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抗帕金森病药Istradefylline的合成 被引量:5
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作者 李凡 侯兴普 +2 位作者 李林 律涛 杜玉民 《中国医药工业杂志》 CAS CSCD 北大核心 2010年第4期241-243,共3页
香草醛经甲基化、Knoevenagel缩合、氯化亚砜氯代得(E)-3,4-二甲氧基苯丙烯酰氯,再与1,3-二乙基-5,6-二氨基尿嘧啶(7)经酰胺化、闭环及甲基化反应制得抗帕金森病药istradefylline。7可由N,N'-二乙基脲和氰乙酸经缩合闭环、亚硝化及... 香草醛经甲基化、Knoevenagel缩合、氯化亚砜氯代得(E)-3,4-二甲氧基苯丙烯酰氯,再与1,3-二乙基-5,6-二氨基尿嘧啶(7)经酰胺化、闭环及甲基化反应制得抗帕金森病药istradefylline。7可由N,N'-二乙基脲和氰乙酸经缩合闭环、亚硝化及还原反应制得。总收率约54%(以N,N'-二乙基脲计)。 展开更多
关键词 istradefylline 抗帕金森病药 腺苷A2a受体拮抗剂 合成
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Differences between Istradefylline Responders and Non-Responders in Parkinson’s Disease
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作者 Asako Yoritaka Nobutaka Hattori 《Advances in Parkinson's Disease》 2017年第2期45-51,共7页
Background: Istradefylline is a selective adenosine A2A receptor antagonist approved for Parkinson’s disease (PD) patients with wearing-off symptoms. The Japanese phase III trial showed that 20 mg of orally administr... Background: Istradefylline is a selective adenosine A2A receptor antagonist approved for Parkinson’s disease (PD) patients with wearing-off symptoms. The Japanese phase III trial showed that 20 mg of orally administrated istradefylline decreased the Off-time. However, istradefylline showed prominent effects in some patients and no benefits in others. We examined the differences in characteristics between responders and non-responders who received 8 weeks of 20 mg/day istradefylline. Methods: Thirty-one patients were enrolled (age, 65.4 [SD 10.4] years;disease duration, 10.4 [SD 6.1] years;daily levodopa dosage, 553.2 [SD 228.7] mg;frequency of levodopa consumption, 4.7 [SD 1.5] times;levodopa equivalent dose, 811.2 [SD 307.5] mg). Results: There were significant differences (p Conclusions: Younger or female patients who are not excessively sleepy during daytime are better candidates for the istradefylline therapy. 展开更多
关键词 Parkinson’s Disease istradefylline ADENOSINE A2A Receptor Antagonist WEARING-OFF SLEEPINESS
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Effectiveness of Istradefylline for Fatigue and Quality of Life in Parkinson’s Disease Patients’ and of Their Caregivers’
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作者 Kazuo Abe Masashi Fujita Hiroo Yoshikawa 《Advances in Parkinson's Disease》 2016年第2期24-28,共5页
Objectives: We evaluated efficacy and safety of istradefylline that is the first selective adenosine A2A receptor antagonist, for the treatment of non-motor symptoms and quality of life (QoL) in Parkinson’s disease (... Objectives: We evaluated efficacy and safety of istradefylline that is the first selective adenosine A2A receptor antagonist, for the treatment of non-motor symptoms and quality of life (QoL) in Parkinson’s disease (PD) patients with and QoL in their caregivers. Methods: This was a multisites study of 40 PD patients (female 24, male 16) who fully filled UK PD society brain bank clinical diagnostic criteria. They received istradefylline 20 mg/day for 8 weeks. We added istradefylline on the previous anti-Parkinson’s drugs. Clinical severities were evaluated by Hoehn-Yahr (H-Y) stage, unified PD rating scale (UPDRS), non-motor symptoms in PD (NMSPD), fatigue severity scale (FSS) and Euro QoL. Also, we evaluated their caregiver’s QoL by Euro QoL. Results: The scores of UPDRS part I improved from 1.3 ± 1.1 to 06 ± 0.9 (P = 0.18), part II improved from 11.9 ± 3.2 to 11.0 ± 3.1 (P = 0.17), part III improved from 34.8 ± 7.2 to 32.1 ± 8.3 (P = 0.105). There was no significant improvement or worsening of the H-Y stages. The scores of NMSPD improved from 49.9 ± 11.2 to 43.9 ± 10.6 (P = 0.08). The scores of FSS improved from 62.8 ± 7.1 to 52.3 ± 9.3 (P = 0.049). The total scores of Euro QoL in PD patients improved from 48.8 ± 14.9 to 57.2 ± 13.0 (P = 0.045). The total scores of Euro QoL in patients’ caregivers improved from 54.2 ± 11.0 to 59.8 ± 10.9 (P = 0.046). Conclusions: Our data demonstrated that istradefylline was associated with few side effects and was modestly effective for the treatment of non-motor symptoms especially fatigue that might improve QoL in PD patients as well as in their caregivers’. 展开更多
关键词 Parkinson’s Disease Non-Motor Symptoms istradefylline FATIGUE Quality of Life CAREGIVERS
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08029 阳性结果为istradefylline的美国申请奠定基础
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作者 张森(摘) 《国外药讯》 2006年第8期17-17,共1页
在三项国际Ⅲ期临床研究获得阳性结果之后,日本的协和发酵工业株式会社计划在今年下半年在美国为它的新帕金森病治疗药物istradefylline(KW-6002)(Ⅰ)提出新药申请。
关键词 istradefylline 阳性结果 美国 Ⅲ期临床研究 新药申请 治疗药物 帕金森病
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Istradefylline将是治疗帕金森病的新型药物 被引量:3
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作者 苏雅茹 蒋雨平 《中国临床神经科学》 2004年第1期85-88,共4页
KW 60 0 2 (Istradefylline)是选择性腺苷A2A受体 (A2AR)阻断剂 ,通过对纹状体苍白球通路的双重调节作用 ,逆转基底节直接通路和间接通路的失衡 ,改善帕金森病的运动困难、延长左旋多巴作用时间 ,但不增加异动症。KW 60 0 2对黑质多巴... KW 60 0 2 (Istradefylline)是选择性腺苷A2A受体 (A2AR)阻断剂 ,通过对纹状体苍白球通路的双重调节作用 ,逆转基底节直接通路和间接通路的失衡 ,改善帕金森病的运动困难、延长左旋多巴作用时间 ,但不增加异动症。KW 60 0 2对黑质多巴胺能神经元有神经保护作用。经临床试验证实 ,KW 60 0 展开更多
关键词 istradefylline 治疗 帕金森病 新型药物 腺苷A2A受体 KW-6002
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