物组合物，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所述的治疗偏瘫的药物组合物，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所述的治疗偏瘫的药物组合物，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所述的治疗偏瘫的药物组合物，其特征在于，所述稀释剂为乳糖。
6.根据权利要求3所述的治疗偏瘫的药物组合物，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.化合物在制备治疗偏瘫的药物中的用途，其特征在于，该化合物具有下列结构：
CN201610115213.8A 2016-03-01 2016-03-01 一种治疗偏瘫的药物组合物 Pending CN105777657A (zh)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101917849A (zh) * 2007-11-28 2010-12-15 达那-法伯癌症研究所 Bcr-abl的小分子豆蔻酸酯抑制剂及其使用方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101917849A (zh) * 2007-11-28 2010-12-15 达那-法伯癌症研究所 Bcr-abl的小分子豆蔻酸酯抑制剂及其使用方法

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
RABAB F.TAYYEM，ET AL.: "Ligand-based designing, in silico screening, and biological evaluation of new potent fructose-1,6-bisphosphatase (FBPase) inhibitors", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 *
STEPHEN W.WRIGHT，ET AL.: "Allosteric Inhibition of Fructose-1,6-bisphosphatase by Anilinoquinazolines", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *
VUONG N.TRIEU，ET AL.: "A Specific Inhibitor of Janus Kinase-3 Increases Survival in a Transgenic Mouse Model of Amyotrophic Lateral Sclerosis", 《BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS》 *

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